title: Preparation of a liposomal delivery system and itsin vitrorelease of rapamycin.
abstract: The aim of this study was to prepare a liposomal delivery system for rapamycin and study itsin vitrorelease 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 thein vitrorelease 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 theirin vitrorelease had a certain delayed-release effect.
authors: Heart Center, The People's Hospital of Liaoning Province, Shenyang, Liaoning 110016, P.R. China.
authors: Zhi-Lin
authors: ZL
authors: Miao
authors: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P.R. China.
authors: Ying-Jie
authors: YJ
authors: Deng
authors: Dalian Medical University Graduate School, Dalian, Liaoning 116044, P.R. China.
authors: Hong-Yang
authors: HY
authors: DU
authors: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P.R. China.
authors: Xu-Bin
authors: XB
authors: Suo
authors: School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, P.R. China.
authors: Xiao-Yu
authors: XY
authors: Wang
authors: Dalian Medical University Graduate School, Dalian, Liaoning 116044, P.R. China.
authors: Xiao
authors: X
authors: Wang
authors: Heart Center, The People's Hospital of Liaoning Province, Shenyang, Liaoning 110016, P.R. China.
authors: Li
authors: L
authors: Wang
authors: Heart Center, The People's Hospital of Liaoning Province, Shenyang, Liaoning 110016, P.R. China.
authors: Li-Jie
authors: LJ
authors: Cui
authors: Heart Center, The People's Hospital of Liaoning Province, Shenyang, Liaoning 110016, P.R. China.
authors: Na
authors: N
authors: Duan
keywords: atherosclerosis; in vitro release kinetics; liposomes; orthogonal design; rapamycin; reverse dialysis; targeted therapy