Study on Preparation and in Vitro Release of Artesunate-loaded Enteric Fibers

OBJECTIVE To prepare artesunate-loaded enteric fibers and investigate their release behavior in vitro. METHODS A series of artesunate-loaded Eudragit fibers S100/ART and L100-55/ART were prepared by electrospinning, with Eudragit S100 and L100-55 as the polymer matrix and adding artesunate. The content of artesunate was determined by UV-Vis spectrophotometry, and the drug loading and entrapment efficiency of fibers S100/ART and L100-55/ART were calculated. The morphology and thermal stability of the fibers were characterized by SEM and TG, respectively. The physical status of artesunate in fibers was determined by FTIR. The in vitro drug release of the fibers was investigated by the paddle method using a dissolution tester. RESULTS The drug-loaded Eudragit fibers S100/ART and L100-55/ART had uniform structures, good thermal stability, controllable drug loading, and high entrapment efficiency. Artesunate was dispersed in fibers in amorphous state. Small amount of the drug were released from these fibers in the simulated gastric fluid of pH 1.2, while in the simulated intestinal fluid of pH 6.8 most of the drug were released. Moreover, S100/ART released less artesunate at pH 1.2 and more at pH 6.8 than L100-55/ART. S100/ART and L100-55/ART could also achieve the sustained release of artesunate. CONCLUSION The drug-loaded Eudragit fibers S100/ART and L100-55/ART can be used as enteric formulations of artesunate, and the artesunate-loaded enteric fiber S100/ART has better performance than L100-55/ART. The fabricated artesunate-loaded enteric fibers can be applied to achieve intestinal-targeted delivery and release of artesunate, and hopefully improve the oral bioavailability of artesunate.