Wang Wen-Xi, Feng Shi-Sen, Zheng Cai-Hong
School of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China.
Women's Hospital School of Medicine Zhejiang University, Hangzhou 310006, China.
Int J Pharm. 2016 Nov 20;513(1-2):387-392. doi: 10.1016/j.ijpharm.2016.09.043. Epub 2016 Sep 15.
A drug-cyclodextrin complex in liposome system was prepared in order to make a comparison with conventional risperidone-loaded liposome. Thin film hydration, reverse phase evaporation and ethanol injection methods were taken as preparation means to obtain the two types of liposome. Differential thermal analysis (DTA) and transmission electron microscopy (TEM) were used to investigate the thermal characters of inclusion complexes and morphology of liposome, respectively. Particle size, zeta potential and encapsulation efficiency were studied by light scattering analysis and ultrafiltration. In vitro release was carried out in the pH 7.4 phosphate buffer solution and samples were collected at the certain time. As a result, drug-cyclodextrin complex in liposome prepared by various methods displayed lower encapsulation efficiency than conventional liposome. However, size was larger and its stability was better than the latter. The second release phase of novel delivery system was slightly slower after initial burst release at the first phase, while the conventional liposome displayed a more regular trait. Thus, the novel liposome have potential to be developed as co-administration formulation with long-acting injection.
制备了脂质体系统中的药物 - 环糊精复合物,以便与传统的载利培酮脂质体进行比较。采用薄膜水化法、逆相蒸发法和乙醇注入法作为制备手段来获得这两种类型的脂质体。分别使用差示热分析(DTA)和透射电子显微镜(TEM)来研究包合物的热性质和脂质体的形态。通过光散射分析和超滤研究粒径、zeta电位和包封率。在pH 7.4的磷酸盐缓冲溶液中进行体外释放,并在特定时间收集样品。结果,通过各种方法制备的脂质体中的药物 - 环糊精复合物显示出比传统脂质体更低 的包封率。然而,其粒径更大,稳定性比后者更好。新型给药系统在第一阶段初始突释后第二释放阶段稍慢,而传统脂质体表现出更规则的特征。因此,新型脂质体有潜力被开发为长效注射的联合给药制剂。