An artificial neural network approach to predict the effects of formulation and process variables on prednisone release from a multipartite system
- Manda, Arthur, Walker, Roderick B, Khamanga, Sandile M
- Authors: Manda, Arthur , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183237 , vital:43933 , xlink:href="https://doi.org/10.3390/pharmaceutics11030109"
- Description: The impact of formulation and process variables on the in-vitro release of prednisone from a multiple-unit pellet system was investigated. Box-Behnken Response Surface Methodology (RSM) was used to generate multivariate experiments. The extrusion-spheronization method was used to produce pellets and dissolution studies were performed using United States Pharmacopoeia (USP) Apparatus 2 as described in USP XXIV. Analysis of dissolution test samples was performed using a reversed-phase high-performance liquid chromatography (RP-HPLC) method. Four formulation and process variables viz., microcrystalline cellulose concentration, sodium starch glycolate concentration, spheronization time and extrusion speed were investigated and drug release, aspect ratio and yield were monitored for the trained artificial neural networks (ANN). To achieve accurate prediction, data generated from experimentation were used to train a multi-layer perceptron (MLP) using back propagation (BP) and the Broyden-Fletcher-Goldfarb-Shanno (BFGS) 57 training algorithm until a satisfactory value of root mean square error (RMSE) was observed. The study revealed that the in-vitro release profile of prednisone was significantly impacted by microcrystalline cellulose concentration and sodium starch glycolate concentration. Increasing microcrystalline cellulose concentration retarded dissolution rate whereas increasing sodium starch glycolate concentration improved dissolution rate. Spheronization time and extrusion speed had minimal impact on prednisone release but had a significant impact on extrudate and pellet quality. This work demonstrated that RSM can be successfully used concurrently with ANN for dosage form manufacture to permit the exploration of experimental regions that are omitted when using RSM alone.
- Full Text:
- Date Issued: 2019
- Authors: Manda, Arthur , Walker, Roderick B , Khamanga, Sandile M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183237 , vital:43933 , xlink:href="https://doi.org/10.3390/pharmaceutics11030109"
- Description: The impact of formulation and process variables on the in-vitro release of prednisone from a multiple-unit pellet system was investigated. Box-Behnken Response Surface Methodology (RSM) was used to generate multivariate experiments. The extrusion-spheronization method was used to produce pellets and dissolution studies were performed using United States Pharmacopoeia (USP) Apparatus 2 as described in USP XXIV. Analysis of dissolution test samples was performed using a reversed-phase high-performance liquid chromatography (RP-HPLC) method. Four formulation and process variables viz., microcrystalline cellulose concentration, sodium starch glycolate concentration, spheronization time and extrusion speed were investigated and drug release, aspect ratio and yield were monitored for the trained artificial neural networks (ANN). To achieve accurate prediction, data generated from experimentation were used to train a multi-layer perceptron (MLP) using back propagation (BP) and the Broyden-Fletcher-Goldfarb-Shanno (BFGS) 57 training algorithm until a satisfactory value of root mean square error (RMSE) was observed. The study revealed that the in-vitro release profile of prednisone was significantly impacted by microcrystalline cellulose concentration and sodium starch glycolate concentration. Increasing microcrystalline cellulose concentration retarded dissolution rate whereas increasing sodium starch glycolate concentration improved dissolution rate. Spheronization time and extrusion speed had minimal impact on prednisone release but had a significant impact on extrudate and pellet quality. This work demonstrated that RSM can be successfully used concurrently with ANN for dosage form manufacture to permit the exploration of experimental regions that are omitted when using RSM alone.
