Artemether And Piperine Encapsulated With PLGA-Chitosan Core-shell Structure Microparticles For Enhanced Sustained Release

Malaria,a malignant parasitic disease that spread by specific types of Plasmodium species,but plasmodium falciparum(P.F)is the most severe form of parasite transported by anopheles mosquitoes that rapidly carry P.F into the bloodstream,infect the liver cells,and red blood cells.Artemether,a highly efficient antimalarial drug revealed to possess the potential to treat the patients suffering from P.F.However,therapeutic potency and clinical dissemination are restricted by its poor bioavailability,short half-life,and rapid degradation.These limitations can be solved by a smart combination with natural bio-enhancer like piperine.Herein,we report the conjugation of artemether and piperine encapsulated polylactic-co-glycolic acid(PLGA)and chitosan-based core-shell microparticles.The particles were prepared using a coaxial electrospray(CES)system,which has been established as a promising strategy to develop core-shell microparticles.By optimized process parameters,artemether-piperine loaded PLGA-chitosan microparticles(AP-PLGA-CS),and artemether-piperine loaded PLGA microparticles(AP-PLGA)with an average size of 2.2 and 1.7?m were produced with the high encapsulation efficiency(EE)of 75.6%and 78.8%with 9.4%and 9.7%of loading rate(LE)respectively having sustained release profile.Furthermore,XRD and DSC results demonstrated that artemether and piperine were transformed to amorphous state when encapsulated in the microparticles through the CES process.The results suggest that the CES has offered a platform to encapsulate multiple drugs with high loading rate in a single step.The encapsulation of drugs in the core tenders its sustained release that can be employed to improve the bioavailability for labile acid drugs like artemether.