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Nationwide Assessment of Population Structure, Stability and Plant Morphology of Two Mimusops Species along a Social-Ecological Gradient in Benin, West Africa

  • Authors: Sinasson, Gisèle K , Shackleton, Charlie M , Sinsin, Brice
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/399805 , vital:69560 , xlink:href="https://doi.org/10.3390/f12111575"
  • Description: Understanding tree species autecology and population structure supports effective conservation actions. Of particular importance are multipurpose trees that provide non-timber forest products (NTFPs). We assessed the population structures and morphologies of two species of NTFP trees in the genus Mimusops across bioclimatic zones in Benin by sampling 288 plots within 11 forests. Structural characteristics were compared between species, forests and zones. Correlations were also observed between Mimusops tree regeneration density, tree features and ecological characteristics. The density of trees ≥5 cm and of regeneration and mean tree height were higher for M. andongensis (within more protected forest) than M. kummel (in forests with access to people), while the highest mean diameter was observed for M. kummel. Tree and regeneration densities and mean height were greatest in the humid zone of Benin, whilst the largest mean diameter was obtained in the sub-humid zone. The results showed significant correlations between regeneration density and soil properties for M. andongensis but not for M. kummel. The correlations between tree morphology and soil characteristics were weak for both species. Ecological characteristics, along with the species’ functional traits and pressures, are important factors related to the observed differences between the species. All diameter classes were represented, and the population seemed more stable in the more protected forest relative to other forests. Mimusops trees with a diameter of 5–15 cm represented more than 30% of this species in most forests; this suggests, for M. kummel, whose trees flower when quite small (≥6 cm dbh), that there are sufficient reproductive trees. Thus, as a long-lived species, its populations could be maintained even with low/episodic recruitment. However, we found no regeneration in many forests and climate change could threaten populations. Therefore, it is important to investigate regeneration growth and dynamics, seed production and germination of the species in relation to the biophysical conditions and disturbances experienced by Mimusops stands.
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  • Date Issued: 2021

Prevalence of Hypertension and Its Associated Risk Factors in a Rural Black Population of Mthatha Town, South Africa

Rapid Synthesis of Thiol-Co-Capped-CdTe/CdSe/ZnSe Core Shell-Shell Nanoparticles

  • Authors: Daramola, Olamide , Siwe-Noundou, Xavier , Tseki, Potlaki , Krause, Rui W M
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/191758 , vital:45161 , xlink:href="https://doi.org/10.3390/nano11051193"
  • Description: CdTe QDs has been demonstrated in many studies to possess good outstanding optical and photo-physical properties. However, it has been established from literature that the toxic Cd2+ that tends to leak out into nearby solutions can be protected by less toxic ZnS or ZnSe shells leading to the synthesis of core-shells and multi-core-shells. Hence, this has allowed the synthesis of CdTe multi-core-shells to have gained much interest. The preparation of most CdTe multi-core-shells reported from various studies usually has a longer reaction time (6–24 h) in reaching their highest emission maxima. The synthesis of CdTe multi-core-shells in this study only took 35 min to obtain a highest emission maximum compared to what has been reported from the literature. CdTe multi-core-shells were synthesized by injecting 7, 14, and 21 mL each of Zn complex solution and Se ions into the reacting mixture containing CdTe core-shells (3 h) at 5 min intervals over a 35 min reaction time. The emission maxima of the MPA-TGA-CdTe multi-core-shells at 21 mL injection was recorded around 625 nm. Therefore, we are reporting the rapid synthesis of five different thiol co-capped CdTe/CdSe/ZnSe multi-core-shell QDs with the highest emission maxima obtained at 35 min reaction time.
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  • Date Issued: 2021

Relationship between Endothelial Function, Antiretroviral Treatment and Cardiovascular Risk Factors in HIV Patients of African Descent in South Africa: A Cross-Sectional Study

Review of the Traditional Uses, Phytochemistry, and Pharmacological Activities of Rhoicissus Species (Vitaceae)

