Tafenoquine (TQ), a new synthetic analog of primaquine, has relatively poor bioavailability and associated toxicity in glucose-6-phosphate dehydrogenase (G6PD)-deficient individuals. A microemulsion formulation of TQ (MTQ) with sizes <20 nm improved the solubility of TQ and enhanced the oral bioavailability from 55% to 99% in healthy mice (area under the curve 0 to infinity: 11,368±1,232 and 23,842±872 min·μmol/L) for reference TQ and MTQ, respectively. Average parasitemia in Plasmodium berghei -infected mice was four- to tenfold lower in the MTQ-treated group. In vitro antiplasmodial activities against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum indicated no change in half maximal inhibitory concentration, suggesting that the microemulsion did not affect the inherent activity of TQ. In a humanized mouse model of G6PD deficiency, we observed reduction in toxicity of TQ as delivered by MTQ at low but efficacious concentrations of TQ. We hereby report an enhancement in the solubility, bioavailibility, and efficacy of TQ against blood stages of Plasmodium parasites without a corresponding increase in toxicity.
Primaquine (PQ) is one of the most widely used antimalarial drugs and is the only available drug that combats the relapsing form of malaria. PQ use in higher doses is limited by severe tissue toxicity including hematological- and gastrointestinal-related side effects. Nanoformulation of drugs in an appropriate drug carrier system has been extensively studied and shown to have the potential to improve bioavailability, thereby enhancing activity, reducing dose frequency, and subsequently reducing toxicity. The aim of this work was to design, synthesize, and characterize PQ-loaded solid lipid nanoparticles (SLNs) (PQ-SLNs) as a potential drug-delivery system. SLNs were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNs were 236 nm, +23 mV, 14%, and 75%, respectively. The zeta potential of the SLNs changed dramatically, from −6.54 mV to +23.0 mV, by binding positively charged chitosan as surface modifier. A spherical morphology of PQ-SLNs was seen by scanning electron microscope. In vitro, release profile depicted a steady drug release over 72 hours. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. Negligible changes in characteristic peaks of drug in Fourier transform infrared spectra indicated absence of any interaction among the various components entrapped in the nanoparticle formulation. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei -infected Swiss albino mice. This study demonstrated an efficient method of forming a nanomedicine delivery system for antimalarial drugs.
We investigated the antiplasmodial properties of crude extracts from Carica papaya leaves to trace the activity through bioassay-guided fractionation. The greatest antiplasmodial activity was observed in the ethyl acetate crude extract. C. papaya showed a high selectivity for P. falciparum against CHO cells with a selectivity index of 249.25 and 185.37 in the chloroquine-sensitive D10 and chloroquine-resistant DD2 strains, respectively. Carica papaya ethyl acetate extract was subjected to bioassay-guided fractionation to ascertain the most active fraction, which was purified and identified using high-pressure liquid chromatography (HPLC) and GC-MS (Gas chromatography-Mass spectrometry) methods. Linoleic and linolenic acids identified from the ethyl acetate fraction showed IC50 of 6.88 μg/ml and 3.58 μg/ml, respectively. The study demonstrated greater antiplasmodial activity of the crude ethyl acetate extract of Carica papaya leaves with an IC50 of 2.96 ± 0.14 μg/ml when compared to the activity of the fractions and isolated compounds.
Orientation: The environmental health graduates are required to complete community service before they could be registered as independent practitioners by the Health Professions Council of South Africa. Community service programme serves as the mechanism to recruit healthcare professionals who will improve the provision of equitable and quality healthcare.Research purpose: The study aimed to explore, identify and describe the factors that had an influence on the effective selection, placement and utilisation of environmental health graduates as well as an evaluation of the effectiveness of community service.Research approach/design and method: A quantitative, cross-sectional study was conducted using self-administered questionnaires. The study included 24 environmental health practitioners who completed their community service and 10 environmental health practitioners responsible for coordinating community service in the municipal, provincial and national spheres of government in the Eastern Cape province of South Africa during 2013–2016. Purposive sample was drawn from each population. T-test and chi-square test were used to determine the statistical significant differences. The open-ended question responses from the structured questionnaire were qualitatively analysed by an independent coder.Main findings: The findings revealed major problems regarding the effective implementation of community service that included decreasing number of community service posts, inadequate material resources, lack of induction, inconsistent supervision, and a lack of evaluation of the community service.Contribution: The study findings suggest important inequalities that should deserve urgent attention. Study concludes by presenting recommendations for the improvement of the community service in the environmental health.
