FORMULATION AND IN VITRO EVALUATION OF PHOSPHOLIPON® 90 H-BASED MICROPARTICLES FOR ORAL DELIVERY OF ARTEMETHER-LUMEFANTRINE

CHUKWUEMEKA CHRISTIAN MBAH*, SYLVESTER OGBONNA, ANDREW CHEKWUBE EZEGBE, OGOCHUKWU NGOZIKA CHIDINMA UMEH, JOSEPHAT IKECHUKWU OGBONNA, NICHOLAS CHINEDU OBITTE, SABINUS IFEANYI OFOEFULE, JACOB OKWUCHUKWU ONYECHI

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, 410001, Enugu State, Nigeria.

^{Afr. J Pharm Res Dev; Volume 12(3): 277-287 (2020)}

ABSTRACT

Lipid-based formulations enhance the delivery of poorly water-soluble drugs. In this study, Phospholipon® 90 H (P90H)-based microparticles co-formulation of artemether-lumefantrine (ATM-LUM) were prepared by emulsion-solvent evaporation method and evaluated for particle morphology, pH, yield, drug content, encapsulation efficiency (EE) and in vitro drug release. The in vitro drug release was studied over an 8 h period using a commercial tablet sample as reference. Microscopic examination of the formulations showed that spherical microparticles were formulated. The drug content and EE values were generally low for both drugs. This was attributed to probable poor dissolution of the drugs in the media used. The optimized formulation (5Mm) had the best pH stability over a one-month period. The products showed low and slow release profiles. However, the P90H-based microparticles formulation had significantly (p< 0.05) higher amounts of the drugs released relative to the reference, despite the generally low levels. The study showed that P90H could be used as a lipid carrier for formulation of ATM-LUM microparticles by emulsion-solvent evaporation technique. Further studies are recommended for the product development.

Email of correspondence: chukwuemeka.mbah@unn.edu.ng;

KEYWORDS: Microparticles; Phospholipids; Artemisinin-based combination therapies (ACTs); Artemether; Lumefantrine; Malaria.