湖南中医药大学学报2024，Vol.44Issue(1)：38-46,9.DOI:10.3969/j.issn.1674-070X.2024.01.006
栀子苷立方液晶凝胶的制备、表征及体外评价
Preparation,characterization,and in vitro evaluation of geniposide cubic liquid crystal gel
摘要
Abstract
Objective To prepare geniposide cubic liquid crystal gel(GE-CLC-G)and characterize and evaluate it in vitro,so as to enhance the transdermal performance of the water-soluble geniposide(GE).Methods Glyceryl monooleate(GMO)was used as the substrate material to prepare GE-CLC-G by injection method;the blank cubic crystal area was screened out by ternary phase diagram;the prescription and process conditions of GE-CLC-G were optimized by single factor method;the HPLC method for the determination of GE content was established.The product was characterized by polarizing microscope(PLM)and small angle X diffraction(SAXS).Modified Franz diffusion cell was used to compare the in vitro transdermal properties of GE-CLC-G and GE ointment,and DHR-2 rheometer was adopted to compare the rheological properties of GE-CLC-G and GE ointment.Results The optimal prescription and process of GE-CLC-G were as follows:GMO:anhydrous ethanol∶ water=64∶3∶33,1%GE dosage,1%penetration enhancer(azone∶ propylene glycol=1∶1),vortex at 60℃for 3 min,sealed and avoiding light in a constant temperature box at 25℃for 3 d.The obtained GE-CLC-G was colorless and clarified gel-like semi-solid;it was a cubic phase and its internal structure was a double diamond(Pn3m)lattice;the content of GE in the measured product was(9.94±0.02)mg/g,with a large drug load,which corresponded with the characteristics of cubic liquid crystal.The 24 h cumulative transdermal rate Q(%)and transdermal rate constant Js of GE-CLC-G containing 1%penetration enhancer were significantly higher than those of GE ointment and GE-CLC-G without penetration enhancer.Rheological studies showed that GE-CLC-G was a non-Newtonian fluid,with good bioadhesion and more stable structure.Conclusion The preparation process of GE-CLC-G is simple,the product appearance is fine;PLM and SAXS can be used to characterize cubic liquid crystal gel,and the content determination method is easy to operate,with good exclusiveness;the in vitro transdermal performance and rheological properties of GE-CLC-G are significantly better than GE ointment.关键词
立方液晶凝胶/栀子苷/三元相图/体外透皮/流变学Key words
cubic liquid crystal gel/geniposide/ternary phase diagram/in vitro transdermal penetration/rheology分类
医药卫生引用本文复制引用
欧阳威,黄星雨,王旭易,骆慧婷,李爽,谭颖,颜红..栀子苷立方液晶凝胶的制备、表征及体外评价[J].湖南中医药大学学报,2024,44(1):38-46,9.基金项目
湖南省自然科学基金面上项目(2022JJ30444) （2022JJ30444）
湖南省中医药科研计划项目(2021223) （2021223）
2022年湖南省研究生科研创新项目(CX20220791) （CX20220791）
湖南中医药大学重点学科中药学科(校行发规字[2023]2号). （校行发规字[2023]2号）
