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目的:研究CD44受体单靶向的透明质酸-十八烷基(HA-C18)、叶酸和CD44受体双靶向的叶酸-透明质酸-十八烷基(FA-HA-C18)载紫杉醇(PTX)胶束的肿瘤细胞靶向功能。方法:选择叶酸和CD44受体表达丰富的MCF-7细胞,评价PTX-HA-C18和PTX-FA-HA-C18胶束的细胞毒性和细胞摄取。结果:相比于市售制剂泰素(taxol),HA载药胶束在低浓度下表现出较强的细胞毒性,且PTX-FA-HA-C18胶束的细胞毒性显著强于PTX-HA-C18胶束。HA胶束能显著提高PTX在细胞中的摄取量,且细胞摄取呈现浓度-时间依赖性。相比于HA-C18胶束,FA-HA-C18胶束表现出更强的摄取能力。结论:HA胶束具有良好的肿瘤细胞靶向功能,FA-HA-C18双靶向胶束表现出最佳的靶向能力。
OBJECTIVE: To study the effect of folic acid and CD44 receptor on the targeting of hyaluronic acid-octadecyl (HA-C18), a single target of CD44 receptor, and the folic acid-hyaluronic acid-octadecyl (FA-HA- Tumor cell targeting function of paclitaxel (PTX) micelles. Methods: MCF-7 cells expressing folic acid and CD44 were selected to evaluate the cytotoxicity and cellular uptake of PTX-HA-C18 and PTX-FA-HA-C18 micelles. Results: HA loaded micelles displayed strong cytotoxicity at low concentrations compared with the commercially available formulation taxol, and the cytotoxicity of PTX-FA-HA-C18 micelles was significantly stronger than that of PTX-HA -C18 micelles. HA micelles can significantly increase the uptake of PTX in the cells, and the cellular uptake appears concentration-time dependent. FA-HA-C18 micelles showed more uptake capacity than HA-C18 micelles. Conclusion: HA micelles have good tumor cell targeting function, and FA-HA-C18 double-targeted micelles show the best targeting ability.