雷公藤甲素立方液晶的制备及体外评价

Preparation and in Vitro Evaluation of Triptolide-Loaded Cubic Liquid Crystals

目的研制雷公藤甲素立方液晶,并对其进行表征,考察其流变学特性及体外透皮特性。方法采用植烷三醇-卡必醇-水3组分体系制备立方液晶(cubic liquid crystal,V2),利用三元相图法优选出目标区域,以体外释药行为作为考察指标优选最佳处方;采用小角度X射线散射(SAXS)、红外光谱分析(IR)及差式扫描量热技术(DSC)对其结构进行表征;并对其流变学性质进行研究;采用改良的Franz扩散池对雷公藤甲素立方液晶及雷公藤甲素凝胶体外释药行为进行比较研究。结果优选出最优处方为植烷三醇-卡必醇-水(54∶6∶40,W/W/W),载药量为0. 1 mg·g^-1,SAXS显示,为双菱形晶格立方液晶;流变学参数良好;DSC结果显示,雷公藤甲素立方液晶在65. 5℃时可转变成六角相,90℃则转变成层状液晶,且药物的加入不会改变液晶结构。雷公藤甲素立方液晶的体外透皮累积渗透量约为凝胶的1. 54倍,且可缓释雷公藤甲素长达48 h。结论本实验制备的雷公藤甲素立方液晶外观良好、流变性适宜,体外透皮累积渗透量及渗透速率均优于雷公藤甲素凝胶,可为雷公藤甲素经皮给药新剂型提供实验依据。

OBJECTIVE To prepare and characterize triptolide cubic liquidcrystal,study the rheological properties and in vitro transdermal properties. METHODS Cubic liquid crystal (V2) was prepared by using phytantriol-carbitol-water three-component system. Using the ternary phase diagram method to optimize the target area. V2 was characterized by small-angle X-ray scattering, infrared spectroscopy and differential scanning calorimetry. Rheological properties of V2 was studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using improved Franz diffusion cell method. RESULTS SAXS is shown as double-diamond lattice cubic liquid crystal;rheological parameters are good;DSC results show V2 can be converted into a hexagonal phase at 65.5 ℃ and converted into a layered liquid crystal at 90 ℃, and the addition of the drug does not change the liquid crystal structure. In vitro transdermal cumulative permeation amount is about 1.54 times that of the gel, and the sustained release of triptolide can be as long as 48 h. CONCLUSION The prepared triptolide liquid crystal has good appearance and suitable rheology, and its cumulative permeation amount and infiltration rate of V2 are superior to the hydrophilic gel, which provides theoretical reference for triptolide percutaneous administration.