Bioequivalence assessment of generic products an innovative South African approach
- Walker, Roderick B, Kanfer, Isadore, Skinner, Michael F
- Authors: Walker, Roderick B , Kanfer, Isadore , Skinner, Michael F
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184256 , vital:44194 , xlink:href="https://doi.org/10.1080/10601330500534014"
- Description: Concurrent with the implementation of new legislation mandating Generic Substitution in South Africa, a new set of guidelines for bioavailability and bioequivalence have been published. Since one of the main objectives of the new legislation in South Africa relating to Generic Substitution is to ensure that medicines of high quality, safety, and efficacy are made more accessible and more affordable to the wider public, the need to speed up approval of such multi-source products has become a regulatory priority. In order to facilitate this process, various bioequivalence issues have been addressed including important issues such as the acceptance criteria and associated bioequivalence intervals, use of a foreign reference product and the issue of assessing highly variable drugs (HVDs). In addition, dispensations have been made with respect to food effect assessment and variability relating to genetic polymorphism in drug metabolism (genotyping/phenotyping). Furthermore, the use of “old” biostudies submitted in support of an application is subject to expiry date. Acceptance of appropriate data requires that specific criteria such as Cmax and AUC, in addition to the usual considerations, also meet the limits specified by the particular registration authority of the country where such products are intended to be marketed. Generally, these limits require that the 90% confidence interval (CI) for AUC and Cmax test/reference ratios lies within the acceptance interval of 0.80–1.25 calculated using log-transformed data. While such acceptance criteria are, in general, ubiquitous, some differences in acceptance criteria do exist between various countries. The new guidelines for bioavailability/bioequivalence studies developed by the South African regulatory authority, the Medicines Control Council (MCC), makes provision for highly variable drugs and the use of a non-South African reference product. The MCC requires that the acceptance criterion for Cmax ratios be set at 0.75–1.33 while maintaining AUC ratios at 0.80–1.25 using a 90% CI. Furthermore, provision is made to apply scaling based on average bioequivalence assessment and, as an interim measure, consideration has also been given to the use of a foreign reference product provided that equivalence between that product and the innovator product currently available on the South African market can be shown using in vitro testing.
- Full Text:
- Date Issued: 2006
- Authors: Walker, Roderick B , Kanfer, Isadore , Skinner, Michael F
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184256 , vital:44194 , xlink:href="https://doi.org/10.1080/10601330500534014"
- Description: Concurrent with the implementation of new legislation mandating Generic Substitution in South Africa, a new set of guidelines for bioavailability and bioequivalence have been published. Since one of the main objectives of the new legislation in South Africa relating to Generic Substitution is to ensure that medicines of high quality, safety, and efficacy are made more accessible and more affordable to the wider public, the need to speed up approval of such multi-source products has become a regulatory priority. In order to facilitate this process, various bioequivalence issues have been addressed including important issues such as the acceptance criteria and associated bioequivalence intervals, use of a foreign reference product and the issue of assessing highly variable drugs (HVDs). In addition, dispensations have been made with respect to food effect assessment and variability relating to genetic polymorphism in drug metabolism (genotyping/phenotyping). Furthermore, the use of “old” biostudies submitted in support of an application is subject to expiry date. Acceptance of appropriate data requires that specific criteria such as Cmax and AUC, in addition to the usual considerations, also meet the limits specified by the particular registration authority of the country where such products are intended to be marketed. Generally, these limits require that the 90% confidence interval (CI) for AUC and Cmax test/reference ratios lies within the acceptance interval of 0.80–1.25 calculated using log-transformed data. While such acceptance criteria are, in general, ubiquitous, some differences in acceptance criteria do exist between various countries. The new guidelines for bioavailability/bioequivalence studies developed by the South African regulatory authority, the Medicines Control Council (MCC), makes provision for highly variable drugs and the use of a non-South African reference product. The MCC requires that the acceptance criterion for Cmax ratios be set at 0.75–1.33 while maintaining AUC ratios at 0.80–1.25 using a 90% CI. Furthermore, provision is made to apply scaling based on average bioequivalence assessment and, as an interim measure, consideration has also been given to the use of a foreign reference product provided that equivalence between that product and the innovator product currently available on the South African market can be shown using in vitro testing.
- Full Text:
- Date Issued: 2006
Co-encapsulation of rifampicin and isoniazid in crude soybean lecithin liposomes
- Nkanga, Christian I, Noundou, Xavier S, Walker, Roderick B, Krause, Rui W M
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
- Full Text:
- Date Issued: 2019
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
- Full Text:
- Date Issued: 2019
Co-loading of isoniazid-grafted phthalocyanine-in-cyclodextrin and rifampicin in crude soybean lecithin liposomes: Formulation, spectroscopic and biological characterization
- Nkanga, Christian I, Roth, Michael, Walker, Roderick B, Noundou, Xavier S, Krause, Rui W M
- Authors: Nkanga, Christian I , Roth, Michael , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183481 , vital:43999 , xlink:href="https://doi.org/10.1166/jbn.2020.2880"
- Description: An inclusion complex of isoniazid-grafted phthalocyanine with gamma-cyclodextrin (Complex) was co-encapsulated with rifampicin (RIF) in crude soybean lecithin liposomes using a heating method. The encapsulation efficiency (%EE) of the Complex-RIF co-loaded liposomes (Rif-Complex-Lips) was determined using UV-Vis spectrophotometry. Rif-Complex-Lips formulations were evaluated using dynamic light scattering, transmission electron microscopy (TEM), 1H-NMR, absorption and emission spectroscopy. Dialysis was used for drug release study in two different media, pH 6.4 and 7.4. HeLa cells were used to assess potential cytotoxicity, and the uptake by lung fibroblasts and epithelial cells was investigated using fluorescence microscopy. The particle size and Zeta potential of Rif-Complex-Lips were approximately 594 nm and –50 mV. Spectroscopic analyses demonstrated molecular distribution of the cargo within the lipid core, and encapsulation efficiency of 58% for Complex and 86% for RIF. TEM analysis unveiled the existence of spherical nanoparticles in our samples, indicating the presence of liposomes. Rif-Complex-Lips exhibited much higher release rates for both INH and RIF at pH 6.4 compared to those tested at pH 7.4. In addition, there was no cytotoxicity on HeLa cells, but remarkable Rif-Complex-Lips internalization by peripheral lung fibroblasts and epithelial cells. Hence, Rif-Complex-Lips are promising vehicles for intracellular delivery of antimicrobial drugs.
