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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[点击复制] |
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| 栀子苷立方液晶凝胶的制备、表征及体外评价 |
| 欧阳威,黄星雨,王旭易,骆慧婷,李爽,谭颖,颜红 |
| (湖南中医药大学, 湖南 长沙 410208;巩义市人民医院, 河南 郑州 451200) |
| 摘要: |
| 目的 为促进水溶性栀子苷的透皮性能而制备栀子苷立方液晶凝胶（geniposide cubic liquid crystal gel， GE-CLC-G），并对其进行表征及体外评价。方法 以甘油单油酸酯（glyceryl monooleate，GMO）为基质材料，采用注入法制备GE-CLC-G，通过三元相图筛选出空白立方液晶区域；采用单因素法优选GE-CLC-G的处方及工艺条件；建立栀子苷的HPLC含量测定方法；采用偏光显微镜（polarizing microscope，PLM）、小角X衍射仪（small angle X diffraction，SAXS）对产品进行表征；采用改良Franz扩散池，比较GE-CLC-G与栀子苷软膏的体外透皮特性；采用DHR-2流变仪，对比GE-CLC-G和栀子苷软膏的流变学性质。结果 优选的GE-CLC-G处方及工艺为GMO：无水乙醇：水=64：3：33，1%栀子苷投药量，1%促渗剂（氮酮：丙二醇=1：1），60℃涡旋3 min，25℃恒温箱密封、避光3 d。制得的GE-CLC-G为无色、澄明的凝胶状半固体；为立方相，其内部结构为双菱形（Pn3m）晶格；测得产品中栀子苷的含量为（9.94±0.02） mg/g，载药量较大，符合立方液晶的特点。含1%促渗剂的GE-CLC-G 24 h累积透皮率Q（%）和透皮速率常数Js明显高于不加促渗剂的栀子苷软膏和不加促渗剂的GE-CLC-G。流变学研究表明，GE-CLC-G属于非牛顿流体，生物黏附性好，结构更稳定。结论 GE-CLC-G制备工艺简单，产品外观良好，PLM和SAXS可用于表征立方液晶凝胶，含量测定方法操作简单，专属性好；GE-CLC-G的体外透皮性能和流变学性质均明显优于栀子苷软膏。 |
| 关键词: 立方液晶凝胶 栀子苷 三元相图 体外透皮 流变学 |
| DOI：10.3969/j.issn.1674-070X.2024.01.006 |
| 投稿时间：2023-07-09 |
| 基金项目:湖南省自然科学基金面上项目（2022JJ30444）；湖南省中医药科研计划项目（2021223）；2022年湖南省研究生科研创新项目（CX20220791）；湖南中医药大学重点学科中药学科（校行发规字﹝2023﹞2号）。 |
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| Preparation, characterization, and in vitro evaluation of geniposide cubic liquid crystal gel |
| OUYANG Wei,HUANG Xingyu,WANG Xuyi,LUO Huiting,LI Shuang,TAN Ying,YAN Hong |
| (Hunan University of Chinese Medicine, Changsha, Hunan 410208, China;Gongyi People's Hospital, Zhengzhou, Henan 451200, China) |
| 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. |
| Key words: cubic liquid crystal gel geniposide ternary phase diagram in vitro transdermal penetration rheology |
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