Enhancement of dissolution of Prosopis africana stem bark extract by solid dispersion technique

Abstract

Background and Aims: Literature reveals many benefits and potentials of the stem bark extract of Prosopis africana but like other plant extracts, its use in the oral pharmaceutical formulation is limited due to its poor aqueous solubility, reduced absorption, and bioavailability. The aim of this study is to develop oral solid dispersion formulations of Prosopis africana extract to improve its dissolution and possible bioavailability. Methods: Crushed stem bark of Prosopis africana was macerated in methanol for 72 h at room temperature. The resulting extract (PREx) was incorporated into polyethylene glycol 4000 (PEG 4000) by the solvent-evaporation and melt-fusion methods using different ratios (1:1, 1:2, 1:4) of extract to polymer; physical mixtures of the same ratio of extract to polymer were also prepared. The crystallinity of the formulations was characterized by differential scanning calorimetry (DSC), possible interaction/incompatibility between the extract and polymer was determined by Fourier transform infra-red spectroscopy (FT-IR). In vitro, release and modeling of the release profile were also determined. Results: No interaction was found between materials used for the preparations while DSC thermograms showed a reduction in crystallinity of PREx in the solid dispersion formulations. In vitro release profile of the formulation prepared with the highest polymer concentration by the melt-fusion method (M3) showed the greatest enhancement in dissolution. Conclusion: This study shows solid dispersion prepared by the melt-fusion method as an effective technique for the enhancement of dissolution of poorly water-soluble Prosopis africana extract.

Keywords

• Melt-fusion
• Prosopis africana extract
• PEG 4000
• solid dispersion

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