- Full Text:
- Date Issued: 2019
Cordidepsine is A Potential New Anti-HIV Depsidone from Cordia millenii
- Zeukang, Rostanie D, Siwe-Noundou, Xavier, Fotsing, Maurice T, Mbafor, Joseph T, Krause, Rui W M, Choudhary, Muhammad I, Atchade, Alex de Theodore
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- Full Text:
- Date Issued: 2019
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- Full Text:
- Date Issued: 2019
Corrosion resistance of aluminum against acid activation: Impact of benzothiazole-substituted gallium phthalocyanine
- Nnaji, Nnaemeka, Nwaji, Njemuwa N, Mack, John, Nyokong, Tebello
- Authors: Nnaji, Nnaemeka , Nwaji, Njemuwa N , Mack, John , Nyokong, Tebello
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/187545 , vital:44670 , xlink:href="https://doi.org/10.3390/molecules24010207"
- Description: This study describes the adsorption behavior of organic inhibitors at the aluminum-HCl solution interface and their corrosion inhibition performance. The organic inhibitors employed are: 4-(benzo [d]thiazol-2ylthio)phthalonitrile (BTThio) and tetrakis[(benzo[d]thiazol-2-yl-thio)phthalocyaninato]gallium(III) chloride (ClGaBTThioPc). The corrosion behavior of these inhibitors is investigated using electrochemical and computational techniques. Open circuit potential results reveal predominant cathodic character for the mechanism of aluminum corrosion inhibition by the inhibitors. Inhibition efficiency values from potentiodynamic polarization measurements increase from 46.9 to 70.8% for BTThio and 59.7 to 81.0% for ClGaBTThioPc within the concentration range of 2 to 10 µM. Scanning electron microscopy (SEM) measurements reveal protection of the metal surface from acid attack, in the presence of the inhibitors and energy dispersive X-ray (EDX) measurements show that the most probable way by which the inhibitors protect the metal surface would be by shielding it from the corrosion attacks of Cl− from the acid. Quantum chemical parameters corroborate well with experimental findings.
- Full Text:
- Date Issued: 2019
- Authors: Nnaji, Nnaemeka , Nwaji, Njemuwa N , Mack, John , Nyokong, Tebello
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/187545 , vital:44670 , xlink:href="https://doi.org/10.3390/molecules24010207"
- Description: This study describes the adsorption behavior of organic inhibitors at the aluminum-HCl solution interface and their corrosion inhibition performance. The organic inhibitors employed are: 4-(benzo [d]thiazol-2ylthio)phthalonitrile (BTThio) and tetrakis[(benzo[d]thiazol-2-yl-thio)phthalocyaninato]gallium(III) chloride (ClGaBTThioPc). The corrosion behavior of these inhibitors is investigated using electrochemical and computational techniques. Open circuit potential results reveal predominant cathodic character for the mechanism of aluminum corrosion inhibition by the inhibitors. Inhibition efficiency values from potentiodynamic polarization measurements increase from 46.9 to 70.8% for BTThio and 59.7 to 81.0% for ClGaBTThioPc within the concentration range of 2 to 10 µM. Scanning electron microscopy (SEM) measurements reveal protection of the metal surface from acid attack, in the presence of the inhibitors and energy dispersive X-ray (EDX) measurements show that the most probable way by which the inhibitors protect the metal surface would be by shielding it from the corrosion attacks of Cl− from the acid. Quantum chemical parameters corroborate well with experimental findings.
