Hu Fu-Qiang, Jiang Xiao-Hong, Huang Xuan, Wu Xiu-Ling, Yuan Hong, Wei Xiao-Hong, Du Yong-Zhong
College of Pharmaceutical Science, Zhejiang University, Hangzhou, People's Republic of China.
J Drug Target. 2009 Jun;17(5):384-91. doi: 10.1080/10611860902894325.
Chlorines are attractive compounds for photodynamic therapy because of their high absorption in the red wavelength region. The stearic acid-grafted chitosan oligosaccharide (CSO-SA) micelles have been presented as potential candidates for intracellular drug delivery carrier because of their special structure. In this study, CSO-SA micelles were prepared to encapsulate chlorine e6 (Ce6). The physicochemical properties of synthesized CSO-SA micelles were characterized. The critical micelle concentration (CMC) of CSO-SA with 4.96% amino substituted degree (SD %) was about 36.27 +/- 1.51 microg/mL. The Ce6-loaded CSO-SA micelles were then prepared by a dialysis method, and the properties and drug release profiles of Ce6- loaded CSO-SA micelles (CSO-SA/Ce6) were investigated. The loading of Ce6 in the CSO-SA micelles could reach higher drug encapsulation efficiency (%), which was approximately 100%. The size of CSO-SA/Ce6 decreased after the loading of Ce6. The zeta potential of CSO-SA/Ce6 and the drug release rate decreased with the loading content of drug. After the Ce6 molecules were encapsulated into the micelles of CSO-SA, the cellular uptake percentage of Ce6 was much more than that of the free drug. And the cellular uptake percentage of CSO-SA/Ce6 micelles was increased with the incubation time in a short period.
由于氯在红色波长区域具有高吸收性，所以它们是光动力疗法中颇具吸引力的化合物。硬脂酸接枝的壳寡糖（CSO-SA）胶束因其特殊结构而被视为细胞内药物递送载体的潜在候选物。在本研究中，制备了CSO-SA胶束以包封氯e6（Ce6）。对合成的CSO-SA胶束的物理化学性质进行了表征。氨基取代度（SD%）为4.96%的CSO-SA的临界胶束浓度（CMC）约为36.27±1.51μg/mL。然后通过透析法制备负载Ce6的CSO-SA胶束，并研究了负载Ce6的CSO-SA胶束（CSO-SA/Ce6）的性质和药物释放曲线。Ce在CSO-SA胶束中的负载可以达到更高的药物包封效率（%），约为100%。负载Ce6后，CSO-SA/Ce6的粒径减小。CSO-SA/Ce6的zeta电位和药物释放速率随药物负载量的增加而降低。将Ce6分子包封到CSO-SA胶束中后，Ce6的细胞摄取率远高于游离药物。并且在短时间内，CSO-SA/Ce6胶束的细胞摄取率随孵育时间的增加而升高。
