Co-delivery of Artemether and Piperine via Core-Shell Microparticles for Enhanced Sustained Release

Abstract Artemether, a highly efficient antimalarial drug, possesses the potential to treat patients suffering from Plasmodium-falciparum (P.F). However, artemether can be degraded rapidly by stomach acids and cleared quickly from the body after oral administration, leading to poor therapeutic effects, which is a significant hindrance in the clinical cure of malaria. To overcome this problem, we developed two types of core-shell microparticles co-loaded with artemether and piperine based on polylactic-co-glycolic acid (PLGA) and chitosan (CS) by using the promising coaxial electrospray system (CES) for sustained drug release. 1.9 μm artemether-piperine loaded PLGA-chitosan (AP-PLGA-CS) microparticles and 1.3 μm artemether-piperine loaded PLGA (AP-PLGA) microparticles were successfully fabricated using optimized operation parameters of CES. X-ray diffractometer (XRD) and differential scanning calorimetry (DSC) results showed the presence of artemether and piperine within the polymer matrix when encapsulated in the microparticles after CES. Both prepared AP-PLGA-CS and AP-PLGA microparticles exhibited high drug encapsulation and drug loading efficiency. Moreover, both of them displayed enhanced sustained drug release behavior due to the PLGA or PLGA-CS shell, which protected the fast degradation of artemether from the acidic gastric juice. All results suggested that the AP-PLGA-CS and AP-PLGA microparticles not only embrace the great potential in the application of malaria treatment but also provide a promising platform to encapsulate multiple drugs in polymeric particles for drug delivery.