- Full Text:
- Date Issued: 2020
- Authors: Nkanga, Christian I , Roth, Michael , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183481 , vital:43999 , xlink:href="https://doi.org/10.1166/jbn.2020.2880"
- Description: An inclusion complex of isoniazid-grafted phthalocyanine with gamma-cyclodextrin (Complex) was co-encapsulated with rifampicin (RIF) in crude soybean lecithin liposomes using a heating method. The encapsulation efficiency (%EE) of the Complex-RIF co-loaded liposomes (Rif-Complex-Lips) was determined using UV-Vis spectrophotometry. Rif-Complex-Lips formulations were evaluated using dynamic light scattering, transmission electron microscopy (TEM), 1H-NMR, absorption and emission spectroscopy. Dialysis was used for drug release study in two different media, pH 6.4 and 7.4. HeLa cells were used to assess potential cytotoxicity, and the uptake by lung fibroblasts and epithelial cells was investigated using fluorescence microscopy. The particle size and Zeta potential of Rif-Complex-Lips were approximately 594 nm and –50 mV. Spectroscopic analyses demonstrated molecular distribution of the cargo within the lipid core, and encapsulation efficiency of 58% for Complex and 86% for RIF. TEM analysis unveiled the existence of spherical nanoparticles in our samples, indicating the presence of liposomes. Rif-Complex-Lips exhibited much higher release rates for both INH and RIF at pH 6.4 compared to those tested at pH 7.4. In addition, there was no cytotoxicity on HeLa cells, but remarkable Rif-Complex-Lips internalization by peripheral lung fibroblasts and epithelial cells. Hence, Rif-Complex-Lips are promising vehicles for intracellular delivery of antimicrobial drugs.
- Full Text:
- Date Issued: 2020
Cyanide-induced free radical production and lipid peroxidation in rat brain homogenate is reduced by aspirin
- Daya, Santylal, Walker, Roderick B, Anoopkumar-Dukie, Shailendra
- Authors: Daya, Santylal , Walker, Roderick B , Anoopkumar-Dukie, Shailendra
- Date: 2000
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184346 , vital:44210 , xlink:href="https://doi.org/10.1007/BF02674529"
- Description: The neuroprotective properties of aspirin were investigated using cyanide-induced neurotoxicity as model. Cyanide, a known neurotoxic agent significantly increased lipid peroxidation and superoxide anion levels in rat brain homogenate in a concentration-dependent manner (0.25–1.0 mM). When homogenate, containing 1.0 mM KCN was cotreated with aspirin (1.0 mM) there was a significant decrease in lipid peroxidation. Aspirin (0.5 mM and 1.0 mM) also significantly reduced KCN-induced superoxide anion generation. The results of the present report therefore indicate a neuroprotective role for aspirin.
- Full Text:
- Date Issued: 2000
- Authors: Daya, Santylal , Walker, Roderick B , Anoopkumar-Dukie, Shailendra
- Date: 2000
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184346 , vital:44210 , xlink:href="https://doi.org/10.1007/BF02674529"
- Description: The neuroprotective properties of aspirin were investigated using cyanide-induced neurotoxicity as model. Cyanide, a known neurotoxic agent significantly increased lipid peroxidation and superoxide anion levels in rat brain homogenate in a concentration-dependent manner (0.25–1.0 mM). When homogenate, containing 1.0 mM KCN was cotreated with aspirin (1.0 mM) there was a significant decrease in lipid peroxidation. Aspirin (0.5 mM and 1.0 mM) also significantly reduced KCN-induced superoxide anion generation. The results of the present report therefore indicate a neuroprotective role for aspirin.
- Full Text:
- Date Issued: 2000
Design, evaluation and optimization of taste masked clarithromycin powder
- Ntemi, Pascal V, Walker, Roderick B, Khamanga, Sandile M
- Authors: Ntemi, Pascal V , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183503 , vital:44001 , xlink:href="https://doi.org/10.1691/ph.2019.8116"
- Description: Clarithromycin (CLA) is an extremely bitter macrolide antibiotic used to treat paediatric and adult infections. The bitter taste affects patient adherence and may compromise therapy. This research developed a taste masked CLA resinate using Indion® 234, a weak acidic cation exchange resin. The factors affecting formation of the CLA-resin complex were assessed. Design of experiments was used to optimize response while evaluating input variables such as temperature, CLA-resin ratio,stirring time and pH. CLA loading efficiency was determined spectrophotometrically and CLA release using USP Apparatus II. Differential Scanning Calorimetry (DSC), Scanning Electron Microscop (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy and X-ray Diffraction (XRD) were used to confirm complex formation. A spectrophotometric method was used to assess taste evaluation. The optimum CLA-resin ratio, temperature, and stirring time were 1:4, 80 °C, 3 hours, respectively, at pH 8. Characterization techniques revealed that CLA was crystalline and the complex amorphous in nature. FT-IR spectra of resinate revealed the absence of resonance due to the tertiary amine functional group that is responsible for the bitter taste of CLA. CLA was stable in simulated salivary fluid and was released within 3 hours in gastric fluid. All CLAresin batches revealed complete taste masking. Taste analysis highlighted the improvement of taste masking properties of the resinate as the CLA to resin ratio, increased.
- Full Text:
- Date Issued: 2019
- Authors: Ntemi, Pascal V , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183503 , vital:44001 , xlink:href="https://doi.org/10.1691/ph.2019.8116"
- Description: Clarithromycin (CLA) is an extremely bitter macrolide antibiotic used to treat paediatric and adult infections. The bitter taste affects patient adherence and may compromise therapy. This research developed a taste masked CLA resinate using Indion® 234, a weak acidic cation exchange resin. The factors affecting formation of the CLA-resin complex were assessed. Design of experiments was used to optimize response while evaluating input variables such as temperature, CLA-resin ratio,stirring time and pH. CLA loading efficiency was determined spectrophotometrically and CLA release using USP Apparatus II. Differential Scanning Calorimetry (DSC), Scanning Electron Microscop (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy and X-ray Diffraction (XRD) were used to confirm complex formation. A spectrophotometric method was used to assess taste evaluation. The optimum CLA-resin ratio, temperature, and stirring time were 1:4, 80 °C, 3 hours, respectively, at pH 8. Characterization techniques revealed that CLA was crystalline and the complex amorphous in nature. FT-IR spectra of resinate revealed the absence of resonance due to the tertiary amine functional group that is responsible for the bitter taste of CLA. CLA was stable in simulated salivary fluid and was released within 3 hours in gastric fluid. All CLAresin batches revealed complete taste masking. Taste analysis highlighted the improvement of taste masking properties of the resinate as the CLA to resin ratio, increased.