- Full Text:
- Date Issued: 2019
Expansive Social Learning, Morphogenesis and Reflexive Action in an Organization Responding to Wetland Degradation
- Lindley, David S, Lotz-Sisitka, Heila
- Authors: Lindley, David S , Lotz-Sisitka, Heila
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/182450 , vital:43831 , xlink:href="https://doi.org/10.3390/su11154230"
- Description: This study (conducted as PhD research at Rhodes University, South Africa) describes a formative interventionist research project conducted to explore factors inhibiting improved wetland management within a corporate plantation forestry context and determine if, and how, expansive social learning processes could strengthen organizational learning and development to overcome these factors. A series of formative interventionist workshops and feedback meetings took place over three years; developing new knowledge amongst staff of Company X, and improved wetland management practices. Through the expansive learning process, the tensions and contradictions that emerged became generative, supporting expansive learning that was reflectively engaged with throughout the research period. The study was== supported by an epistemological framework of cultural historical activity theory and expansive learning. Realist social theory, emerging from critical realism, with its methodological compliment the morphogenetic framework gave the research the depth of detail required to explain how the expansive learning, organizational social change, and boundary crossings that are necessary for assembling the collective were taking place. This provided ontological depth to the research. The research found that expansive learning processes, which are also social learning processes (hence we use the term ‘expansive social learning’, supported organizational learning and development for improved wetland management. Five types of changes emerged from the research: (1) Changes in structure, (2) changes in practice, (3) changes in approach, (4) changes in discourse, and (5) changes in knowledge, values, and thinking. The study was able to explain how these changes occurred via the interaction of structural emergent properties and powers; cultural emergent properties and powers; and personal emergent properties and powers of agents. It was concluded that expansive learning could provide an environmental education platform to proactively work with the sociological potential of morphogenesis to bring about future change via an open-ended participatory and reflexive expansive learning process.
- Full Text:
- Date Issued: 2019
- Authors: Lindley, David S , Lotz-Sisitka, Heila
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/182450 , vital:43831 , xlink:href="https://doi.org/10.3390/su11154230"
- Description: This study (conducted as PhD research at Rhodes University, South Africa) describes a formative interventionist research project conducted to explore factors inhibiting improved wetland management within a corporate plantation forestry context and determine if, and how, expansive social learning processes could strengthen organizational learning and development to overcome these factors. A series of formative interventionist workshops and feedback meetings took place over three years; developing new knowledge amongst staff of Company X, and improved wetland management practices. Through the expansive learning process, the tensions and contradictions that emerged became generative, supporting expansive learning that was reflectively engaged with throughout the research period. The study was== supported by an epistemological framework of cultural historical activity theory and expansive learning. Realist social theory, emerging from critical realism, with its methodological compliment the morphogenetic framework gave the research the depth of detail required to explain how the expansive learning, organizational social change, and boundary crossings that are necessary for assembling the collective were taking place. This provided ontological depth to the research. The research found that expansive learning processes, which are also social learning processes (hence we use the term ‘expansive social learning’, supported organizational learning and development for improved wetland management. Five types of changes emerged from the research: (1) Changes in structure, (2) changes in practice, (3) changes in approach, (4) changes in discourse, and (5) changes in knowledge, values, and thinking. The study was able to explain how these changes occurred via the interaction of structural emergent properties and powers; cultural emergent properties and powers; and personal emergent properties and powers of agents. It was concluded that expansive learning could provide an environmental education platform to proactively work with the sociological potential of morphogenesis to bring about future change via an open-ended participatory and reflexive expansive learning process.
- Full Text:
- Date Issued: 2019
Exploring group solidarity for insights into qualities of T-learning
- Mudokwani, Kuda, Mukute, Mutizwa
- Authors: Mudokwani, Kuda , Mukute, Mutizwa
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/390612 , vital:68568 , xlink:href="https://doi.org/10.3390/su11236825"
- Description: Across the world, organised groups of farmers participating in just and sustainability transformations encounter multiple obstacles. Through solidarity manifested in iterative processes of questioning, co-learning, collective action and reflection, and value creation for themselves and for others, some succeed in overcoming them. This article investigates how a district organic farmer association in Zimbabwe is encountering and handling group solidarity challenges arising from shifting from local to district level coordinated organic production and marketing. Based on the use of change laboratory, this paper explores solidarity at the local niche and networked district level to seek insights into the qualities of T-learning.
- Full Text:
- Date Issued: 2019
- Authors: Mudokwani, Kuda , Mukute, Mutizwa
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/390612 , vital:68568 , xlink:href="https://doi.org/10.3390/su11236825"
- Description: Across the world, organised groups of farmers participating in just and sustainability transformations encounter multiple obstacles. Through solidarity manifested in iterative processes of questioning, co-learning, collective action and reflection, and value creation for themselves and for others, some succeed in overcoming them. This article investigates how a district organic farmer association in Zimbabwe is encountering and handling group solidarity challenges arising from shifting from local to district level coordinated organic production and marketing. Based on the use of change laboratory, this paper explores solidarity at the local niche and networked district level to seek insights into the qualities of T-learning.