  • Authors: Dube, Nondumiso , Siwe-Noundou, Xavier , Krause, Rui W M , Kemboi, Douglas , Tembu, Vuyelwa J , Manicum, Amanda-Lee
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/191769 , vital:45162 , xlink:href="https://doi.org/10.3390/molecules26082306"
  • Description: Species within the genus Rhoicissus (Vitaceae) are commonly used in South African traditional medicine. The current review discusses the occurrence, distribution, traditional uses, phytochemistry, and pharmacological properties of Rhoicissus species covering the period 1981–2020. The data reported were systematically collected, read, and analysed from scientific electronic databases including Scopus, Scifinder, Pubmed, and Google Scholar. Reported evidence indicates that species in this genus are used for the treatment of gastrointestinal complaints, sexually transmitted infections (STIs), and infertility, as well as to tone the uterus during pregnancy and to facilitate delivery. Pharmacological studies have further shown that members of the Rhoicissus genus display antidiabetic, uterotonic, ascaricidal, hepatoprotective, antioxidant, antimicrobial, anticancer, and anti-inflammatory properties. They are linked to the presence of bioactive compounds isolated from the genus. Hence, Rhoicissus species can potentially be an alternative therapeutic strategy to treat diseases and develop safer and more potent drugs to combat diseases. Plant species of this genus have valuable medicinal benefits due to their significant pharmacological potential. However, scientific investigation and information of the therapeutic potential of Rhoicissus remain limited as most of the species in the genus have not been fully exploited. Therefore, there is a need for further investigations to exploit the therapeutic potential of the genus Rhoicissus. Future studies should evaluate the phytochemical, pharmacological, and toxicological activities, as well as the mode of action, of Rhoicissus crude extracts and secondary compounds isolated from the species.
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  • Date Issued: 2021

Single Nucleotide Polymorphisms Associated with Metformin and Sulphonylureas’ Glycaemic Response among South African Adults with Type 2 Diabetes Mellitus

Solar Driven Photocatalytic Activity of Porphyrin Sensitized TiO2

  • Authors: Otieno, Sebastien , Lanterna, Anabel E , Mack, John , Derese, Solomon , Amuhaya, Edith K , Nyokong, Tebello , Scaiano, Juan C
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/190612 , vital:45010 , xlink:href="https://doi.org/10.3390/molecules26113131"
  • Description: The absence of a secure long-term sustainable energy supply is recognized as a major worldwide technological challenge. The generation of H2 through photocatalysis is an environmentally friendly alternative that can help solve the energy problem. Thus, the development of semiconductor materials that can absorb solar light is an attractive approach. TiO2 has a wide bandgap that suffers from no activity in the visible spectrum, limiting its use of solar radiation. In this research, the semiconductor absorption profile was extended into the visible region of the solar spectrum by preparing porphyrin-TiO2 (P-TiO2 ) composites of meso-tetra(4-bromophenyl)porphyrin (PP1) and meso-tetra(5-bromo-2-thienyl)porphyrin (PP2) and their In(III), Zn(II) and Ga(III) metal complexes. Density functional theory (DFT) and time-dependent density functional theory (TD-DFT) calculations were performed on the porphyrins to gain insight into their electron injection capability. The results demonstrate that P-TiO2 systems merit further in-depth study for applications that require efficient photocatalytic H2 generation.
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  • Date Issued: 2021

Top-Down Synthesis of a Lamivudine-Zidovudine Nano Co-Crystal

  • Authors: Witika, Bwalya A , Smith, Vincent J , Walker, Roderick B
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183172 , vital:43918 , xlink:href="https://doi.org/10.3390/cryst11010033"
  • Description: Lamivudine (3TC) and zidovudine (AZT) are antiretroviral agents used to manage HIV/AIDS infection. A wet media milling top-down approach was used to develop and produce nano co-crystals of 3TC and AZT. Micro co-crystals were prepared by solvent evaporation and subsequently milled in the presence of two surfactants, viz., sodium lauryl sulfate (SLS) and α-tocopheryl polyethylene glycol succinate 1000 (TPGS 1000). Optimisation was undertaken using design of experiments (DoE) and response surface methodology (RSM) to establish and identify parameters that may affect the manufacturing of nano co-crystals. The impact of SLS and TPGS 1000 concentration, milling time, and number of units of milling medium on the manufacturing of nano co-crystals, was investigated. The critical quality attributes (CQA) monitored were particle size (PS), Zeta potential (ZP), and polydispersity index (PDI). Powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry, transmission electron microscopy, energy dispersive X-ray spectroscopy scanning electron microscopy, and cytotoxicity assays were used for additional characterization of the optimised nano co-crystal. The mean PS, PDI, and ZP of the optimised top-down nanocrystal were 271.0 ± 92.0 nm, 0.467 ± 0.073, and −41.9 ± 3.94 mV, respectively. In conclusion, a simple, inexpensive, rapid, and precise method of nano co-crystal manufacturing was developed, validated, and optimised using DoE and RSM, and the final product exhibited the target CQA.
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  • Date Issued: 2021