- Full Text:
- Date Issued: 2019
Design, Optimization, Manufacture and Characterization of Efavirenz-Loaded Flaxseed Oil Nanoemulsions
- Mazonde, Priveledge, Khamanga, Sandile M, Walker, Roderick B
- Authors: Mazonde, Priveledge , Khamanga, Sandile M , Walker, Roderick B
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183183 , vital:43919 , xlink:href="https://doi.org/10.3390/pharmaceutics12090797"
- Description: The formation, manufacture and characterization of low energy water-in-oil (w/o) nanoemulsions prepared using cold pressed flaxseed oil containing efavirenz was investigated. Pseudo-ternary phase diagrams were constructed to identify the nanoemulsion region(s). Other potential lipid-based drug delivery phases containing flaxseed oil with 1:1 m/m surfactant mixture of Tween® 80, Span® 20 and different amounts of ethanol were tested to characterize the impact of surfactant mixture on emulsion formation. Flaxseed oil was used as the oil phase as efavirenz exhibited high solubility in the vehicle when compared to other vegetable oils tested. Optimization of surfactant mixtures was undertaken using design of experiments, specifically a D-optimal design with the flaxseed oil content set at 10% m/m. Two solutions from the desired optimization function were produced based on desirability and five nanoemulsion formulations were produced and characterized in terms of in vitro release of efavirenz, physical and chemical stability. Metastable nanoemulsions containing 10% m/m flaxseed oil were successfully manufactured and significant isotropic gel (semisolid) and o/w emulsions were observed during phase behavior studies. Droplet sizes ranged between 156 and 225 nm, zeta potential between −24 and −41 mV and all formulations were found to be monodisperse with polydispersity indices ≤ 0.487.
- Full Text:
- Date Issued: 2020
- Authors: Mazonde, Priveledge , Khamanga, Sandile M , Walker, Roderick B
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183183 , vital:43919 , xlink:href="https://doi.org/10.3390/pharmaceutics12090797"
- Description: The formation, manufacture and characterization of low energy water-in-oil (w/o) nanoemulsions prepared using cold pressed flaxseed oil containing efavirenz was investigated. Pseudo-ternary phase diagrams were constructed to identify the nanoemulsion region(s). Other potential lipid-based drug delivery phases containing flaxseed oil with 1:1 m/m surfactant mixture of Tween® 80, Span® 20 and different amounts of ethanol were tested to characterize the impact of surfactant mixture on emulsion formation. Flaxseed oil was used as the oil phase as efavirenz exhibited high solubility in the vehicle when compared to other vegetable oils tested. Optimization of surfactant mixtures was undertaken using design of experiments, specifically a D-optimal design with the flaxseed oil content set at 10% m/m. Two solutions from the desired optimization function were produced based on desirability and five nanoemulsion formulations were produced and characterized in terms of in vitro release of efavirenz, physical and chemical stability. Metastable nanoemulsions containing 10% m/m flaxseed oil were successfully manufactured and significant isotropic gel (semisolid) and o/w emulsions were observed during phase behavior studies. Droplet sizes ranged between 156 and 225 nm, zeta potential between −24 and −41 mV and all formulations were found to be monodisperse with polydispersity indices ≤ 0.487.
- Full Text:
- Date Issued: 2020
Development and assessment of a USP Apparatus 3 dissolution test method for sustained-release Nevirapine matrix tablets
- Mwila, Chiluba, Khamanga, Sandile M M, Walker, Roderick B
- Authors: Mwila, Chiluba , Khamanga, Sandile M M , Walker, Roderick B
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184779 , vital:44271 , xlink:href="https://doi.org/10.14227/dt230316p22"
- Description: Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5–10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.
- Full Text:
- Date Issued: 2016
- Authors: Mwila, Chiluba , Khamanga, Sandile M M , Walker, Roderick B
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184779 , vital:44271 , xlink:href="https://doi.org/10.14227/dt230316p22"
- Description: Dissolution testing is a quality control tool used to assess batch-to-batch performance of dosage forms, thereby providing continued assurance of product quality. Analytical methods for the assessment of pharmaceutical product quality must be validated according to regulatory guidelines to ensure that tests are reliable and valid. Agitation rate, mesh pore size, surfactant concentration, and dissolution medium molarity are experimental parameters that may affect nevirapine (NVP) release and were investigated and optimized to ensure that consistent, reliable, and valid results using Apparatus 3 were produced. Agitation rate was investigated to establish an equivalent response to that observed for NVP release using Apparatus 2 at 50 rpm. A reciprocation rate of 5–10 dpm produced dissolution profiles that were similar to those observed using Apparatus 2. An increase in the molarity of the dissolution medium slightly increased the release rate of NVP, and a 50 mM buffer maintained at pH values mimicking gastrointestinal tract (GIT) conditions was selected for all experiments. With the addition of 2% sodium lauryl sulfate (SLS) to the dissolution medium, >80% NVP was released from the tablets over the test period. The NVP release rate increased with an increase in the mesh pore size; however, the extent of release was not affected by this parameter. Dissolution test samples were analyzed using HPLC, and dissolution methods were validated for NVP stability in the dissolution medium, specificity, linearity and range, repeatability, intermediate precision, and accuracy as defined by ICH. The dissolution method used for testing NVP tablets can be regarded as an appropriate tool for the evaluation of sustained-release (SR) NVP formulations and the impact of formulation composition and product quality attributes on drug release.
- Full Text:
- Date Issued: 2016
Development and validation of a stability-indicating analytical method for the quantitation of oxytocin in pharmaceutical dosage forms
- Chaibva, Faith A, Walker, Roderick B
- Authors: Chaibva, Faith A , Walker, Roderick B
- Date: 2006
- Language: English
- Type: Article
- Identifier: vital:6349 , http://hdl.handle.net/10962/d1006030
- Description: A single stability-indicating assay for oxytocin (OT) in pharmaceutical dosage forms using gradient elution over 21 min has been reported in the literature. Furthermore, published and compendial methods for the analysis of OT containing dosage forms also involve using HPLC with gradient elution and complicated mobile phases that include hydrophobic ion pairing agents. A simple isocratic and stability-indicating assay was developed and validated. The conditions are as follows, column: Phenomenex® C18 Hypersil, 5 μm packing, 4.6 mm × 150 mm with acetonitrile–phosphate buffer (pH 5; 0.08 M) (20:80) as the mobile phase with UV detection at 220 nm The method was found to be specific for OT in the presence of degradation products and chlorbutol (preservative) with an overall analytical run time of 16 min. Accuracy was determined to be 0.77–1.18% bias for all samples tested. Intra-assay precision (repeatability) was found to be 0.22–1.04%R.S.D. while the inter-day precision (intermediate precision) was found to be 1.27–1.68%R.S.D. for the samples studied. The calibration curve was found to be linear with the equation y = 1.81x + 0.02 and a linear regression coefficient of 0.9991 over the range 0.4–12.0 IU/ml. The LOD and the LOQ were determined to be 0.1 and 0.4 IU/ml, respectively. Syntocinon®, a commercially available dosage form of OT was assayed resulting in 100.5–106.6% recovery of the label claim and an average of 10.04 IU/ml.
