Zhang Denghao, Tao Liang, Zhao Hongli, Yuan Huihui, Lan Minbo
a Shanghai Key Laboratory of Functional Materials Chemistry, and Research Centre of Analysis and Test , East China University of Science and Technology , Shanghai 200237 , P.R. China.
J Biomater Sci Polym Ed. 2015;26(8):468-82. doi: 10.1080/09205063.2015.1030136. Epub 2015 Apr 8.
Functional polymeric micelles play an important role in the efficient delivery of therapeutic drugs into tumours. In this study, a functional drug delivery platform with ligands for targeting and fluorescent imaging was designed based on Pluronic F127 (PF127). Using folic acid (FA) and fluorescein isothiocyanate (FITC) to chemically conjugate with PF127, two functional polymers, Pluronic F127-FA (PF127-FA) and Pluronic F127-FITC (PF127-FITC), were synthesized. Solasodine-loaded micelles were then prepared via the thin-film hydration method. By employing A549 and HeLa cells, the results of in vitro cell assays performed using confocal laser scanning microscopy and flow cytometry suggested that the proposed micelles could provide the desired specific targeting and fluorescent imaging functions. In addition, the results of in vitro cytotoxicity experiments showed that the growth inhibition rates of A549 and HeLa cells treated with solasodine-loaded micelles were remarkably higher than those of cells treated with free solasodine. Solasodine-loaded micelles exhibited a more distinct inhibitory effect against HeLa cells than against A549 cells. Thus, an effective drug delivery system for targeting and imaging cancer cells was developed.
功能性聚合物胶束在将治疗药物有效递送至肿瘤中发挥着重要作用。在本研究中,基于普朗尼克F127(PF127)设计了一种具有靶向和荧光成像配体的功能性药物递送平台。使用叶酸(FA)和异硫氰酸荧光素(FITC)与PF127进行化学共轭,合成了两种功能性聚合物,即普朗尼克F127-叶酸(PF127-FA)和普朗尼克F127-异硫氰酸荧光素(PF127-FITC)。然后通过薄膜水化法制备了负载澳洲茄碱的胶束。通过使用A549和HeLa细胞,利用共聚焦激光扫描显微镜和流式细胞术进行的体外细胞实验结果表明,所提出的胶束能够提供所需的特异性靶向和荧光成像功能。此外,体外细胞毒性实验结果表明,负载澳洲茄碱的胶束处理的A549和HeLa细胞的生长抑制率显著高于游离澳洲茄碱处理的细胞。负载澳洲茄碱的胶束对HeLa细胞的抑制作用比对A549细胞更明显。因此,开发了一种用于靶向和成像癌细胞的有效药物递送系统。