利用环糊精的衍生物6-CHO-β-CD和十八胺发生席夫碱反应形成具备pH敏感性聚合物6-β-环糊精十八烷基亚胺（6-β-CD-N-（CH₂）₁₇-CH₃），以透析法制备紫杉醇（PTX）载药胶束。采用荧光探针技术测定其临界胶束浓度（CMC）；测定了紫杉醇载药胶束的粒径、形态、包封率和载药量；利用紫外分光光度法考察载药胶束在不同pH条件下的释放情况。结果表明，胶束材料的临界胶束浓度CMC为3.98×10^-2 g/L；载药胶束的包封率为（34.3±1.0）%，载药量为（1.97±0.3）%，平均粒径为261.6 nm，且形状为棒状结构。在酸性（pH 5.0）条件下药物的释放量明显高于生理环境（pH 7.4）介质中药物的释放量，且在72 h后有突释现象，可以实现在酸性条件下靶向治疗癌细胞的效果。聚合物6-β-CD-N-（CH₂）₁₇-CH₃自组装形成的棒状胶束具有一定的pH敏感特性。

Paclitaxel-loading micelles are prepared via dialysis method using a pH-sensitive imine bond polymer 6-β-CD-N-(CH₂)₁₇-CH₃ that is synthesized by Schiff base reaction between 6-CHO-β-CD and octadecylamine.The critical micelle concentration (CMC) of the polymer is measured by means of Pyrene fluorescent probe technique.The particle size,morphology,encapsulation efficiency and drug loading amount are determined.The release of drug-loading micelles at different pH values is investigated by UV spectrophotometry.It is indicated that CMC,entrapment efficiency and drug-loading amount of the micelles are 3.98×10^-2 g·L^-1,34.3±1.0% and 1.97±0.3%,respectively.Paclitaxel-loading micelle is rod-like with an average particle size of 261.6 nm.The release rates of paclitaxel under acidic condition (pH=5.0) are significantly higher than in the physiological medium (pH=7.4) and there is a burst after 72 h,which can achieve the curable effect of targeting cancer cells under acidic conditions.The rod-like micelles formed by self-assembly of 6-β-CD-N-(CH₂)₁₇-CH₃ have certain pH-sensitive properties.

姜伟伟(1991-),女,硕士研究生,主要研究方向为药用高分子材料,1184839913@qq.com