Ultrasound-Triggered Release of 5-Fluorouracil from Soy Lecithin Echogenic Liposomes

  • Authors: Ezekiel, Charles I , Bapolisi, Alain M , Walker, Roderick B , Krause, Rui W M
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183115 , vital:43913 , xlink:href="https://doi.org/10.3390/pharmaceutics13060821"
  • Description: Colorectal cancer is the third most diagnosed cancer and the second leading cause of death. The use of 5-fluorouracil (5-FU) has been the major chemotherapeutic treatment for colorectal cancer patients. However, the efficacy of 5-FU is limited by drug resistance, and bone marrow toxicity through high-level expression of thymidylate synthase, justifying the need for improvement of the therapeutic index. In this study, the effects of ultrasound on echogenic 5-FU encapsulated crude soy liposomes were investigated for their potential to address these challenges. Liposomes were prepared by thin-film hydration using crude soy lecithin and cholesterol. Argon gas was entrapped in the liposomes for sonosensitivity (that is, responsiveness to ultrasound). The nanoparticles were characterized for particle size and morphology. The physicochemical properties were also evaluated using differential scanning calorimetry, Fourier transform infrared and X-ray diffraction. The release profile of 5-FU was assessed with and without 20 kHz low-frequency ultrasound waves at various amplitudes and exposure times. The result reveal that 5-FU-loaded liposomes were spherical with an encapsulation efficiency of approximately 60%. Approximately 65% of 5-FU was released at the highest amplitude and exposure time was investigated. The results are encouraging for the stimulated and controlled release of 5-FU for the management of colorectal cancer.
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  • Date Issued: 2021

Unlocking the Diversity of Pyrroloiminoquinones Produced by Latrunculid Sponge Species

  • Authors: Kalinski, Jarmo-Charles J , Krause, Rui W M , Parker-Nance, Shirley , Waterworth, Samantha C , Dorrington, Rosemary A
  • Date: 2021
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/191802 , vital:45165 , xlink:href="https://doi.org/10.3390/md19020068"
  • Description: Sponges of the Latrunculiidae family produce bioactive pyrroloiminoquinone alkaloids including makaluvamines, discorhabdins, and tsitsikammamines. The aim of this study was to use LC-ESI-MS/MS-driven molecular networking to characterize the pyrroloiminoquinone secondary metabolites produced by six latrunculid species. These are Tsitsikamma favus, Tsitsikamma pedunculata, Cyclacanthia bellae, and Latrunculia apicalis as well as the recently discovered species, Tsitsikamma nguni and Tsitsikamma michaeli. Organic extracts of 43 sponges were analyzed, revealing distinct species-specific chemical profiles. More than 200 known and unknown putative pyrroloiminoquinones and related compounds were detected, including unprecedented makaluvamine-discorhabdin adducts and hydroxylated discorhabdin I derivatives. The chemical profiles of the new species T. nguni closely resembled those of the known T. favus (chemotype I), but with a higher abundance of tsitsikammamines vs. discorhabdins. T. michaeli sponges displayed two distinct chemical profiles, either producing mostly the same discorhabdins as T. favus (chemotype I) or non- or monobrominated, hydroxylated discorhabdins. C. bellae and L. apicalis produced similar pyrroloiminoquinone chemistry to one another, characterized by sulfur-containing discorhabdins and related adducts and oligomers. This study highlights the variability of pyrroloiminoquinone production by latrunculid species, identifies novel isolation targets, and offers fundamental insights into the collision-induced dissociation of pyrroloiminoquinones.
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  • Date Issued: 2021

A comparative study of the effect of different stabilizers on the critical quality attributes of self-assembling nano co-crystals

  • Authors: Witika, Bwalya A , Smith, Vincent J , Walker, Roderick B
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183224 , vital:43931 , xlink:href=" https://doi.org/10.3390/pharmaceutics12020182"
  • Description: Lamivudine (3TC) and zidovudine (AZT) are antiviral agents used orally to manage HIV/AIDS infection. A pseudo one-solvent bottom-up approach was used to develop and produce nano co-crystals of 3TC and AZT. Equimolar amounts of 3TC dissolved in de-ionized water and AZT in methanol were rapidly injected into a pre-cooled vessel and sonicated at 4 °C. The resultant suspensions were characterized using a Zetasizer. The particle size, polydispersity index and Zeta potential were elucidated. Further characterization was undertaken using powder X-ray diffraction, Raman spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and energy dispersive X-ray spectroscopy scanning electron microscopy. Different surfactants were assessed for their ability to stabilize the nano co-crystals and for their ability to produce nano co-crystals with specific and desirable critical quality attributes (CQA) including particle size (PS) less than 1000 nm, polydispersity index (PDI) less than 0.500 and Zeta potential (ZP) less than −30 mV. All surfactants produced co-crystals in the nanometer range. The PDI and PS are concentration-dependent for all nano co-crystals manufactured while only ZP was within specification when sodium dodecyl sulfate was used in the process.
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  • Date Issued: 2020

