College of Basic Science, Jinzhou Medical University, Jinzhou 121001, China.
Molecules. 2020 Mar 9;25(5):1221. doi: 10.3390/molecules25051221.
Large-scale preparation of biocompatible drug delivery systems with targeted recognition and controlled release properties has always been attractive. However, this strategy has been constrained by a lot of design challenges, such as complicated steps and premature drug release. Herein, in this paper, we address these problems by a facile in situ mineralization method, which synthesizes biodegradable tea polyphenol coated monodisperse calcium phosphate nanospheres using for targeted and controlled delivery of doxorubicin. Dialysis diffusion method was used to control ion release to form mineralized nanospheres. The polyphenol coatings and calcium phosphate used in this work could be biodegraded by intracellular glutathione and acidic microenvironment, respectively, resulting the release of encapsulated drug. According to confocal fluorescence microscopy, and cytotoxicity experiments, the prepared tea polyphenol functionalized, doxorubicin loaded calcium phosphate nanospheres were confirmed to have highly efficient internalization and obvious cell killing effect on target tumor cells, but not normal cells. Our results suggest that these tea polyphenols functionalized calcium phosphate nanospheres are promising vehicles for controlled release of an anticancer drug in cancer therapy.
大规模制备具有靶向识别和控制释放性能的生物相容性药物输送系统一直很有吸引力。然而，这种策略受到了许多设计挑战的限制，例如复杂的步骤和过早的药物释放。在此，我们通过一种简便的原位矿化方法来解决这些问题，该方法使用可生物降解的茶多酚包覆的单分散磷酸钙纳米球合成多柔比星的靶向和控制释放。透析扩散法用于控制离子释放以形成矿化纳米球。本工作中使用的多酚涂层和磷酸钙分别可以被细胞内谷胱甘肽和酸性微环境降解，从而释放包封的药物。根据共聚焦荧光显微镜和细胞毒性实验，证实了制备的茶多酚功能化、多柔比星负载的磷酸钙纳米球对靶肿瘤细胞具有高效的内化作用和明显的细胞杀伤作用，而对正常细胞没有。我们的研究结果表明，这些茶多酚功能化的磷酸钙纳米球有望成为癌症治疗中抗癌药物控制释放的载体。
