PREPARATION, CHARACTERIZATION AND DISSOLUTION ENHANCEMENT OF DIHYDROARTEMISININ MICROPARTICLES

Abstract

The objective of the present study was to prepare a Dihydroartemisinin microparticles using spray drying method to enhance the solubility and 
dissolution rate which will help for improvement of oral bioavailability. Dihydroartemisinin is the active metabolite of artemisinin compound and a 
drug of choice for treatment of malaria. Dihydroartemisinin has poor aqueous solubility, incompletely absorbed after oral intake due to poor dissolution 
characteristics in the intestinal fluid which limits its application. To address these issues, spray dried microparticles of Dihydroartemisinin were prepared 
using Poloxamer 188, non-ionic surfactant with different ratios of drug and carrier. Based on results of solubility study, spray dried microparticles 
formulation with highest aqueous solubility was analyzed for Fourier transform infrared spectroscopy, X-ray powder diffraction and Differential 
scanning calorimetry study. Spray dried microparticles evaluated for determination of percent yield, solubility, drug content, encapsulation efficiency, 
micromeritic properties and in vitro dissolution parameters. Surface morphology study by Scanning electron microscopy revealed spherical shape of 
microparticles. Prepared microparticles showed good flow property, improved aqueous solubility and faster in vitro dissolution rate compared with pure 
drug. The spray dried microparticles of Dihydroartemisinin with Poloxamer 188 in a ratio of 1:4 w/w showed 2.5 times enhancement of aqueous 
solubility and > 95 % drug release in 120 min when compared with pure drug alone. Thus from the result it can be concluded that spray dried 
microparticles of Dihydroartemisinin using Poloxamer 188 is useful technique to enhance the solubility and dissolution rate that will help to improve 
oral bioavailability.