A novel dimeric exoglucanase (GH5_38)

  • Authors: Mafa, Mpho S , Dirr, Heinrich W , Malgas, Samkelo , Krause, Rui W M , Pletschke, Brett I
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/193976 , vital:45412 , xlink:href="https://doi.org/10.3390/molecules25030746"
  • Description: An exoglucanase (Exg-D) from the glycoside hydrolase family 5 subfamily 38 (GH5_38) was heterologously expressed and structurally and biochemically characterised at a molecular level for its application in alkyl glycoside synthesis. The purified Exg-D existed in both dimeric and monomeric forms in solution, which showed highest activity on mixed-linked β-glucan (88.0 and 86.7 U/mg protein, respectively) and lichenin (24.5 and 23.7 U/mg protein, respectively). They displayed a broad optimum pH range from 5.5 to 7 and a temperature optimum from 40 to 60 °C. Kinetic studies demonstrated that Exg-D had a higher affinity towards β-glucan, with a Km of 7.9 mg/mL and a kcat of 117.2 s−1, compared to lichenin which had a Km of 21.5 mg/mL and a kcat of 70.0 s−1. The circular dichroism profile of Exg-D showed that its secondary structure consisted of 11% α-helices, 36% β-strands and 53% coils. Exg-D performed transglycosylation using p-nitrophenyl cellobioside as a glycosyl donor and several primary alcohols as acceptors to produce methyl-, ethyl- and propyl-cellobiosides. These products were identified and quantified via thin-layer chromatography (TLC) and liquid chromatography–mass spectrometry (LC-MS). We concluded that Exg-D is a novel and promising oligomeric glycoside hydrolase for the one-step synthesis of alkyl glycosides with more than one monosaccharide unit.
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  • Date Issued: 2020

A relational approach to landscape stewardship: Towards a new perspective for multi-actor collaboration

  • Authors: Cockburn, Jessica J , Rosenberg, Eureta , Copteros, Athina , Cornelius, Susanna F , Libala, Notiswa , Metcalfe, Liz , Van der Waal, Benjamin C W
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/370098 , vital:66297 , xlink:href="https://doi.org/10.3390/land9070224"
  • Description: Landscape stewardship is increasingly understood within the framing of complex social-ecological systems. To consider the implications of this, we focus on one of the key characteristics of complex social-ecological systems: they are relationally constituted, meaning that system characteristics emerge out of dynamic relations between system components. We focus on multi-actor collaboration as a key form of relationality in landscapes, seeking a more textured understanding of the social relations between landscape actors. We draw on a set of ‘gardening tools’ to analyse the boundary-crossing work of multi-actor collaboration. These tools comprise three key concepts: relational expertise, common knowledge, and relational agency. We apply the tools to two cases of landscape stewardship in South Africa: the Langkloof Region and the Tsitsa River catchment. These landscapes are characterised by economically, socio-culturally, and politically diverse groups of actors. Our analysis reveals that history and context strongly influence relational processes, that boundary-crossing work is indeed difficult, and that doing boundary-crossing work in smaller pockets within a landscape is helpful. The tools also helped to identify three key social-relational practices which lend a new perspective on boundary-crossing work: 1. belonging while differing, 2. growing together by interacting regularly and building common knowledge, and 3. learning and adapting together with humility and empathy.
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  • Date Issued: 2020

Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives

  • Authors: Waleguele, Christine C , Mba'ning, Brice M , Awantu, Angelbert F , Bankeu, Jean J , Fongang, Yannick S F , Ngouela, Augustin S , Tsamo, Etienne , Sewald, Norbert , Lenta, Bruno N , Krause, Rui W M
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/193364 , vital:45325 , xlink:href="https://doi.org/10.3390/molecules25122862"
  • Description: The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.
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  • Date Issued: 2020