- Full Text:
- Date Issued: 2006
- Authors: Chaibva, Faith A , Walker, Roderick B
- Date: 2006
- Language: English
- Type: Article
- Identifier: vital:6349 , http://hdl.handle.net/10962/d1006030
- Description: A single stability-indicating assay for oxytocin (OT) in pharmaceutical dosage forms using gradient elution over 21 min has been reported in the literature. Furthermore, published and compendial methods for the analysis of OT containing dosage forms also involve using HPLC with gradient elution and complicated mobile phases that include hydrophobic ion pairing agents. A simple isocratic and stability-indicating assay was developed and validated. The conditions are as follows, column: Phenomenex® C18 Hypersil, 5 μm packing, 4.6 mm × 150 mm with acetonitrile–phosphate buffer (pH 5; 0.08 M) (20:80) as the mobile phase with UV detection at 220 nm The method was found to be specific for OT in the presence of degradation products and chlorbutol (preservative) with an overall analytical run time of 16 min. Accuracy was determined to be 0.77–1.18% bias for all samples tested. Intra-assay precision (repeatability) was found to be 0.22–1.04%R.S.D. while the inter-day precision (intermediate precision) was found to be 1.27–1.68%R.S.D. for the samples studied. The calibration curve was found to be linear with the equation y = 1.81x + 0.02 and a linear regression coefficient of 0.9991 over the range 0.4–12.0 IU/ml. The LOD and the LOQ were determined to be 0.1 and 0.4 IU/ml, respectively. Syntocinon®, a commercially available dosage form of OT was assayed resulting in 100.5–106.6% recovery of the label claim and an average of 10.04 IU/ml.
- Full Text:
- Date Issued: 2006
Development and validation of a stability-indicating method for the quantitation of paclitaxel in pharmaceutical dosage forms
- Mohammadi, Ali, Esimaeili, Farnaz, Dinarvand, Rasoul, Atyabi, Fatemeh, Walker, Roderick B
- Authors: Mohammadi, Ali , Esimaeili, Farnaz , Dinarvand, Rasoul , Atyabi, Fatemeh , Walker, Roderick B
- Date: 2009
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184278 , vital:44196 , xlink:href="https://doi.org/10.1093/chromsci/47.7.599"
- Description: A simple, rapid stability-indicating isocratic assay has been developed and validated for the determination of Paclitaxel (PTX) in commercial injection formulations. The assay is performed using a Nucleosil RP-18 (5 µm, 250 × 4.0 mm i.d) column protected by a Nucleosil C18 precolumn (5 µm, 4.0 × 4.0 mm i.d.) with a mobile phase of methanol–water (80:20) and UV detection at 230 nm. The method was found to be specific for PTX in the presence of degradation products with an overall analytical run time of ~ 9 min. Accuracy reported as % bias was found to be 0.1–2.5% bias for all samples tested. Intra-assay precision (repeatability) was found to be 0.22–2.65% RSD, while inter-day precision (intermediate precision) was found to be 1.0–3.0% RSD for the samples studied. The calibration curve was found to be linear with the equation y = 29.78x + 7.65, and a linear regression coefficient of 0.9994 over the concentration range 0.05–20 µg/mL. The limits of quantitation and detection were 0.05 and 0.02 µg/mL, respectively. Taxol (30 mg/5 mL), a commercially available dosage form of PTX, was assayed and 100.6–103.6% of the label claim was recovered.
- Full Text:
- Date Issued: 2009
- Authors: Mohammadi, Ali , Esimaeili, Farnaz , Dinarvand, Rasoul , Atyabi, Fatemeh , Walker, Roderick B
- Date: 2009
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184278 , vital:44196 , xlink:href="https://doi.org/10.1093/chromsci/47.7.599"
- Description: A simple, rapid stability-indicating isocratic assay has been developed and validated for the determination of Paclitaxel (PTX) in commercial injection formulations. The assay is performed using a Nucleosil RP-18 (5 µm, 250 × 4.0 mm i.d) column protected by a Nucleosil C18 precolumn (5 µm, 4.0 × 4.0 mm i.d.) with a mobile phase of methanol–water (80:20) and UV detection at 230 nm. The method was found to be specific for PTX in the presence of degradation products with an overall analytical run time of ~ 9 min. Accuracy reported as % bias was found to be 0.1–2.5% bias for all samples tested. Intra-assay precision (repeatability) was found to be 0.22–2.65% RSD, while inter-day precision (intermediate precision) was found to be 1.0–3.0% RSD for the samples studied. The calibration curve was found to be linear with the equation y = 29.78x + 7.65, and a linear regression coefficient of 0.9994 over the concentration range 0.05–20 µg/mL. The limits of quantitation and detection were 0.05 and 0.02 µg/mL, respectively. Taxol (30 mg/5 mL), a commercially available dosage form of PTX, was assayed and 100.6–103.6% of the label claim was recovered.
- Full Text:
- Date Issued: 2009
Development and Validation of a Stability-indicating RP-HPLC Method Using Quality by Design for Estimating Captopril
- Veerubhotla, Krishna, Walker, Roderick B
- Authors: Veerubhotla, Krishna , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183525 , vital:44003 , xlink:href="10.4172/pharmaceutical-sciences.1000478"
- Description: The applicability of a quality by design framework for the development of a sensitive, simple and selective, stability-indicating reversed-phase high-performance liquid chromatography analytical method for the analysis of captopril was investigated. Design of experiments using a central composite design approach was used for method development. Twenty experimental runs were performed with acetonitrile content ranging between 28 and 36 % v/v, pH from 2.8 to 3.6 and temperature between 22° and 32°. The experimental data obtained was used to derive a quadratic model for the retention time of captopril. The optimized method produced sharp peaks with good resolution (>2) for captopril and the internal standard with retention times of 3.1 and 6.2 min, respectively. The experimental data revealed that acetonitrile content in the mobile phase and pH are significant factors that affect the retention time and resolution of captopril. Normal probability plots revealed that the residual and predicted data fall approximately on a straight line, indicating that the experimental error for these studies was evenly distributed suggesting that the model could be used to navigate the design space. This approach is useful to expedite method development and optimization activities in analytical laboratories.
- Full Text:
- Date Issued: 2019
- Authors: Veerubhotla, Krishna , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183525 , vital:44003 , xlink:href="10.4172/pharmaceutical-sciences.1000478"
- Description: The applicability of a quality by design framework for the development of a sensitive, simple and selective, stability-indicating reversed-phase high-performance liquid chromatography analytical method for the analysis of captopril was investigated. Design of experiments using a central composite design approach was used for method development. Twenty experimental runs were performed with acetonitrile content ranging between 28 and 36 % v/v, pH from 2.8 to 3.6 and temperature between 22° and 32°. The experimental data obtained was used to derive a quadratic model for the retention time of captopril. The optimized method produced sharp peaks with good resolution (>2) for captopril and the internal standard with retention times of 3.1 and 6.2 min, respectively. The experimental data revealed that acetonitrile content in the mobile phase and pH are significant factors that affect the retention time and resolution of captopril. Normal probability plots revealed that the residual and predicted data fall approximately on a straight line, indicating that the experimental error for these studies was evenly distributed suggesting that the model could be used to navigate the design space. This approach is useful to expedite method development and optimization activities in analytical laboratories.
