[关键词]
[摘要]
目的:探讨脱氧胆酸基接枝的壳聚糖衍生物负载姜黄素纳米粒的合成方法及该药物纳米粒对人视网膜色素上皮(hRPE)细胞的作用。
方法:合成姜黄素/壳聚糖-脱氧胆酸纳米粒并分析其性能。将负载荧光染料异硫氰酸荧光素的壳聚糖-脱氧胆酸及姜黄素/壳聚糖-脱氧胆酸作用于hRPE细胞24h后,于倒置荧光显微镜下观察避光培养1、3、5d后二者与hRPE细胞的相互关系。
结果:通过将姜黄素与壳聚糖-脱氧胆酸混合制成负载药的壳聚糖衍生物纳米粒为淡黄色; 药物从纳米粒中的释放在96h后达到平衡,累积释放药物量为31.6%。异硫氰酸/壳聚糖-脱氧胆酸与hRPE细胞作用1d后,壳聚糖-脱氧胆酸纳米粒大部分仍位于近细胞膜的部位; 作用3d后,纳米粒逐渐向细胞核会聚,且大部分位于细胞核周围; 作用5d后,可看到壳聚糖-脱氧胆酸纳米粒已进入细胞核,且纳米粒可能在细胞内溶酶体的作用下有部分降解。姜黄素/壳聚糖-脱氧胆酸纳米粒和hRPE细胞作用的关系与壳聚糖-脱氧胆酸大致相同。
结论:通过壳聚糖-脱氧胆酸包载的姜黄素纳米粒能持续释放出姜黄素,具有较持久的缓释功能。
[Key word]
[Abstract]
AIM: To investigate the synthesis method of curcumin nanoparticles grafted with deoxycholic acid and the effect of curcumin nanoparticles on human retinal pigment epithelial(hRPE)cells.
METHODS: The synthesis and performance analysis of Cur/Chit-DC. The relationship between FITC/Chit-DC and hRPE cells was observed under an inverted fluorescence microscope after treating hRPE cells with FITC(FITC/Chit-DC)and Cur/Chit-DC(FITC/Cur/Chit-DC)for 24h, keeping them in dark for 1, 3 and 5d respectively.
RESULTS: By mixing Cur and Chit-DC, the nanoparticles containing chitosan derivatives were light yellow. The drug release from the nanoparticles reached equilibrium after 96h, and the cumulative drug release amount was 31.6%. After FITC/Chit-DC was treated with hRPE cells for 1d, most of Chit-DC nanoparticles were still located near the cell membrane. After 3d, the nanoparticles gradually converged towards the nucleus and most of them were located around the nucleus. After 5d, it was observed that Chit-DC nanoparticles had entered the nucleus and were partially degraded under the action of intracellular lysosomes. The relationship between Cur/Chit-DC and cellular action is roughly the same as the relationship between Chit-DC and cellular action.
CONCLUSION: Cur can be continuously released from Cur/Chit-DC nanoparticle, which has long-lasting sustained-release function.
[中图分类号]
[基金项目]
海南省自然科学基金项目(No.819MS133)