A Comparative Study of Influence of Different Polymers on Lumefantrine: Piperine Solid Dispersion

Abstract

To improve the oral delivery of biopharmaceutical classification system (BCS) class II drugs, solid dispersions techniques are generally adopted in drug product develooment in pharmaceuticals. The choice of polymer in these designs significantly affects a drug’s solubility and dissolution properties. The crystalline nature and the involvement of P-glycoprotein in active ingredient efflux further hinder drug absorption and bioavailability. In this study, solid dispersion (SD) of an antimalarial drug (lumefantrine) combined with piperine (a P-gp and CYP3A4 inhibitor), was created using different polymeric carriers: Soluplus, Klucel, Poloxamer, Povidone/PVP K30 (PVP), and Copovidone/Kollidon® VA64 (KOL). Among these, LUMF-PIP solid dispersion with SOL exhibited the maximum water solvency and fastest release across various media. These findings indicate that the choice of polymeric carrier significantly impacts LUMF’s solubility and dissolution behavior in solid dispersion. SOL emerges as the most promising polymer for enhancing LUMF’s solubility and dissolution, ultimately leading to improved bioavailability upon oral administration.