- Full Text:
- Date Issued: 2019
Making (non) sense of urban water flows: Qualities and processes for transformative and transgressive learning moments
- Authors: James, Anna
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/390665 , vital:68572 , xlink:href="https://doi.org/10.3390/su11236817"
- Description: Urban sustainability and justice depend upon the flow of water across complex urban space. Yet, the characteristics of urban space produce a fragmented sense of our water resources. Cape Town, South Africa, the context of this research, is one such city whose water challenges have been exacerbated by climate change-induced drought, to the extent that the city nearly shut off the water running to residents’ taps. This context presents a particular challenge for the focus of this special issue, transformative and transgressive learning, an emerging arena of thought and practice concerned with learning processes that might foster more sustainable socio-ecological relations. The empirical material for this research draws from 12 arts-based inquiry workshops run with youth in an environmental organisation over four months, exploring a local water crisis. The data were generated through an engaged arts-based research process. The paper traces how transformative and transgressive learning in the context of urban water crisis might be characterised as making (non)sense by bringing the empirical material into dialogue with five entry points of transformative and transgressive learning literature rooted in Freirean educational praxis. This paper crafts and engages the concept of making (non)sense, a way of thinking about qualities and processes of learning praxis that responds to the wicked sustainability challenges we face today, particularly in terms of a Global South perspective. I argue such a praxis needs qualities and processes that disrupt and trouble the norm in the context of the socio-ecological challenge of urban water.
- Full Text:
- Date Issued: 2019
- Authors: James, Anna
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/390665 , vital:68572 , xlink:href="https://doi.org/10.3390/su11236817"
- Description: Urban sustainability and justice depend upon the flow of water across complex urban space. Yet, the characteristics of urban space produce a fragmented sense of our water resources. Cape Town, South Africa, the context of this research, is one such city whose water challenges have been exacerbated by climate change-induced drought, to the extent that the city nearly shut off the water running to residents’ taps. This context presents a particular challenge for the focus of this special issue, transformative and transgressive learning, an emerging arena of thought and practice concerned with learning processes that might foster more sustainable socio-ecological relations. The empirical material for this research draws from 12 arts-based inquiry workshops run with youth in an environmental organisation over four months, exploring a local water crisis. The data were generated through an engaged arts-based research process. The paper traces how transformative and transgressive learning in the context of urban water crisis might be characterised as making (non)sense by bringing the empirical material into dialogue with five entry points of transformative and transgressive learning literature rooted in Freirean educational praxis. This paper crafts and engages the concept of making (non)sense, a way of thinking about qualities and processes of learning praxis that responds to the wicked sustainability challenges we face today, particularly in terms of a Global South perspective. I argue such a praxis needs qualities and processes that disrupt and trouble the norm in the context of the socio-ecological challenge of urban water.
- Full Text:
- Date Issued: 2019
Participatory mapping in a developing country context: Lessons from South Africa
- Weyer, Dylan J, Bezerra, Joana C, de Vos, Alta
- Authors: Weyer, Dylan J , Bezerra, Joana C , de Vos, Alta
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/416333 , vital:71340 , xlink:href="https://doi.org/10.3390/land8090134"
- Description: Digital participatory mapping improves accessibility to spatial information and the way in which knowledge is co-constructed and landscapes co-managed with impoverished communities. However, many unintended consequences for social and epistemic justice may be exacerbated in developing country contexts. Two South African case studies incorporating Direct-to-Digital participatory mapping in marginalized communities to inform land-use decision-making, and the ethical challenges of adopting this method are discussed. Understanding the past and present context of the site and the power dynamics at play is critical to develop trust and manage expectations among research participants. When employing unfamiliar technology, disparate literacy levels and language barriers create challenges for ensuring participants understand the risks of their involvement and recognize their rights. The logistics of using this approach in remote areas with poor infrastructure and deciding how best to leave the participants with the maps they have co-produced in an accessible format present further challenges. Overcoming these can however offer opportunity for redressing past injustices and empowering marginalized communities with a voice in decisions that affect their livelihoods.
