乙二胺四乙酸铵梯度法制备盐酸伊立替康脂质体

Preparation of irinotecan hydrochloride liposomes by ammonium ethylenediaminetetraacetate gradient method

目的制备盐酸伊立替康脂质体,考察包封率及粒径的影响因素。方法采用乙二胺四乙酸铵梯度法制备盐酸伊立替康脂质体,以阳离子交换树脂分离脂质体和游离药物,并以紫外分光光度法和激光粒度仪分别测定盐酸伊立替康脂质体的包封率和粒径;考察不同处方和制备工艺对脂质体包封率及粒径的影响。结果通过处方工艺优化,盐酸伊立替康脂质体包封率达到95.73%,粒径为112.8 nm。结论以乙二胺四乙酸铵梯度法制备的盐酸伊立替康脂质体包封率较高,方法可行。

Objective To prepare irinotecan hydrochloride （CPT-11 ）liposomes, and study the influence of factors on the entrapment efficiency and size. Methods CPT-11 was encapsulated in the liposomes by ammonium ethylenediaminetetraacetate（NH4EDTA） gradient method. Free CPT-11 and liposomes were separated by cation exchange resin. Ultraviolet spectrophotometry and laser particle analyzer were applied to determine the entrapment efficiency and the size of CPT-11 liposomes, respectively. The influence of various factors on the entrapment efficiency and size of CPT-11 liposomes were investigated. Results Through optimizing the formulations and preparation conditions, the CPT-11 liposomes were with high entrapment efficiency to 95.73% and the mean diameter to 112. 8 nm. Conclusions The CPT-11 liposomes with high entrapment efficiency can be prepared by NH4EDTA gradient method, and the method is proved to be feasible.