Physicochemical Characterization of Artemether-Entrapped Solid Lipid Microparticles Prepared from Templated- Compritol and Capra hircus (Goat Fat) Homolipid

Abstract

The purpose of this study was to formulate and evaluate the physicochemical properties of artemetherloaded solid lipid microparticles (SLM) prepared from templated-compritol 888^®ATO and Capra hircus (goat fat) homolipid. Various ratios of compritol 888^®ATO, goat fat and Phospholipon^® 90G were used to prepare the templated lipid matrices and characterized by differential scanning calorimetry (DSC). Plain and artemether-loaded SLM (0, 1.0, 3.0 and 5.0% drug) were prepared by melt-homogenization. The SLM were characterized regarding the compatibility by DSC, morphology and particle size by polarized light microscopy (PLM), encapsulation efficiency (EE%), in vitro release in simulated gastric fluid (SGF, pH 1.2), simulated intestinal fluid (SIF, pH 7.2) and alcoholic buffer (pH 3.6), and time-resolved pH-dependent stability. Stable, smooth and mostly spherical SLM with particle sizes in the range 18.77-43.79 μm and EE% ranging from 62.22% to 99.05% were obtained. DSC results showed the compatibility of drug and the formulation excipients as well as the stability of artemether in the developed SLM. Results showed significantly (p<0.05) higher drug release (88.25%) in alcoholic buffer than in SIF and SGF. By implication, incorporation of alcohol in the formulation would be a practical approach to improve artemether bioavailability from the SLM. This study has shown that the physicochemical properties of artemether were improved by SLM based on templated-compritol 888^®ATO and goat fat.

Dhaka Univ. J. Pharm. Sci. 20(1): 67-80, 2021 (June)