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为了确保将抗肿瘤药物递送到肿瘤部位并在肿瘤细胞内快速释药,本研究设计并制备了包载紫杉醇(PTX)的聚(2-乙基-2-噁唑啉)-维生素E琥珀酸酯(PEOz-VES)p H敏感聚合物胶束。用1H NMR确证了所合成的PEOz-VES的结构,用GPC测定其分子量为1212 g/mol,酸碱滴定法测定其p Ka为6.01,芘荧光探针法测定其临界胶束浓度为(5.84±0.02)mg/L。采用薄膜水化法制备包载PTX的PEOz-VES胶束,载药量和包封率分别为(2.63±0.16)%和(84.1±3.38)%。动态光散射法测得胶束的粒径约为30 nm,Zeta电势为4.86 m V。TEM显示胶束呈均匀的球形。体外释放结果表明,PEOz-VES胶束具有p H依赖性释放行为,随着p H降低胶束的释放逐渐加快。因此该胶束可以识别正常组织和肿瘤组织间的p H差异并能响应胞内的p H梯度,预示该胶束具有肿瘤靶向性和胞内快速释药的特征,是一种较有潜力的抗肿瘤药物递送载体。
In order to ensure that the antitumor drug is delivered to the tumor site and released rapidly in the tumor cells, the present study designed and prepared paclitaxel (PTX) -containing poly (2-ethyl-2-oxazoline) -vitamin E succinate Ester (PEOz-VES) p H Sensitive Polymer Micelles. The structure of the synthesized PEOz-VES was confirmed by1H NMR. The molecular weight of the synthesized PEOz-VES was 1212 g / mol by GPC. The pKa was 6.01 as determined by acid-base titration. The critical micelle concentration was 5.84 ± 0.02) mg / L. The PEOz-VES micelles coated with PTX were prepared by the membrane hydration method. The drug loading and encapsulation efficiency were (2.63 ± 0.16)% and (84.1 ± 3.38)%, respectively. The particle size of micelles was about 30 nm and the Zeta potential was 4.86 mV by dynamic light scattering. TEM shows that the micelles are uniformly spherical. The results of in vitro release showed that the release of PEOz-VES micelles was p H-dependent, and the release of micelles accelerated with the decrease of p H. Therefore, the micelles can recognize the p H difference between normal tissues and tumor tissues and respond to the intracellular p H gradient, which indicates that the micelles are more potential for tumor targeting and rapid intracellular release Antitumor drug delivery vehicle.