性质可比自微乳处方的制备、筛选及其对白藜芦醇增溶能力的研究

目的 通过制备一系列不同油相组成的自微乳处方,从中筛选出能形成相近粒径、表面电荷和均一性微乳的可比处方,进一步考察其对白藜芦醇的增溶能力.方法 分别以中链脂肪酸甘油酯、长链脂肪酸甘油酯和非甘油三脂肪酸酯为油相,通过伪三元相图法确定微乳区,并利用纳米粒度电位分析仪测定所得微乳的粒径、多分散性和Zeta电位,从中筛选出性质可比自微乳处方;通过HPLC测定自微乳及稀释后微乳对白藜芦醇的增溶能力.结果 通过筛选,选择了4种自微乳处方,其中油相为MCT(60%)或蓖麻油(40%)的微乳处方,粒径为140 nm左右;油相为MCT(40%)或油酸乙酯(40%)的微乳处方,粒径为60 nm左右.所得自微乳处方对白藜芦醇的增溶能力达到其水溶解度的8000倍左右.结论 本研究获得了一系列具有可比性的自微乳处方:当组分相同时,所得微乳粒径及分散性差别较大;当组分不同时,所得微乳粒径及分散性相近,可以用于考察微乳性质对药物生物利用度的影响.

Preparation and selection of comparable self-microemulsifying drug delivery systems (SMEDDS) and their solubilizing capabilities on resveratrol

Objective To prepare and select comparable self-microemulsifying drug delivery system (SMEDDS) formulations with similar particle sizes,zeta potentials and polydispersity indexes and to detect their solubilizing capabilities on resveratrol.Methods We prepared a series of SMEDDS formulations composed of medium-chain triglycerides, long-chain triglycerides and non-triglycerides.Their particle sizes, polydispersity indexes and zeta potentials were studied by Zetasizer Nano ZS90, and selected the comparable SMEDDS formulations.The solubilizing capability of the selected SMEDDS formulations on resveratrol was detected by HPLC.Results The formulations containing 60% MCT or 40% castor oil as oil phase could form microemulsions of diameter 140 nm;while the formulations containing 40% MCT or 40% ethyl oleate could form microemulsions of diameter 60 nm.The solubilities of resveratrol in the four SMEDDS formulation were about 8000-fold of that in water.Conclusion If the compositions of SMEDDS were the same, the particle sizes and polydispersity indexes varied significantly, while if the composition of SMEDDS were different, the particle sizes and polydispersity indexes were similar.The obtained SMEDDS formulation could be applied to study the effect of SMEDDS properties on the drug bioavailability.