Characteristics of Artemether loaded PLGA microparticles fabricated by the coaxial electrospray:Validation of enhanced encapsulation efficiency and bioavailability

摘要

Artemether is one of the most effective drugs for the treatment of chloroquine-resistant and Plasmodium falciparum strains of malaria.However, its therapeutic potency is hindered by its poor bioavailability.To overcome this limitation,we encapsulate Artemether in poly (lactic-co-glycolic) acid (PLGA) core-shell microparticles by a coaxial eleetrospray (CES) method.With optimized process parameters including liquid flow rates and applied electric voltages, experiments are systematically carried out to generate a stable cone-jet mode to produce drug-loaded microparticles with an average size of around 2 μm and an encapsulation efficiency of 78.56％.The in vitro study demonstrates the controll978ed release of Artemether from the core-shell structure, in comparison with that of plain Artemether and that of microparticles produced by single-axial electrospray with no any relevant cytotoxicity.The in vivo studies are performed to evaluate the pharmacokinetic characteristics of the Artemether loaded PLGA microparticles.Our study implies that the CES process can potentially enhance the oral bioavailability of Artemether for greater therapeutic potency.