白藜芦醇三甲醚脂质体的制备及其质量评价

Preparation of resveratrol trimethyl ether liposomes and their quality evaluation

目的制备白藜芦醇三甲醚(BTM)脂质体,对其质量特性进行评价,并考察脂质体对BTM的增溶作用。方法采用薄膜分散法制备BTM脂质体,以包封率为评价指标,通过正交试验设计优化处方工艺,微柱离心法测定其包封率,观察其形态、粒径及稳定性,并考察其对BTM的增溶作用。结果优化的最佳处方工艺为BTM与卵磷脂质量比为1∶20,胆固醇与卵磷脂质量比为1∶4,水化介质为5%甘露醇;按该处方制备的BTM脂质体包封率达(86.4±2.2)%;与游离BTM相比,BTM脂质体在水中的溶解度增大了1 012倍。结论采用最佳处方制备得到的BTM脂质体包封率较高,形态和粒径较均匀,并且可以较好地提高BTM的溶解度。

Objective To prepare resveratrol trimethyl ether （3, 5, 4＇-trimethoxy-trans-stilbene, BTM） liposomes, evaluate their quality, and observe the solubilization of BTM. Methods The film dispersion method was used to prepare BTM liposomes. Orthogonal test design was used to optimize the formula by taking encapsulation efficiency （EE） as index. The EE was determined by the microcolumn centrifugation method. The properties of liposomes including morphology, mean diameter, stability, and solubilization of BTM were studied. Results The best prescription was BTM-phospholipid （1 ： 20）, Cholesterol-phospholipid （1：4）, and 5% mannitol as hydration medium. The EE of the prepared BTM liposomes was （86.4±2.2）%, and the solubility of BTM was increased by 1 012 times compared with free BTM. Conclusion The BTM liposomes prepared according to the optimized formula have the higher EE and the uniform morphology and diameter. Liposomes could improve the solubility of BTM.