Sustain Release Microsponge Based Drug Delivery System for the Plasmodium Treatment: Formulation Development and In vitro - In vivo Evaluation

Abstract

The aim behind the present research work was to develop a microsponge based dosage form for sustained delivery of Artemether prepared by quasi-emulsion solvent diffusion method using polymer Eudragit RS-100 with two factors drug-polymer ratios and rate of agitation for optimization purposes, these two factors influences micro particles and physical properties. Sophisticated characterization techniques followed for the formed microsponges were DSC, FT-IR, SEM and particle size analysis, along with morphology, drug loading and in-vivo - in-vitro drug release data, DSC and FT-IR data reveals that there were no chemical interactions between drug Artemether and polymers Eudragit RS-100 used. The drug-polymer ratio and rate of agitation showed remarkable impact on drug content, encapsulation efficiency and particle size, SEM micrographs revealed that microsponges formed were spherical in shape with porous surface, and had 21.2591 ± 0.08 μm mean particle size. The microsponges were then loaded in capsules followed by in-vitro drug release study; which depicted that microsponges with drug-polymer ratio of 1:5 at 500 rpm were more proficient to give extended drug release of 96.46 ± 0.06 % at the end of 12 h, better in contrast to conventional market formulation. Hence, the developed microsponge based formulation of Artemether would be an expectant, promising substitute to conventional therapy for the Plasmodium treatment.

Keywords:

• Artemether
• SEM
• DSC
• particle size analysis
• HPLC