Development and characterization of Soluplus-based solid dispersion to improve solubility
Résumé
Purpose: To improve the solubility of lumefantrine (lum), using developed solid dispersions (SDs) with Soluplus and Kollidon VA 64, at various lum: carrier ratios to produce new-generation solid dispersions (NG.SDs). Methods: Lumefantrine:soluplus® ratios; 1:1, 1:2, and 1:3 were employed in preparing samples B1 – B3 (2nd generation SDs), B4 – B9 (3rd generation SDs), B10 – B18 (NG.SDs). Prepared batches (B10 – B18) were characterized for loading efficiency (LE), Differential scanning calorimetry (DSC) and wide-angle x-ray diffraction (WXRD). In vitro release was determined using USP Type I Apparatus. In vivo antimalarial study on 20 female Albino rats weighing 180 – 200 g was done by adopting Peter’s four-day suppressive test, where 10 mg/kg of NG.SDs were used as test group and chloroquine tablets (CQ) were used as positive control group. Drugs were orally administered once daily for three days, and parasitemia level was assessed. Results: Developed NG.SDs gave the highest LE of 96.70 ± 0.12 % (p < 0.05) and the fastest drug release when compared to other generations (2nd and 3rd) of solid dispersions (samples B1 – B9). More so, DSC and WAXD of selected NG.SDs depicted broader peaks and less crystallinity when compared to pure lumefantrine (p < 0.05), indicating higher drug solubilization and amorphous existence in SDs. A significantly (p < 0.05) higher antimalarial activity (96 %) was obtained for the developed NG.SDs than physical mixture, CQ and pure lumefantrine. Conclusion: Soluplus and Kollidon VA 64-based solid dispersion matrix is a promising approach for improving the poor aqueous solubility of Lumefantrine.
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