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目的：制备一种姜黄素共聚物胶束以提高姜黄素的水溶性及其抗肿瘤活性。方法：采用乳化溶剂挥发法制备了载姜黄素的共聚物胶束（Cur/PTL1 胶束），对其粒径、载药量、包封率和体外药物释放行为进行了考察；并采用MTT 法考察了PTL1 空白胶束和Cur/PTL1 胶束的体外细胞毒作用。结果：制备了粒径在40 nm左右的载姜黄素共聚物胶束，载药量为9.78± 0.29 %，包封率为 97.24± 2.68 %。体外药物释放实验表明，游离姜黄素在24 h内的药物累积释放率达到90 %以上，而Cur/PTL1 胶束在24 h内药物累积释放率为23.8 %，能够持续释放14 天，14 天内累积释放率为85.9 %，具有一定的缓释能力。MTT 实验结果表明，当PTL1 空白胶束浓度达到1 mg/mL时，细胞的存活率仍在90 %以上；Cur/PTL1 胶束组IC50 为4.73± 0.23 ug/mL，游离姜黄素组IC50 为 6.42± 0.35 ug/mL。结论：实验结果表明，Cur/PTL1 胶束可以作为一种有前景的纳米药物输送系统。

英文摘要:

Objective:To improve the water solubility and anti-tumor activity of curcumin by encapsulating curcumin into polymeric micelles.Methods:The Cur-loaded polymeric micelles (Cur/PTL1 micelles) were prepared by the emulsion solvent evaporation method, and then the characteristics of the Cur-loaded micelles (e.g., size, drug loading content, encapsulation efficiency and in vitro drug release behavior) were investigated. In vitro cytotoxicity of the blank PTL1 micelles and Cur-loaded PTL1 micelles was investigated by a standard MTT assay.Results:The hydrodynamic diameter of the prepared Cur-loaded micelles was about 40 nm, the drug loading was 9.78± 0.29 % and the encapsulation efficiency was 97.24± 2.68 %. The cumulative release rate of free curcumin was above 90 % within 24 h; while the Cur-loaded PTL1 micelles presented a sustained drug release profile, the cumulative release rates were 23.8 % within 24 h and 85.9 % in the 14 days. Cell viabilities were all >90 % after incubating with the blank PTL1 micelles, even at very high micelle concentration (up to 1 mg/mL). The IC50 values of free Cur and Cur/PTL1 micelles against B16F10 were 6.42± 0.35 ug/mL and 4.73± 0.23 ug/mL, respectively.Conclusion:Cur/PTL1 micelles may be a potential nanoscale drug delivery system.

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