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 have encapsulated artemether in poly(lactic-co-glycolic) acid (PLGA) core–shell microparticles (MPs) using the coaxial electrospray 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 artemether-loaded PLGA-MPs with an average size of 2 μm, an encapsulation efficiency of 78 ± 5.6%, and a loading efficiency of 11.7%. The in vitro release study demonstrates the sustained release of artemether from the core–shell structure in comparison with that of plain artemether and that of MPs produced by single-axial electrospray without any relevant cytotoxicity. The in vivo studies are performed to evaluate the pharmacokinetic characteristics of the artemether-loaded PLGA-MPs. Our study implies that artemether can be effectively encapsulated in a protective shell of PLGA for controlled release kinetics and enhanced oral bioavailability.

中文翻译：

---

蒿甲醚-加载聚（乳酸-特点共同增强封装效率的验证和生物利用度：通过同轴电-glycolic）酸微粒捏造

蒿甲醚是治疗抗氯喹和恶性疟原虫菌株的最有效药物之一。但是，其生物利​​用度差阻碍了它的治疗效力。在聚为了克服这种限制，我们已经封装蒿甲醚（乳酸-共-乙醇酸（PLGA）核-壳微粒（MPs）使用同轴电喷雾方法。通过优化的工艺参数（包括液体流速和施加的电压），系统地进行实验以产生稳定的锥形喷射模式，以生产平均粒径为2μm，包封效率为78±5.6％的蒿甲醚负载的PLGA-MP。 ，并且加载效率为11.7％。体外释放研究表明，与普通蒿甲醚和单轴电喷雾产生的MP相比，蒿甲醚从核-壳结构中持续释放没有任何相关的细胞毒性。进行体内研究以评估蒿甲醚负载的PLGA-MP的药代动力学特征。