Artemisinin-Polyvinylpyrrolidone Composites Prepared by Evaporative Precipitation of Nanosuspension for Dissolution Enhancement

Nanoparticles of a poorly water-soluble anti-malarial drug, artemisinin (ART), and its composite particles with a hydrophilic polymer, polyvinylpyrrolidone (PVP), were synthesized using a nanofabrication method called the evaporative precipitation of nanosuspension (EPN). ART nanoparticles and ART/PVP composite particles containing ART nanoparticles coated with PVP were successfully prepared with the aim of improving the dissolution rate of ART. The effect of polymer concentration on the physical and morphological properties, and dissolution rate of the EPN-prepared ART/PVP composite particles was investigated. The crystallinity of ART nanoparticles decreased with increasing polymer concentration, as suggested by the differential scanning calorimetry and X-ray diffraction studies. The phase solubility studies revealed an A(L)-type of curve, indicating a linear increase in the drug solubility with PVP concentration. The dissolution of the ART nanoparticles and ART/PVP composite particles markedly increased as compared to that of the original ART powder due to lower particle size and reduced crystallinity of the drug particles. The percent dissolution efficiency (DE), relative dissolution (RD), t(75%) and similarity factor (f(2)) were calculated for the statistical analysis. Various mathematical models, viz., zero-order, first-order, Korsemeyer-Peppas and Higuchi, were applied to fit the experimental drug-dissolution data and diffusion was found to be the drug release mechanism. (C) Koninklijke Brill NV, Leiden, 2011