Huo Peipei, Han Xinxu, Zhang Wenyu, Zhang Jing, Kumar Parveen, Liu Bo
Laboratory of Functional Molecules and Materials, School of Physics and Optoelectronic Engineering, Shandong University of Technology, Xincun West Road 266, Zibo 255000, China.
School of Materials Science and Engineering, Shandong University of Technology, Zibo 255000, China.
Pharmaceutics. 2021 Aug 9;13(8):1228. doi: 10.3390/pharmaceutics13081228.
The application of artemisinin (ART) in the treatment of malaria has been restricted to a certain degree due to its inherent limitations, such as short half-life, poor solubility, limited bioavailability, and re-crystallization. Electrospun nanofibers loaded with ART provide an excellent solution to these limitations and yield sustained drug release as well as inhibition of drug re-crystallization. In this study, ART-loaded polycaprolactone (PCL)/collagen (Col) nanofibers with different proportions of polymers were prepared. ART-loaded PCL/Col nanofibers were characterized, and further ART anti-crystallization and release behaviors were studied. SEM was used to observe the morphology of PCL/Col nanofibers. X-ray diffraction (XRD) was used to characterize the physical state of ART in ART-loaded PCL/Col nanofibers. Fourier transform infrared spectroscopy (FTIR), water contact angle measurement, weight loss, degree of swelling, and drug release experiments can verify the differences in performance of ART-loaded PCL/Col nanofibers due to different polymer ratios. The release curve was analyzed by kinetics, showing sustained release for up to 48 h, and followed the Fickian release mechanism, which was shown by the diffusion index value obtained from the Korsmeyer-Peppas equation.
由于青蒿素(ART)存在固有局限性,如半衰期短、溶解度差、生物利用度有限以及重结晶现象,其在疟疾治疗中的应用受到了一定程度的限制。负载ART的电纺纳米纤维为解决这些局限性提供了极佳的方案,能够实现药物的持续释放并抑制药物重结晶。在本研究中,制备了不同聚合物比例的负载ART的聚己内酯(PCL)/胶原蛋白(Col)纳米纤维。对负载ART的PCL/Col纳米纤维进行了表征,并进一步研究了ART的抗结晶和释放行为。使用扫描电子显微镜(SEM)观察PCL/Col纳米纤维的形态。采用X射线衍射(XRD)表征负载ART的PCL/Col纳米纤维中ART的物理状态。傅里叶变换红外光谱(FTIR)、水接触角测量、失重、溶胀度和药物释放实验可以验证由于聚合物比例不同而导致的负载ART的PCL/Col纳米纤维性能差异。通过动力学分析释放曲线,结果表明其可持续释放长达48小时,并遵循菲克扩散释放机制,这由从Korsmeyer-Peppas方程获得的扩散指数值所证明。