Biocompatibility of biomaterials for nanoencapsulation: Current approaches

  • Authors: Witika, Bwalya A , Makoni, Pedzisai A , Matafwali, Scott K , Chabalenge, Billy , Mwila, Chiluba , Kalungia, Aubrey C , Nkanga, Christian I , Bapolisi, Alain M , Walker, Roderick B
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183289 , vital:43939 , xlink:href="https://doi.org/10.3390/nano10091649"
  • Description: Nanoencapsulation is an approach to circumvent shortcomings such as reduced bioavailability, undesirable side effects, frequent dosing and unpleasant organoleptic properties of conventional drug delivery systems. The process of nanoencapsulation involves the use of biomaterials such as surfactants and/or polymers, often in combination with charge inducers and/or ligands for targeting. The biomaterials selected for nanoencapsulation processes must be as biocompatible as possible. The type(s) of biomaterials used for different nanoencapsulation approaches are highlighted and their use and applicability with regard to haemo- and, histocompatibility, cytotoxicity, genotoxicity and carcinogenesis are discussed.
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  • Date Issued: 2020

Combination of CTec2 and GH5 or GH26 Endo-Mannanases for Effective Lignocellulosic Biomass Degradation

  • Authors: Malgas, Samkelo , Pletschke, Brett I
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/429397 , vital:72607 , xlink:href="https://doi.org/10.3390/catal10101193"
  • Description: Among endo-mannanases, glycoside hydrolase (GH) family 26 enzymes have been shown to be more catalytically active than GH5 enzymes on mannans. However, only GH5 endo-mannanases have been used for the formulation of enzyme cocktails. In this study, Bacillus sp.-derived GH5 and GH26 endo-mannanases were comparatively analysed biochemically for their synergistic action with a commercial cellulase blend, CTec2, during pre-treated lignocellulose degradation. Substrate specificity and thermo-stability studies on mannan substrates showed that GH26 endo-mannanase was more catalytically active and stable than GH5. GH26 also exhibited higher binding affinity for mannan than GH5, while GH5 showed more affinity for lignocellulosic substrates than GH26. Applying the endo-mannanases in combination with CTec2 for lignocellulose degradation led to synergism with a 1.3-fold increase in reducing sugar release compared to when CTec2 was used alone. This study showed that using the activity of endo-mannanases displayed with model substrates is a poor predictor of their activity and synergism on complex lignocelluloses.
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  • Date Issued: 2020

Design, Optimization, Manufacture and Characterization of Efavirenz-Loaded Flaxseed Oil Nanoemulsions

  • 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.
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  • Date Issued: 2020

Drought Influences on Food Insecurity in Africa: A Systematic Literature Review

Formulation and Characterisation of a Combination Captopril and Hydrochlorothiazide Microparticulate Dosage Form

  • Authors: Chikukwa, Mellisa T R , Walker, Roderick B , Khamanga, Sandile M
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183200 , vital:43926 , xlink:href="https://doi.org/10.3390/pharmaceutics12080712"
  • Description: Cardiovascular diseases such as hypertension and cardiac failure in South African children and adolescents are effectively managed long term, using a combination treatment of captopril and hydrochlorothiazide. The majority of commercially available pharmaceutical products are designed for adult patients and require extemporaneous manipulation, prior to administration to paediatric patients. There is a need to develop an age appropriate microparticulate dosing technology that is easy to swallow, dose and alter doses whilst overcoming the pharmacokinetic challenges of short half-life and biphasic pharmacokinetic disposition exhibited by hydrochlorothiazide and captopril. An emulsion solvent evaporation approach using different combinations of polymers was used to manufacture captopril and hydrochlorothiazide microparticles. Design of experiments was used to develop and analyse experimental data, and identifyoptimum formulation and process conditions for the preparation of the microparticles. Characterisation studies to establish encapsulation efficiency, in vitro release, shape, size and morphology of the microparticles were undertaken. The microparticles produced were in the micrometre size range, with an encapsulation efficiency >75% for both hydrochlorothiazide and captopril. The microparticulate technology is able to offer potential resolution to the half-life mediated dosing frequency of captopril as sustained release of the molecule was observed over a 12-h period. The release of hydrochlorothiazide of >80% suggests an improvement in solubility limited dissolution.
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  • Date Issued: 2020

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

  • Authors: Mwila, Chiluba , Walker, Roderick B
  • Date: 2020
  • Subjects: To be catalogued
  • Language: English
  • Type: text , article
  • Identifier: http://hdl.handle.net/10962/183210 , vital:43929 , xlink:href="https://doi.org/10.3390/pharmaceutics12030234"
  • Description: The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin.
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  • Date Issued: 2020
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