- Full Text:
- Date Issued: 2019
Development of a stability-indicating high performance liquid chromatographic method for the analysis of topiramate and dissolution rate testing in topiramate tablets
- Mohammadi, Ali, Rezanour, Nasrin, Ansari Dogaheh, M, Walker, Roderick B
- Authors: Mohammadi, Ali , Rezanour, Nasrin , Ansari Dogaheh, M , Walker, Roderick B
- Date: 2010
- Language: English
- Type: text , Article
- Identifier: vital:6412 , http://hdl.handle.net/10962/d1006507
- Description: A stability-indicating high performance liquid chromatographic(HPLC) method was developed and validated for the quantitation and dissolution determination of topiramate in tablet dosage forms. An isocratic separation was achieved using a phenyl column with a flow rate of 1 mL/min using UV detection at 264 nm. Topiramate has low UV absorbtivity and was subjected to derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). The mobile phase for the separation consisted of acetonitrile: 50 mM sodium dihydrogen phosphate(NaH2PO4) containing 3 % v/v triethylamine (pH 2.8) in a 48:52 v/v ratio. Topiramate was subjected to oxidation, hydrolysis, photolysis and heat for the purposes of stress testing. Separation was achieved for the parent compound and all the degradation products in an overall analytical run time of approximately 15 min with the parent compound topiramate eluting at approximately 9.2 min. The method was linear over the concentration range of 1-100 μg/mL (r = 0.9996) with limits of quantitation and detection of 1 and 0.3 μg/mL, respectively.
- Full Text:
- Date Issued: 2010
- Authors: Mohammadi, Ali , Rezanour, Nasrin , Ansari Dogaheh, M , Walker, Roderick B
- Date: 2010
- Language: English
- Type: text , Article
- Identifier: vital:6412 , http://hdl.handle.net/10962/d1006507
- Description: A stability-indicating high performance liquid chromatographic(HPLC) method was developed and validated for the quantitation and dissolution determination of topiramate in tablet dosage forms. An isocratic separation was achieved using a phenyl column with a flow rate of 1 mL/min using UV detection at 264 nm. Topiramate has low UV absorbtivity and was subjected to derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). The mobile phase for the separation consisted of acetonitrile: 50 mM sodium dihydrogen phosphate(NaH2PO4) containing 3 % v/v triethylamine (pH 2.8) in a 48:52 v/v ratio. Topiramate was subjected to oxidation, hydrolysis, photolysis and heat for the purposes of stress testing. Separation was achieved for the parent compound and all the degradation products in an overall analytical run time of approximately 15 min with the parent compound topiramate eluting at approximately 9.2 min. The method was linear over the concentration range of 1-100 μg/mL (r = 0.9996) with limits of quantitation and detection of 1 and 0.3 μg/mL, respectively.
- Full Text:
- Date Issued: 2010
Development, manufacture and characterization of niosomes for the delivery for nevirapine
- Witika, Bwalya A, Walker, Roderick B
- Authors: Witika, Bwalya A , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183514 , vital:44002 , xlink:href="https://doi.org/10.1691/ph.2019.8168"
- Description: Nevirapine (NVP), used for the treatment of HIV/AIDS, exhibits unpredictable oral bioavailability, has a poor side effect profile and requires frequent dosing. Niosomes are novel drug delivery systems that have the potential to overcome these challenges. A thin layer hydration approach was used to produce niosomes and optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) establish and identify parameters that may affect the manufacture of niosomes. The impact of cholesterol and surfactant content, hydration time and temperature on manufacture was investigated. Critical quality attributes (CQA) in respect of particle size (PS), entrapment efficiency (EE), polydispersity index (PDI) and the amount of NVP released at 48 hours was also assessed. The optimised niosome composition was identified and manufactured and the CQA characterised prior to placing the batch on stability for 12 weeks at 4±2 °C and 22±2 °C. The PS, PDI, EE and % NVP released at 48 h was 523.36±23.16 nm, 0.386±0.054, 96.8 % and 25.3 % for niosomes manufactured with Span® 20. Similarly, the parameters were 502.87±21.77 nm and 0.394±0.027, 98.0 % and 25.0 % for mean PS, PDI, EE and %NVP released at 48 h for Span® 80 niosomes. All characterisation was undertaken on the day of manufacture. In conclusion, a simple, cheap, rapid and precise method of manufacture of NVP niosomes was developed, validated and optimised using DoE and RSM and the product exhibited the target CQA.
- Full Text:
- Date Issued: 2019
- Authors: Witika, Bwalya A , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183514 , vital:44002 , xlink:href="https://doi.org/10.1691/ph.2019.8168"
- Description: Nevirapine (NVP), used for the treatment of HIV/AIDS, exhibits unpredictable oral bioavailability, has a poor side effect profile and requires frequent dosing. Niosomes are novel drug delivery systems that have the potential to overcome these challenges. A thin layer hydration approach was used to produce niosomes and optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) establish and identify parameters that may affect the manufacture of niosomes. The impact of cholesterol and surfactant content, hydration time and temperature on manufacture was investigated. Critical quality attributes (CQA) in respect of particle size (PS), entrapment efficiency (EE), polydispersity index (PDI) and the amount of NVP released at 48 hours was also assessed. The optimised niosome composition was identified and manufactured and the CQA characterised prior to placing the batch on stability for 12 weeks at 4±2 °C and 22±2 °C. The PS, PDI, EE and % NVP released at 48 h was 523.36±23.16 nm, 0.386±0.054, 96.8 % and 25.3 % for niosomes manufactured with Span® 20. Similarly, the parameters were 502.87±21.77 nm and 0.394±0.027, 98.0 % and 25.0 % for mean PS, PDI, EE and %NVP released at 48 h for Span® 80 niosomes. All characterisation was undertaken on the day of manufacture. In conclusion, a simple, cheap, rapid and precise method of manufacture of NVP niosomes was developed, validated and optimised using DoE and RSM and the product exhibited the target CQA.
