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脂质体是可静脉注射的靶向、控释给药系统。本研究的主要目的是制备洛莫司汀脂质体,评价其物理化学性质,并对其静脉注射后的组织靶向性进行研究。用薄膜分散法制备洛莫司汀脂质体,37℃磷酸盐缓冲溶液(pH=6.8)中考察体外释放特性,反相高效液相色谱法测定静脉注射洛莫司汀HP-β-CD包合物溶液和脂质体后组织中的药物浓度。该实验制备的洛莫司汀脂质体平均粒径为(189.8±28.5)nm,zeta电位(-19.13±0.12)mV。释放曲线符合Weibull方程。以新西兰兔为试验动物,分别静脉注射洛莫司汀溶液和脂质体,脂质体组的消除半衰期(t_(1/2β)显著增加。洛莫司汀脂质体在小鼠脑组织中的AUC、Te和Re明显提高。实验结果表明该脂质体对脑部有被动靶向效果。
Liposomes are intravenous, targeted, controlled release drug delivery systems. The main purpose of this study was to prepare lomustine liposomes, to evaluate its physicochemical properties, and to study its tissue targeting after intravenous injection. The lomustine liposomes were prepared by thin-film dispersion method and the in vitro release characteristics were examined in phosphate buffered solution (pH = 6.8) at 37 ℃. The injection of lomustine HP-β-CD was determined by reversed-phase high performance liquid chromatography The drug concentration in the compound solution and in the tissue behind the liposomes. The average particle size of the lomustine liposome prepared in this experiment was (189.8 ± 28.5) nm, zeta potential (-19.13 ± 0.12) mV. The release curve follows the Weibull equation. Using New Zealand rabbit as experimental animal, the elimination half-life (t_ (1 / 2β)) of lomustine solution and liposome were significantly increased, respectively. Lomustine liposomes in mouse brain tissue Of AUC, Te and Re significantly increased.The experimental results show that the liposome has a passive targeting effect on the brain.