Water, sanitation and hygiene (WASH) are vital indicators to healthy living and safe environments for child development. The aim of the study was to determine WASH status and practices in ECD centres located in low socio-economic areas of Nelson Mandela Bay during 2017. This cross-sectional study elicited responses from 46 ECD centres which had a total of 3,254 children and 172 caregivers. A structured questionnaire and visual observation were used. Using core WASH in schools' indicators (WinS) showed that despite improved water sources being available in 91% of the facilities, WinS for hygiene was poor. The study observed that 57% of the respondents had improved toilets accommodating both genders. In 29% of ECD centres, 6–10 children make use of a ‘pottie’ while in 9% of the cases, more than 20 children make use of one ‘pottie’. The use of the bucket system was noted in 22% of the ECD centres. In 79% of the ECD centres, children wash their hands in a communal plastic bowl. Only 11% of the study population washed hands hygienically under a running tap or tippy tap. WASH conditions in the ECD centres in the study area require urgent attention and further investigation for practical solutions. This article has been made Open Access thanks to the generous support of a global network of libraries as part of the Knowledge Unlatched Select initiative.
Background. Schistosomiasis remains a public health concern in South Africa (SA), with the highest prevalence of infection found among schoolchildren under the age of 15 years. Knowledge, attitude, and practices (KAP) studies on schistosomiasis among schoolchildren under the age of 15 years are lacking in the study area. The study therefore assessed primary schoolchildren in Grades 4–7 to determine their knowledge regarding schistosomiasis in the various ages represented in these grades. Methods. The study employed a quantitative descriptive, cross-sectional survey research design approach. A structured, close-ended, Likert-scale, self-administered questionnaire was used to collect data from 458 learners in Grades 4 to 7 aged from 9 to 16 years. Data were analysed using Statistica version 13 software. Bivariate and multivariate techniques were further used to analyse and describe the data and significant associations at p = 0.05 were further interrogated using Cohen’s d and Cramér’s V , to determine the practical significance. Results. Of the 458 learners who completed the questionnaire, 248 (54%) acknowledged having heard of schistosomiasis previously. There was a positive correlation between knowledge and attitude (0.779). The KAP scores were calculated as a percentage ranging between 0% and 100%, and this range was split into five equal width intervals 0–19%, 20–39%, 40–60%, 61–80%, and 81–100%. For knowledge, 210 (46%) of the participants obtained a score in the interval 0–19%. For attitudes, 237 (52%) of the participants obtained a score in the interval 0–19%. Therefore, the overall knowledge and attitudes among the study participants towards schistosomiasis were poor. There was a significant difference ( p = 0.0005 , V = 0.42 medium) between male and female participants relating to their practices. It was observed that a high percentage, 69 (15%) of males reported to swimming in slow-moving water compared to a significantly lower percentage, 9 (5%) of females. Furthermore, 23% of the participants reported that there was a river on the way to school. Conclusion. The study revealed that there was a positive correlation between knowledge and attitude. The overall knowledge and attitudes on schistosomiasis were poor. Furthermore, a gender-related difference based on practices emerged significant in the study. The findings are thus valuable in designing effective and targeted schistosomiasis control programmes.
To explore and describe caregivers' handwashing knowledge and practices in the context of underprivileged urban communities. Design: A qualitative descriptive and exploratory study was conducted during August and September 2017, through five focusgroup discussions, with caregivers of children younger than five years attending ECD centres. Setting: Early childhood development (ECD) centres in various underprivileged communities in Ibhayi and Motherwell, Nelson Mandela Bay. Subjects: Thirty-five adults, aged between 24 and 60 years, functioning as primary or secondary caregivers to 105 children, participated.Results: Three themes emerged, of which the first entailed the knowledge of handwashing and compliance with water, sanitation and hygiene (WASH) recommendations. Practical challenges that may prevent compliance with recommendations were highlighted. Handwashing as a social norm emerged as the second theme, and reflection on strategies at primary health care level to increase awareness regarding handwashing in communities was the third theme. Conclusion and recommendations:Current handwashing counselling at primary health care sites may not be perceived as relevant in underprivileged communities. However, with adequate support ECD practitioners have influence to change the handwashing behaviour and knowledge of pre-school children and families. Furthermore, communication and dissemination of handwashing messages should be clear, practical and relevant to address inappropriateness of current poster images and should include suggestions on what to do when experiencing infrastructure challenges and in times of water restrictions. Health-promotion strategies should focus on optimising handwashing practices while caring for pre-school children.
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