- Full Text:
- Date Issued: 2019
Drug transport mechanisms from carbopol/eudragit verapamil sustained-release tablets
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184801 , vital:44273 , xlink:href="https://doi.org/10.14227/dt180311p30"
- Description: The objectives of this study were to compare dissolution profiles of a verapamil (VRP) formulation manufactured inhouse and Isoptin SR using USP Apparatus 2 and 3 and to elucidate drug release kinetics of these dosage forms. Eudragit NE 30D (ethyl acrylate–methyl methacrylate copolymer in a 2:1 ratio) aqueous dispersion was used as a granulating binder for the manufacture of VRP mini-matrix sustained-release tablets. The wet granulation process was performed to prepare free-flowing granules that were blended with Carbopol. The tablets were manufactured using a single-punch press by compression of the granules with magnesium stearate as a lubricant. Drug release was determined in phosphate buffer solution using USP Apparatus 2 and 3. Dissolution data were fitted to zero- and first-order models; in addition, the kinetic data were determined by evaluation of Higuchi release kinetics. The mechanism of drug release was established using the Korsmeyer–Peppas model. In general, all tablets showed high mechanical resistance with less than 1% friability. There was no significant difference between the dissolution profiles of the formulation manufactured in-house and the commercially available product. The release mechanism of the formulated and marketed products was controlled by anomalous non-Fickian diffusion. VRP release was prolonged for 12 h indicating the usefulness of the formulation as a twice-daily dosage form. The mechanism of drug release for the dosage forms was unaffected by the choice of apparatus.
- Full Text:
- Date Issued: 2011
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184801 , vital:44273 , xlink:href="https://doi.org/10.14227/dt180311p30"
- Description: The objectives of this study were to compare dissolution profiles of a verapamil (VRP) formulation manufactured inhouse and Isoptin SR using USP Apparatus 2 and 3 and to elucidate drug release kinetics of these dosage forms. Eudragit NE 30D (ethyl acrylate–methyl methacrylate copolymer in a 2:1 ratio) aqueous dispersion was used as a granulating binder for the manufacture of VRP mini-matrix sustained-release tablets. The wet granulation process was performed to prepare free-flowing granules that were blended with Carbopol. The tablets were manufactured using a single-punch press by compression of the granules with magnesium stearate as a lubricant. Drug release was determined in phosphate buffer solution using USP Apparatus 2 and 3. Dissolution data were fitted to zero- and first-order models; in addition, the kinetic data were determined by evaluation of Higuchi release kinetics. The mechanism of drug release was established using the Korsmeyer–Peppas model. In general, all tablets showed high mechanical resistance with less than 1% friability. There was no significant difference between the dissolution profiles of the formulation manufactured in-house and the commercially available product. The release mechanism of the formulated and marketed products was controlled by anomalous non-Fickian diffusion. VRP release was prolonged for 12 h indicating the usefulness of the formulation as a twice-daily dosage form. The mechanism of drug release for the dosage forms was unaffected by the choice of apparatus.
- Full Text:
- Date Issued: 2011
DSC screening of potential prochlorperazine-excipient interactions in preformulation studies
- Brown, Michael E, Antunes, Edith M, Glass, Beverley M, Lebete, Mosimotsana L, Walker, Roderick B
- Authors: Brown, Michael E , Antunes, Edith M , Glass, Beverley M , Lebete, Mosimotsana L , Walker, Roderick B
- Date: 1999
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184367 , vital:44212 , xlink:href="https://doi.org/10.1023/A:1010150305542"
- Description: Differential scanning calorimetry was used to examine the thermal behaviour of mixtures of the drug prochlorperazine with standard excipients, to assess potential interactions, and of mixtures with cyclodextrins, to investigate inclusion complexation which could increase the photostability of the drug. For most of the excipients (magnesium stearate, stearic acid, Explotab®, Ac-Di-Sol®, Encompress® and Ludipress®, lactose and Starch 1500) disappearance or broadening of the melting endotherm of the drug indicated interactions. Lubritab® was the only 'inert' excipient tested. Mixtures of prochlorperazine and the cyclodextrins gave incomplete inclusion complexation as shown by only partial disappearance of the melting endotherm of the drug.
- Full Text: false
- Date Issued: 1999
- Authors: Brown, Michael E , Antunes, Edith M , Glass, Beverley M , Lebete, Mosimotsana L , Walker, Roderick B
- Date: 1999
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184367 , vital:44212 , xlink:href="https://doi.org/10.1023/A:1010150305542"
- Description: Differential scanning calorimetry was used to examine the thermal behaviour of mixtures of the drug prochlorperazine with standard excipients, to assess potential interactions, and of mixtures with cyclodextrins, to investigate inclusion complexation which could increase the photostability of the drug. For most of the excipients (magnesium stearate, stearic acid, Explotab®, Ac-Di-Sol®, Encompress® and Ludipress®, lactose and Starch 1500) disappearance or broadening of the melting endotherm of the drug indicated interactions. Lubritab® was the only 'inert' excipient tested. Mixtures of prochlorperazine and the cyclodextrins gave incomplete inclusion complexation as shown by only partial disappearance of the melting endotherm of the drug.
- Full Text: false
- Date Issued: 1999
Electropolymerized Fluorinated Aniline-Based Fiber for Headspace Solid-Phase Microextraction and Gas Chromatographic Determination of Benzaldehyde in Injectable Pharmaceutical Formulations
- Mohammadi, Ali, Mohammadi, Somayeh, Moghaddam, Bayandori A, Masoumi, Vahideh, Walker, Roderick B
- Authors: Mohammadi, Ali , Mohammadi, Somayeh , Moghaddam, Bayandori A , Masoumi, Vahideh , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184120 , vital:44175 , xlink:href="https://doi.org/10.1093/chromsci/bmt152"
- Description: In this study, a simple method was developed and validated to detect trace levels of benzaldehyde in injectable pharmaceutical formulations by solid-phase microextraction coupled with gas chromatography–flame ionization detector. Polyaniline was electrodeposited on a platinum wire in trifluoroacetic acid solvent by cyclic voltammetry technique. This fiber shows high thermal and mechanical stability and high performance in extraction of benzaldehyde. Extraction and desorption time and temperature, salt effect and gas chromatography parameters were optimized as key parameters. At the optimum conditions, the fiber shows good linearity between peak area ratio of benzaldehyde/3-chlorobenzaldehyde and benzaldehyde concentration in the range of 50–800 ng/mL with percent relative standard deviation values ranging from 0.75 to 8.64% (n 5 3). The limits of quantitation and detection were 50 and 16 ng/mL, respectively. The method has the requisite selectivity, sensitivity, accuracy and precision to assay benzaldehyde in injectable pharmaceutical dosage forms.
