Development and Evaluation of Artemether-loaded Microspheres Delivery System for Oral Application in Malaria Treatment doi.org/10.26538/tjnpr/v5i11.23
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Abstract
The application of artemether for the treatment of malaria is limited by its poor solubility leading to low bioavailability. The current study formulated sustained-release artemether mucoadhesive microspheres for oral delivery to prolong oral artemether delivery and improve the low bioavailability. Microspheres were formulated with mixtures of Eudragit®RS100 and Eudragit®RL100 in ratios of; 1:1 (A1), 1:3 (A2), and 3:1 (A3) by solvent evaporation techniques. The percentage yield, particle sizes, encapsulation efficiency (EE%), flow property, differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), bioadhesion study, in vitro and in vivo studies of the microspheres were evaluated and characterized. Results show that microspheres exhibited an overall high percentage yield of up to 98%. Particle sizes were between 29.40 ± 0.18 - 41.42 ± 0.12 µm. EE (%) obtained were 93.0, 94.5, and 95.0% for A1, A2, and A3, respectively. Flow characteristics indicated that the microspheres had good flowability. Thermal analysis of the drug and the microspheres showed sharp melting peaks which indicated that the drug was pure and crystalline. Morphological characteristics exhibited fairly spherical in shape. Bioadhesion properties depicted that microspheres exhibited good mucoadhesion properties on the bovine ileum. Drug release in simulated gastric fluid (SGF) ranged from 2.24 to 19.3% as compared to 60.43-83.31% in simulated intestinal fluid (SIF). The decreased in parasitemia levels are 91.78 ± 0.53%, 87.35 ± 0.23%, and 81.82 ± 0.31% for A3, A2 and A1, respectively. This method shows a promising result for possible delivery of artemether with improved sustained release activity.
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