包载紫杉醇的透明质酸聚合物胶束细胞毒性及细胞摄取研究

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。

Study on Cytotoxicity and Cellular Uptake of Paclitaxel-loaded Hyaluronic Acid Polymeric Micelles

Objective: To study the cytotxicity and cellular uptake of CD44 receptor targeting paclitaxel-hyaluronic acid-octadecyl (PTX-HA-C₁₈) and folate and CD44 receptors dual targeting PTX-folate-HA-C₁₈ (PTX-FA-HA-C₁₈) micelles. Method: Cytotoxicity and cellular uptake in vitro of Taxol and PTX-loaded micelles were performed using folate and CD44 receptors over expressing MCF-7 cell. Result: PTX-loaded HA micelles exhibited higher cytotoxicity compared with Taxol at lower PTX concentration. The cellular inhibition of FA-HA-C₁₈ micelle was more obvious than that by HA-C₁₈ micelle. HA micelles possessed high cellular uptake capacity, and the cellular uptake was concentration and time-dependent. FA-HA-C₁₈ micelles exhibited higher cellular uptake compared with HA-C₁₈ micelles. Conclusion: HA micelles has good tumor targeting ability, and FA-HA-C₁₈ micelle exhibits excellent tumor targeting efficiency.