- Full Text:
- Date Issued: 2019
- Authors: Weyer, Dylan J , Bezerra, Joana C , de Vos, Alta
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/416333 , vital:71340 , xlink:href="https://doi.org/10.3390/land8090134"
- Description: Digital participatory mapping improves accessibility to spatial information and the way in which knowledge is co-constructed and landscapes co-managed with impoverished communities. However, many unintended consequences for social and epistemic justice may be exacerbated in developing country contexts. Two South African case studies incorporating Direct-to-Digital participatory mapping in marginalized communities to inform land-use decision-making, and the ethical challenges of adopting this method are discussed. Understanding the past and present context of the site and the power dynamics at play is critical to develop trust and manage expectations among research participants. When employing unfamiliar technology, disparate literacy levels and language barriers create challenges for ensuring participants understand the risks of their involvement and recognize their rights. The logistics of using this approach in remote areas with poor infrastructure and deciding how best to leave the participants with the maps they have co-produced in an accessible format present further challenges. Overcoming these can however offer opportunity for redressing past injustices and empowering marginalized communities with a voice in decisions that affect their livelihoods.
- Full Text:
- Date Issued: 2019
Research for the people, by the people: The political practice of cognitive justice and transformative learning in environmental social movements
- Authors: Burt, Jane C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/392177 , vital:68728 , xlink:href="https://doi.org/10.3390/su11205611"
- Description: This paper describes how Changing Practice courses, developed by environmental activists in South Africa and based on social learning practice, have seeded cognitive justice action. For the educator-activists who facilitated these courses, it became apparent that we needed a bold emancipatory pedagogy which included cognitive justice issues. This enabled us and the activist-researcher participants to understand the extent to which local, indigenous, and spiritual knowledge had been excluded from water governance. The paper investigates how participants in the ‘Water and Tradition’ change project, established by the Vaal Environmental Justice Alliance (VEJA, engaged with cognitive justice, to demonstrate how African spiritual practice offers a re-visioning of the natural world. Finally, using the tools of critical realist theory, the paper reviews how VEJA bring about transformative social action through their participation in the Changing Practice course.
- Full Text:
- Date Issued: 2019
- Authors: Burt, Jane C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/392177 , vital:68728 , xlink:href="https://doi.org/10.3390/su11205611"
- Description: This paper describes how Changing Practice courses, developed by environmental activists in South Africa and based on social learning practice, have seeded cognitive justice action. For the educator-activists who facilitated these courses, it became apparent that we needed a bold emancipatory pedagogy which included cognitive justice issues. This enabled us and the activist-researcher participants to understand the extent to which local, indigenous, and spiritual knowledge had been excluded from water governance. The paper investigates how participants in the ‘Water and Tradition’ change project, established by the Vaal Environmental Justice Alliance (VEJA, engaged with cognitive justice, to demonstrate how African spiritual practice offers a re-visioning of the natural world. Finally, using the tools of critical realist theory, the paper reviews how VEJA bring about transformative social action through their participation in the Changing Practice course.
- Full Text:
- Date Issued: 2019
Short term stability testing of efavirenz-loaded solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) dispersions
- Makoni, Pedzisai A, Kasongo, Kasongo W, Walker, Roderick B
- Authors: Makoni, Pedzisai A , Kasongo, Kasongo W , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183492 , vital:44000 , xlink:href="https://doi.org/10.3390/pharmaceutics11080397"
- Description: The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.
- Full Text:
- Date Issued: 2019
- Authors: Makoni, Pedzisai A , Kasongo, Kasongo W , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183492 , vital:44000 , xlink:href="https://doi.org/10.3390/pharmaceutics11080397"
- Description: The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.
