羧甲基壳聚糖基胶束的制备及其缓释性

Preparation and Sustained Release of Carboxymethyl Chitosan Derived Micelles

以羧甲基壳聚糖接枝聚己内酯(CMCS-g-PCL)作为阿帕替尼的载体,制备了载药胶束以降低阿帕替尼的副作用。通过紫外-可见分光光度法,分别研究了采用乳化-挥发法、透析法以及薄膜水化法所制得载药胶束的包封率及载药量,并对胶束的稳定性、缓释性以及细胞毒性进行了研究。研究表明:乳化-挥发法最适合用于制备载药胶束,制得的胶束平均粒径在100~150nm,在水溶液中能够稳定维持21d以上,而在PBS溶液中仅能维持7d左右。该载药胶束具有良好的缓释效果,且释放率随着载体接枝率的上升而下降。细胞增殖抑制实验证明,载药胶束对人脐静脉内皮细胞(HUVECs)的抑制效果随着培养时间的推移逐渐增大,有利于实现长效治疗。

Carboxymethyl chitosan-gra ft-polycaprolactone(CMCS-g-PCL)was selected as the carrier of Apatinib and drug-loaded micelles were prepared to reduce Apatinib’s side effects.Emulsion-evaporation method,dialysis method and film hydration method were used to prepare drug-loaded micelles and UV-Vis spectrophotometry was used to test drug loading contents and encapsulation efficiency of micelles.Then the stability,release and cytotoxicity of micelles were studied.Research showed that emulsion-evaporation method was the best method for preparing drug-loaded micelles and the particle sizes of the prepared micelles were approximately 100~150 nm.The micelles could be stable for more than 21 d in aqueous solution while maintained 7 d in PBS solution.The micelles had a good sustained-release effect and the release rate decreased with the increase of grafting ratio of carrier.Cell proliferation inhibition test showed that the inhibitory effect of drug-loaded micelles on human umbilical vein endothelial cells(HUVECs)gradually increased with the increase of culture time,which was beneficial to long-term treatment.