- Full Text:
- Date Issued: 2014
- Authors: Mohammadi, Ali , Mohammadi, Somayeh , Moghaddam, Bayandori A , Masoumi, Vahideh , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184120 , vital:44175 , xlink:href="https://doi.org/10.1093/chromsci/bmt152"
- Description: In this study, a simple method was developed and validated to detect trace levels of benzaldehyde in injectable pharmaceutical formulations by solid-phase microextraction coupled with gas chromatography–flame ionization detector. Polyaniline was electrodeposited on a platinum wire in trifluoroacetic acid solvent by cyclic voltammetry technique. This fiber shows high thermal and mechanical stability and high performance in extraction of benzaldehyde. Extraction and desorption time and temperature, salt effect and gas chromatography parameters were optimized as key parameters. At the optimum conditions, the fiber shows good linearity between peak area ratio of benzaldehyde/3-chlorobenzaldehyde and benzaldehyde concentration in the range of 50–800 ng/mL with percent relative standard deviation values ranging from 0.75 to 8.64% (n 5 3). The limits of quantitation and detection were 50 and 16 ng/mL, respectively. The method has the requisite selectivity, sensitivity, accuracy and precision to assay benzaldehyde in injectable pharmaceutical dosage forms.
- Full Text:
- Date Issued: 2014
Electro‐oxidation of acetaminophen on nickel/poly (o‐aminophenol)/multi‐walled carbon nanotube nanocomposite modified graphite electrode.
- Naeemy, Ali, Mohammadi, Ali, Bakhtiari, Hediech, Ashouri, Nasim, Walker, Roderick B
- Authors: Naeemy, Ali , Mohammadi, Ali , Bakhtiari, Hediech , Ashouri, Nasim , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184107 , vital:44173 , xlink:href="https://ietresearch.onlinelibrary.wiley.com/doi/pdf/10.1049/mnl.2014.0197"
- Description: Poly(o-aminophenol) (POAP)/multi-walled carbon nanotube (MWCNT) nanocomposite and POAP in the absence of the MWCNT were fabricated by consecutive cyclic voltammetry (CV) on a graphite (G) electrode. The dispersion of nickel (II) ions was accomplished and incorporated into the polymeric electrodes (G/POAP and G/POAP-MWCNT) by immersing them into a 0.1 M nickel (II) solution. Following preparation of G/POAP/Ni and G/POAP-MWCNT/Ni, the electrochemical behaviour was examined using CV. Scanning electron microscopy was used for characterisation of the nanocomposite. The prepared electrodes showed enhanced electrocatalytic activity for the oxidation of acetaminophen and facilitated the detection of acetaminophen in a 0.1 M NaOH solution. Compared with the G/POAP/Ni electrode, the G/POAP-MWCNT/Ni electrode had a significant current response of acetaminophen oxidation because of the synergistic effects of POAP and the MWCNT. By CV, the calibration plot was linear in the range of 1–13 mM with standard deviation between 0.3 and 6.54% for acetaminophen. The G/POAP-MWCNT/Ni was successfully applied for acetaminophen determination in tablets and the results showed sufficient precision and achieved a mean recovery of 96.8% (R.S.D. = 4.9%).
- Full Text:
- Date Issued: 2014
- Authors: Naeemy, Ali , Mohammadi, Ali , Bakhtiari, Hediech , Ashouri, Nasim , Walker, Roderick B
- Date: 2014
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184107 , vital:44173 , xlink:href="https://ietresearch.onlinelibrary.wiley.com/doi/pdf/10.1049/mnl.2014.0197"
- Description: Poly(o-aminophenol) (POAP)/multi-walled carbon nanotube (MWCNT) nanocomposite and POAP in the absence of the MWCNT were fabricated by consecutive cyclic voltammetry (CV) on a graphite (G) electrode. The dispersion of nickel (II) ions was accomplished and incorporated into the polymeric electrodes (G/POAP and G/POAP-MWCNT) by immersing them into a 0.1 M nickel (II) solution. Following preparation of G/POAP/Ni and G/POAP-MWCNT/Ni, the electrochemical behaviour was examined using CV. Scanning electron microscopy was used for characterisation of the nanocomposite. The prepared electrodes showed enhanced electrocatalytic activity for the oxidation of acetaminophen and facilitated the detection of acetaminophen in a 0.1 M NaOH solution. Compared with the G/POAP/Ni electrode, the G/POAP-MWCNT/Ni electrode had a significant current response of acetaminophen oxidation because of the synergistic effects of POAP and the MWCNT. By CV, the calibration plot was linear in the range of 1–13 mM with standard deviation between 0.3 and 6.54% for acetaminophen. The G/POAP-MWCNT/Ni was successfully applied for acetaminophen determination in tablets and the results showed sufficient precision and achieved a mean recovery of 96.8% (R.S.D. = 4.9%).
- Full Text:
- Date Issued: 2014
Encapsulation and physicochemical evaluation of efavirenz in liposomes
- Okafor, Nnamdi Ikemefuna, Nkanga, Christian I, Walker, Roderick B, Noundou, Xavier S, Krause, Rui W M
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
Enhancement of Biological and Pharmacological Properties of an Encapsulated Polyphenol: Curcumin
- Witika, Bwalya A, Makoni, Pedzisai A, Matafwali, Scott K, Mweetwa, Larry L, Shandele, Ginnethon C, Walker, Roderick B
- Authors: Witika, Bwalya A , Makoni, Pedzisai A , Matafwali, Scott K , Mweetwa, Larry L , Shandele, Ginnethon C , Walker, Roderick B
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183161 , vital:43917 , xlink:href="https://doi.org/10.3390/molecules26144244"
- Description: There is a dearth of natural remedies available for the treatment of an increasing number of diseases facing mankind. Natural products may provide an opportunity to produce formulations and therapeutic solutions to address this shortage. Curcumin (CUR), diferuloylmethane; I,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione is the major pigment in turmeric powder which has been reported to exhibit a number of health benefits including, antibacterial, antiviral, anti-cancer, anti-inflammatory and anti-oxidant properties. In this review, the authors attempt to highlight the biological and pharmacological properties of CUR in addition to emphasizing aspects relating to the biosynthesis, encapsulation and therapeutic effects of the compound. The information contained in this review was generated by considering published information in which evidence of enhanced biological and pharmacological properties of nano-encapsulated CUR was reported. CUR has contributed to a significant improvement in melanoma, breast, lung, gastro-intestinal, and genito-urinary cancer therapy. We highlight the impact of nano-encapsulated CUR for efficient inhibition of cell proliferation, even at low concentrations compared to the free CUR when considering anti-proliferation. Furthermore nano-encapsulated CUR exhibited bioactive properties, exerted cytotoxic and anti-oxidant effects by acting on endogenous and cholinergic anti-oxidant systems. CUR was reported to block Hepatitis C virus (HCV) entry into hepatic cells, inhibit MRSA proliferation, enhance wound healing and reduce bacterial load. Nano-encapsulated CUR has also shown bioactive properties when acting on antioxidant systems (endogenous and cholinergic). Future research is necessary and must focus on investigation of encapsulated CUR nano-particles in different models of human pathology.
