Lumefantrine-neusilin® based amorphous multicomponent solid dispersion: In vivo and in vitro characterization

Purpose: To develop Neusilin-based amorphous multi-component solid dispersions (NAM-SDs) to improve poor aqueous solubility, low bioavailability and absorption of lumefantrine and enhance the antiplasmodial activity.Methods: Solvent evaporation technique was adopted to produce second-generation SDs (N1 - N3); third-generation SDs (N4 - N6 and N10 - N12); and multi-component SDs, NAM-SDs, (N7 - N9 and N13 - N18). In vitro drug release, in vivo anti-plasmodial activity, differential scanning calorimetry (DSC), and wide-angle x-ray diffraction (WAXD) were carried out on the SDs.Results: The highest drug release (80 %) was observed in multi-component SDs (NAM-SDs, formulation N17 containing Kollidon® VA 64). A significant antiplasmodial activity (p < 0.05) was observed in mice that received NAM-SDs. The DSC and WAXD studies showed that the formulations solubilized and exhibited an amorphous state.Conclusion: Multi-component amorphous-based lumefantrine SDs (NAM-SDs) may serve as a potential alternative carrier system for oral lumefantrine delivery.