Development and characterization of sustained-release artemether loaded solid lipid microparticles based on mixed lipid core and a polar heterolipid.
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Date
2022
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Publisher
African Journal of Pharmaceutical Research & Development
Abstract
The objective of this study was to formulate and evaluate artemether-loaded solid lipid microparticles SLMs from templated captex 300® and Capra hircus (goat fat) homolipid for sustained delivery in the treatment of malaria. Various ratios of captex 300®, goat fat and Phospholipon® 90G were used to prepare the templated lipid matrices and characterized by differential scanning calorimetry (DSC). The templated lipid matrices were employed to formulate SLMs containing various concentrations (1.0, 3.0 and 5.0 %w/v) of artemether by melt-emulsification technique. Physicochemical characterizations were performed on the SLMs with respect to mean particle size, morphology, encapsulation efficiency, compatibility, time-dependent pH stability and drug release in phosphate buffered saline (PBS, pH 7.4) compared with artemether injection (control). The DSC results showed that the formulated lipid matrices were suitable for the development of the SLMs. Stable spherical artemether-loaded SLMs with encapsulation efficiency and mean particle size that ranged from 20.49 ± 1.15 % to 87.02 ± 3.13 % and 1.60 ± 0.05 μm to 21.30 ± 0.50 μm, respectively, were developed. Among the formulations, SLMs based on Captex 300® and goat fat (1:1) at 1.0 and 3.0% artemether concentrations (batches A1 and A2) as well as SLMs based on Captex 300® and goat fat at (2:1) at 1.0% artemether concentration (batch C1) gave significantly (p<0.05) greater in vitro drug release in PBS than artemether injection. This study has shown that artemether-loaded SLMs based on Captex 300® and goat fat templated with Phospholipon® 90G could be employed as an alternative sustained-release formulation than artemether injection for enhanced malaria treatment.
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Keywords
Artemether-loaded solid lipid microparticles (SLMs), sustained release, Capra hircus (goat fat), captex 300®, Phospholipon® 90G