乳糖化-去甲斑蝥素磷脂复合物及其pH敏感型脂质体的制备

摘要

Objective: To prepare lactosyl-norcantharitin (Lac-NCTD) phospholipid complex and its pH-sensitive liposomes. Methods: Lac-NCTD phospholipid complex was prepared using solvent-evaporation, and its correlated physicochemical properties were confirmed with solubility test, FT-IR, DSC and 1H-NMR. The phospholipid complex liposomes were prepared by the reverse phase evaporation method, and then pH-sensitive liposomes of Lac-NCTD phospholipid complex were obtained with the carboxymethyl chitosan ( CMCT) absorbed on the surface of the liposomes. The drug loading rate, encapsulation efficiency, particle distribution and in vitro release of Lac-NCTD from liposomes were investigated, respectively. Results: The drug loading rate of phospholipid complex was (97. 2 ±2. 01 )% , the average entrapment rate of liposome was (70. 00 ± 1. 30) % . The mean particle size was (47.18 ±4.16) nm, particle span was (0.70 ±0.07) , and in vitro release was followed Weibull equation. Conclusion: Alternative pH-sensitive liposomes of Lac-NCTD phospholipid complex with high drug loading rate and sustained release have been obtained.%目的:合成乳糖化-去甲斑蝥素磷脂复合物,并制备其pH敏感型脂质体.方法:将乳糖化-去甲斑蝥素与磷脂聚合成药物磷脂复合物,并采用FT-IR、DSC和(1)H-NMR对其进行表征.逆向蒸发法制备药物磷脂复合物脂质体;利用羧甲基壳聚糖与脂质体表面的静电吸附作用,使羧甲基壳聚糖吸附在脂质体表面,制备乳糖化-去甲斑蝥素磷脂复合物pH敏感型脂质体;考察了药物与磷脂的复合率,磷脂复合物脂质体的包封率,粒径大小和分布,以及体外释药特性.结果:药物磷脂复合率为(97.2±2.01)%,磷脂复合物脂质体的平均包封率为(70.00±1.30)%,平均粒径为(47.18±4.16)nm,粒径跨距为(0.70±0.07),电镜显示其形态圆整,体外释药符合Weibull方程.结论:乳糖化-去甲斑蝥素磷脂复合率高,制成的pH敏感型脂质体性质稳定,且具有缓释特性.