溴新斯的明多囊脂质体的制备及其体外释放行为的初步研究

Preliminary study on preparation and in vitro release of neostigmine bromide multivesicular liposomes

目的:制备溴新斯的明多囊脂质体(NB-MVL),并对其体外药物释放行为进行考察。方法:采用复乳法制备载药多囊脂质体,并用单因素试验优化处方,以动态透析技术与f2相似因子评价法对NB-MVL与溴新斯的明在体外不同释放介质中的释放行为进行研究,计算其药物释放度与相似因子。结果:NB-MVL的包封率受投料比、药物浓度等因素影响;NB-MVL在不同的释放介质中所获得的释放模型均符合Weibull模型,同时与溴新斯的明溶液在不同释放介质中所得累积释放曲线间的相似因子小于50。结论:本试验制备所得NB-MVL包封率较高,且体外药物释放行为与溴新斯的明存在显著性差异,表现出良好的缓释作用。

OBJECTIVE To prepare neostigmine bromide multivesicular liposomes（NB-MVL）and study on release of NBMVL in different media in vitro.METHODS NB-MVL was prepared by multiple emulsion method.Single factor test was used to investigate and optimize encapsulation efficiency.Kinetics model and similarity factor（f2 value）were used to compare in vitro release characteristics of NB-MVL and NB in different media,and cumulative release profile and similarity factors were calculated.RESULTS Encapsulation efficiency of NB-MVL was obviously affected by contents of NB and phospholipids/Cholesterol.The in vitro release characteristics of NB-MVL in different release media fitted with Weibull model,while similarity factors among release curve of different media were less than 50.CONCLUSION NB-MVL shows high encapsulation efficiency.The in vitro drug release of NB-MVL here is significantly different from that of NB.NB-MVL shows good sustained release.