Solid Self-Microemulsifying Drug Delivery System (SMEDDS) of Primaquine: Bio-distribution and Enhanced Liver Uptake

Abstract

Aim: The present research work was aimed at developing a self-microemulsifying drug delivery system (SMEDDS) of Primaquine (PQ) with increased liver uptake and hence enhanced antimalarial efficacy against the liver stages of Plasmodium vivax. Materials and methods: SMEDDS was formulated using generally regarded as safe (GRAS) excipients and adsorbed on Aerosil 200. The optimized SMEDDS were characterized for various physicochemical parameters. Pharmacodynamic efficacy in murine model was evaluated using Peter’s Four Day Suppresive Test. Biodistribution studies were carried out using flow cytometry. Results: The adsorbed SMEDDS showed a particle size of 75 nm and exhibited enhanced antimalarial efficacy as compared to marketed formulations. Biodistribution studies revealed enhanced uptake in the liver. Conclusion: Preliminary studies in lower animals indicated the potential of SMEDDS to enhance the uptake of PQ at its site of action i.e. liver.