School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
Int J Pharm. 2012 Feb 28;423(2):480-8. doi: 10.1016/j.ijpharm.2011.12.004. Epub 2011 Dec 13.
α-Tocopherol succinate hydrophobically modified chitosan (CS-TOS) containing 17 α-tocopherol groups per 100 anhydroglucose units was synthesized by coupling reaction. The formation of CS-TOS was confirmed by (1)H NMR and FT-IR analysis. In aqueous medium, the polymer could self-aggregate to form micelles, and the critical micelle concentration (CMC) was determined to be 5.8 × 10(-3) mg/ml. Transmission electron microscopy (TEM) observation revealed that both bare and paclitaxel-loaded micelles were near spherical in shape. The mean particle size and zeta potential of drug-loaded micelles were about 78 nm and +25.7 mV, respectively. The results of DSC and XRD analysis indicated that paclitaxel was entrapped in the micelles in molecular or amorphous state. In vitro cytotoxicity and hemolysis study revealed the effectiveness and safety of this delivery system, which was further confirmed by the in vivo antitumor evaluations. It can be concluded that the CS-TOS was a potential micellar carrier for paclitaxel.
α-生育酚琥珀酸酯疏水改性壳聚糖（CS-TOS）每 100 个脱水葡萄糖单元含有 17 个α-生育酚基团，通过偶联反应合成。（1）H NMR 和 FT-IR 分析证实了 CS-TOS 的形成。在水介质中，该聚合物可以自组装形成胶束，临界胶束浓度（CMC）确定为 5.8×10（-3）mg/ml。透射电子显微镜（TEM）观察表明，裸和紫杉醇负载的胶束均呈近球形。载药胶束的平均粒径和 Zeta 电位分别约为 78nm 和+25.7mV。DSC 和 XRD 分析结果表明，紫杉醇以分子或无定形状态包封在胶束中。体外细胞毒性和溶血研究表明了该递药系统的有效性和安全性，体内抗肿瘤评价进一步证实了这一点。可以得出结论，CS-TOS 是紫杉醇的一种潜在的胶束载体。
