Preparation and Characterization of Poloxamer 188 solid dispersions of Indomethacin

Abstract

The objective of this study was to improve the dissolution rate of a hydrophobic non-steroidal anti-inflammatory drug (NSAID), indomethacin (IMC) which shows poor bioavailability due to its poor solubility in the gastrointestinal fluids. Poloxamer 188 (PXM 188) was employed as a hydrophilic carrier at various IMC: PXM 188 ratios to prepare IMC-loaded solid dispersions (SDs) using the fusion method. Characterization based on surface morphology, particle size, absolute drug content and moisture sorption properties were carried out on the SDs. The in vitro release of IMC from the SDs was performed in simulated intestinal fluid without pancreatin (SIF, pH 7.4 ). Results indicate that discrete and irregularly-shaped SDs of mean particle size in the range 2.10 ± 0.68 to 6.95 ± 0.98 μm, which were stable over 3 months, were obtained. The moisture sorption studies indicated the amorphous/ microcrystalline state of IMC in the SDs, which also exhibited good encapsulation efficiency (EE%) and marked increase in the dissolution rate of IMC from the SDs when compared to pure IMC. Increasing PXM 188 concentration in SD formulation resulted in an increase in the dissolution rate of the drug (IMC). This study has shown that IMC/PXM 188 SDs could be a promising approach for dissolution and bioavailability enhancement of the poorly water-soluble drug, IMC.

Journal of Pharmaceutical and Allied Sciences, Vol. 9 No. 3 (2012)