Miao Zhi-Lin, Deng Ying-Jie, DU Hong-Yang, Suo Xu-Bin, Wang Xiao-Yu, Wang Xiao, Wang Li, Cui Li-Jie, Duan Na
Heart Center, The People's Hospital of Liaoning Province, Shenyang, Liaoning 110016, P.R. China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P.R. China.
Exp Ther Med. 2015 Mar;9(3):941-946. doi: 10.3892/etm.2015.2201. Epub 2015 Jan 22.
The aim of this study was to prepare a liposomal delivery system for rapamycin and study its release characteristics. The results may provide a foundation for the further development of a liposomal delivery system for rapamycin and the establishment of a new active treatment method targeted towards the cellular components of atherosclerotic plaques. The ethanol injection method was used to prepare rapamycin-containing liposomes. The formulation was optimized by orthogonal design, and the degree of rapamycin release by the liposomes was measured by the reverse dialysis method. Orthogonal testing showed that the optimum formulation had a phospholipid concentration of 4%, a phospholipid-cholesterol mass ratio of 8:1, a drug-lipid mass ratio of 1:20 and an aqueous phase pH of 7.4. Rapamycin-containing liposomes with an encapsulation efficiency of 82.11±2.13% were prepared, and the release of rapamycin from the liposomes complied with a first-order kinetic equation. In conclusion, the formulation was optimized, the prepared liposomes had a high rapamycin encapsulation rate and good reproducibility, and their release had a certain delayed-release effect.
本研究的目的是制备雷帕霉素脂质体递送系统并研究其释放特性。研究结果可为雷帕霉素脂质体递送系统的进一步开发以及建立针对动脉粥样硬化斑块细胞成分的新型活性治疗方法奠定基础。采用乙醇注入法制备含雷帕霉素脂质体。通过正交设计对制剂进行优化，并用反向透析法测定脂质体对雷帕霉素的释放度。正交试验表明，最佳制剂的磷脂浓度为4%，磷脂与胆固醇质量比为8:1，药物与脂质质量比为1:20，水相pH值为7.4。制备了包封率为82.11±2.13%的含雷帕霉素脂质体，雷帕霉素从脂质体中的释放符合一级动力学方程。综上所述，优化了制剂，所制备的脂质体雷帕霉素包封率高、重现性好，其释放具有一定的缓释效果。
