李敏 郭爱洁 张骁 汪芸 沈园园△.姜黄素共聚物胶束的制备与体外细胞毒评价[J].现代生物医学进展英文版,2016,16(3):427-430. |
姜黄素共聚物胶束的制备与体外细胞毒评价 |
Preparation and in vitro Cytotoxicity of Curcumin-loaded Polymeric Micelles |
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DOI: |
中文关键词: 姜黄素 共聚物胶束 细胞毒作用 |
英文关键词: Curcumin Polymeric micelles Cytotoxicity |
基金项目:上海交大医工结合基金项目(YG2012MS36) |
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中文摘要: |
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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