- Full Text:
- Date Issued: 2019
Stability indicating HPLC-ECD method for the analysis of clarithromycin in pharmaceutical dosage forms: Method scaling versus re-validation.
- Makoni, Pedzisai A, Chikukwa, Mellisa, Khamanga, Sandile M, Walker, Roderick B
- Authors: Makoni, Pedzisai A , Chikukwa, Mellisa , Khamanga, Sandile M , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183387 , vital:43984 , xlink:href="https://doi.org/10.3390/scipharm87040031"
- Description: An isocratic high-performance liquid chromatographic method using electrochemical detection (HPLC-ECD) for the quantitation of clarithromycin (CLA) was developed using Response Surface Methodology (RSM) based on a Central Composite Design (CCD). The method was validated using International Conference on Harmonization (ICH) guidelines with an analytical run time of 20 min. Method re-validation following a change in analytical column was successful in reducing the analytical run time to 13 min, decreasing solvent consumption thus facilitating environmental and financial sustainability. The applicability of using the United States Pharmacopeia (USP) method scaling approach in place of method re-validation using a column with a different L–designation to the original analytical column, was investigated. The scaled method met all USP system suitability requirements for resolution, tailing factor and % relative standard deviation (RSD). The re-validated and scaled method was successfully used to resolve CLA from manufacturing excipients in commercially available dosage forms. Although USP method scaling is only permitted for columns within the same L-designation, these data suggest that it may also be applicable to columns of different designation.
- Full Text:
- Date Issued: 2019
- Authors: Makoni, Pedzisai A , Chikukwa, Mellisa , Khamanga, Sandile M , Walker, Roderick B
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183387 , vital:43984 , xlink:href="https://doi.org/10.3390/scipharm87040031"
- Description: An isocratic high-performance liquid chromatographic method using electrochemical detection (HPLC-ECD) for the quantitation of clarithromycin (CLA) was developed using Response Surface Methodology (RSM) based on a Central Composite Design (CCD). The method was validated using International Conference on Harmonization (ICH) guidelines with an analytical run time of 20 min. Method re-validation following a change in analytical column was successful in reducing the analytical run time to 13 min, decreasing solvent consumption thus facilitating environmental and financial sustainability. The applicability of using the United States Pharmacopeia (USP) method scaling approach in place of method re-validation using a column with a different L–designation to the original analytical column, was investigated. The scaled method met all USP system suitability requirements for resolution, tailing factor and % relative standard deviation (RSD). The re-validated and scaled method was successfully used to resolve CLA from manufacturing excipients in commercially available dosage forms. Although USP method scaling is only permitted for columns within the same L-designation, these data suggest that it may also be applicable to columns of different designation.
- Full Text:
- Date Issued: 2019
Ursolic Acid and its derivatives as bioactive agents
- Mlala, Sithenkosi, Oyedeji, Adebola Omowunmi, Gondwe, Mavuto, Oyedeji, Opeoluwa Oyehan
- Authors: Mlala, Sithenkosi , Oyedeji, Adebola Omowunmi , Gondwe, Mavuto , Oyedeji, Opeoluwa Oyehan
- Date: 2019
- Subjects: Noncommunicable diseases , Pentacyclic triterpenoids , Ursolic acid , Clinical trials
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1576 , vital:37793 , https://doi.org/10.3390/molecules24152751
- Description: Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCD.
- Full Text:
- Date Issued: 2019
- Authors: Mlala, Sithenkosi , Oyedeji, Adebola Omowunmi , Gondwe, Mavuto , Oyedeji, Opeoluwa Oyehan
- Date: 2019
- Subjects: Noncommunicable diseases , Pentacyclic triterpenoids , Ursolic acid , Clinical trials
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1576 , vital:37793 , https://doi.org/10.3390/molecules24152751
- Description: Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCD.
- Full Text:
- Date Issued: 2019
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