Abstract

FORMULATION, EVALUATION AND CHARACTERIZATION OF LUMEFANTRINE – PEG BASED SOLID DISPERSION

Calister E. Ugwu, Nicholas C Obitte and Oluchi B Madu

Abstract

Poor aqueous solubility of drugs presents one of the major challenges to be tackled in order to improved oral bioavailability of some drugs. Lumefantrine is one of such drug with solubility and permeability challenges. Fusion method was used in preparing lumefantrine PEG solid dispersion. Different drug: carrier ratios (1:1, 1:2 and 1:3) were used. Solubility study of the drug was carried out. The following evaluation studies were done: percentage yield, loading efficiency, micromeritics properties, in vitro release profile. Then, characterized using differential scanning calorimetry (DSC) and wide angle x-ray diffraction (WAXD). The result showed that lumefantrine showed highest solubility in PEG 6000, Kollidon® 12 PF and kolliphor® HS 15 as 98.36 ± 0.03, 96. 99 ± 0. 01 and 95.76 ± 0.11 mg/ ml respectively. The batch Pk17 had the highest loading efficiency (L.E) of 88.20 ± 0.22 %. There was significant variation (p < 0.5) in the L.E of SDs formulation (Pk 10 – 21) and (P1 – 9) without Kollidon® 12 PF. This variation might be due to high solubilizing capacity of Kollidon® 12 PF. The batch Pk17 also exhibited the highest release profile amomg the batches. The DSC and WAXD results also showed less crystalline products with higher solubilization potential and also characterized the formulation as a eutectic solid dispersion. Lumenfantrine – PEG loaded solid dispersion with Kollidon 12 PF had an improvement on the solubility and dissolution rate of the drug with potential inhibition of crystal formation.

Keywords: lumefantrine, PEG 6000, Kollidon® 12 PF, Solid dispersion.