洛莫司汀-碘海醇复方脂质体的制备及包封率测定

Preparation of Lomustine-iohexol Compound Liposomes and Determination of the Entrapment Efficiency

目的:制备洛莫司汀-碘海醇复方脂质体,并考察其质量、测定其包封率。方法:以逆相蒸发法制备复方脂质体;以磷脂种类(A)、磷脂与胆固醇质量比(B)、脂质质量浓度(C)为因素,以两主药的包封率为评价指标,采用正交设计法优化处方;以两主药的包封率及脂质体的粒径和Zeta电位为指标进行验证试验。结果:优化处方结果显示,A为大豆磷脂80,B为2∶1,C为33mg/ml。验证试验结果显示,洛莫司汀包封率约为75.7%,碘海醇包封率约为65.7%;脂质体粒径约为236.5 nm,Zeta电位约为-42.2mV。结论:采用该处方与工艺可成功制备包封率较高的洛莫司汀-碘海醇复方脂质体,质量符合要求。

OBJECTIVE： To prepare Lomustine-iohexol compound liposomes, and to evaluate the properties and determine the entrapment efficiency. METHODS： Compound liposomes were prepared by reverse evaporation method; orthogonal design was used to optimize the formulation with the types of phospholipid （A）, the proportion of phospholipid to cholesterol （B） and the con- tent of lipid （C） as factors using the entrapment efficiency of two main components as index. The entrapment efficiency of two main components, particle size and Zeta-potential of Compound lipidsomes were determined to validate the formulation. RE- SULTS ： The optimal formulation was as follows ： A was soybean phospholipid 80 ; B was 2 ： 1 ; C was 33 mg/ml. The entrapment efficiency of lomustine was 75.7% and that of iohexol was 65.7%; the particle size of compound liposomes was 236.5 nm, and Ze- ta potentials of them were --42.2 inV. CONCLUSIONS： The formulation and preparation technology can be used to prepare Lomus- tine-iohexol compound liposomes with high entrapment efficiency successfully, and the quality of them is up to the standard.