- Full Text:
- Date Issued: 2021
- Authors: Witika, Bwalya A , Makoni, Pedzisai A , Matafwali, Scott K , Mweetwa, Larry L , Shandele, Ginnethon C , Walker, Roderick B
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183161 , vital:43917 , xlink:href="https://doi.org/10.3390/molecules26144244"
- Description: There is a dearth of natural remedies available for the treatment of an increasing number of diseases facing mankind. Natural products may provide an opportunity to produce formulations and therapeutic solutions to address this shortage. Curcumin (CUR), diferuloylmethane; I,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione is the major pigment in turmeric powder which has been reported to exhibit a number of health benefits including, antibacterial, antiviral, anti-cancer, anti-inflammatory and anti-oxidant properties. In this review, the authors attempt to highlight the biological and pharmacological properties of CUR in addition to emphasizing aspects relating to the biosynthesis, encapsulation and therapeutic effects of the compound. The information contained in this review was generated by considering published information in which evidence of enhanced biological and pharmacological properties of nano-encapsulated CUR was reported. CUR has contributed to a significant improvement in melanoma, breast, lung, gastro-intestinal, and genito-urinary cancer therapy. We highlight the impact of nano-encapsulated CUR for efficient inhibition of cell proliferation, even at low concentrations compared to the free CUR when considering anti-proliferation. Furthermore nano-encapsulated CUR exhibited bioactive properties, exerted cytotoxic and anti-oxidant effects by acting on endogenous and cholinergic anti-oxidant systems. CUR was reported to block Hepatitis C virus (HCV) entry into hepatic cells, inhibit MRSA proliferation, enhance wound healing and reduce bacterial load. Nano-encapsulated CUR has also shown bioactive properties when acting on antioxidant systems (endogenous and cholinergic). Future research is necessary and must focus on investigation of encapsulated CUR nano-particles in different models of human pathology.
- Full Text:
- Date Issued: 2021
Evaluation of rate of swelling and erosion of verapamil (VRP) sustained-release matrix tablets
- Khamanga, Sandile M, Walker, Roderick B
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184232 , vital:44192 , xlink:href="https://doi.org/10.1080/03639040600599822"
- Description: Tablets manufactured in-house were compared to a marketed sustained-release product of verapamil to investigate the rate of hydration, erosion, and drug-release mechanism by measuring the wet and subsequent dry weights of the products. Swelling and erosion rates depended on the polymer and granulating fluid used, which ultimately pointed to their permeability characteristics. Erosion rate of the marketed product was highest, which suggests that the gel layer that formed around these tablets was weak as opposed to the robust and resistant layers of test products. Anomalous and near zero-order transport mechanisms were dominant in tests and commercial product, respectively.
- Full Text:
- Date Issued: 2006
- Authors: Khamanga, Sandile M , Walker, Roderick B
- Date: 2006
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184232 , vital:44192 , xlink:href="https://doi.org/10.1080/03639040600599822"
- Description: Tablets manufactured in-house were compared to a marketed sustained-release product of verapamil to investigate the rate of hydration, erosion, and drug-release mechanism by measuring the wet and subsequent dry weights of the products. Swelling and erosion rates depended on the polymer and granulating fluid used, which ultimately pointed to their permeability characteristics. Erosion rate of the marketed product was highest, which suggests that the gel layer that formed around these tablets was weak as opposed to the robust and resistant layers of test products. Anomalous and near zero-order transport mechanisms were dominant in tests and commercial product, respectively.
- Full Text:
- Date Issued: 2006
Evaluation of the in vitro differential protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (NLCs) for potential targeting to the brain
- Kasongo, Kasongo W, Jansch, Mirko, Müller, Rainer H, Walker, Roderick B
- Authors: Kasongo, Kasongo W , Jansch, Mirko , Müller, Rainer H , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184035 , vital:44160 , xlink:href="https://doi.org/10.3109/08982104.2010.539186"
- Description: The preferential in vitro adsorption of apolipoprotein E (Apo E) onto the surface of colloidal drug carriers may be used as a strategy to evaluate the in vivo potential for such systems to transport drugs to the brain. The aim of this research was to investigate the in vitro protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (DDI-NLCs), using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), in order to establish the potential for NLCs to deliver DDI to the brain. NLC formulations were manufactured using high-pressure homogenization using a lipid matrix consisting of a mixture of Precirol® ATO 5 and Transcutol® HP. The 2-D PAGE analysis revealed that NLCs in formulations stabilized using Solutol® HS 15 alone or with a ternary surfactant system consisting of Solutol® HS 15, Tween® 80, and Lutrol® F68, preferentially adsorbed proteins, such as Apo E. Particles stabilized with Tween® 80 and Lutrol® F68 did not adsorb Apo E in these studies, which could be related to the relatively large particle size and hence small surface area observed for these NLCs. These findings have revealed that DDI-loaded NLCs may have the potential to deliver DDI to the brain in vivo and, in addition, to Tween® 80, which has already been shown to have the ability to facilitate the targeting of colloidal drug delivery systems to the brain. Solutol® HS 15–stabilized nanoparticles may also achieve a similar purpose.
- Full Text:
- Date Issued: 2011
- Authors: Kasongo, Kasongo W , Jansch, Mirko , Müller, Rainer H , Walker, Roderick B
- Date: 2011
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/184035 , vital:44160 , xlink:href="https://doi.org/10.3109/08982104.2010.539186"
- Description: The preferential in vitro adsorption of apolipoprotein E (Apo E) onto the surface of colloidal drug carriers may be used as a strategy to evaluate the in vivo potential for such systems to transport drugs to the brain. The aim of this research was to investigate the in vitro protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (DDI-NLCs), using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), in order to establish the potential for NLCs to deliver DDI to the brain. NLC formulations were manufactured using high-pressure homogenization using a lipid matrix consisting of a mixture of Precirol® ATO 5 and Transcutol® HP. The 2-D PAGE analysis revealed that NLCs in formulations stabilized using Solutol® HS 15 alone or with a ternary surfactant system consisting of Solutol® HS 15, Tween® 80, and Lutrol® F68, preferentially adsorbed proteins, such as Apo E. Particles stabilized with Tween® 80 and Lutrol® F68 did not adsorb Apo E in these studies, which could be related to the relatively large particle size and hence small surface area observed for these NLCs. These findings have revealed that DDI-loaded NLCs may have the potential to deliver DDI to the brain in vivo and, in addition, to Tween® 80, which has already been shown to have the ability to facilitate the targeting of colloidal drug delivery systems to the brain. Solutol® HS 15–stabilized nanoparticles may also achieve a similar purpose.
- Full Text:
- Date Issued: 2011