中国中药杂志

2022, v.47(10) 2634-2642

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淫羊藿富集部位微乳凝胶的制备及药效学评价
Preparation of microemulsion gel loading enriched ingredients of Epimedii Folium and its pharmacodynamics evaluation

刘玉娟;刘欣妍;李婷婷;李鑫;梅凯;王昕怡;王灵敏;吴清;
LIU Yu-juan;LIU Xin-yan;LI Ting-ting;LI Xin;MEI Kai;WANG Xin-yi;WANG Ling-min;WU Qing;Beijing University of Chinese Medicine;

摘要(Abstract):

该研究拟在淫羊藿富集部位微乳的前期研究基础上,制备淫羊藿富集部位微乳凝胶剂,进行质量评价并考察其对化疗药损伤周围神经系统的保护作用。该实验从流变学、制备难易程度及载药量角度,对凝胶的制备方法、基质的种类及用量进行筛选,确定最优处方并制备淫羊藿富集部位微乳凝胶;以朝藿定A1、A、B、C及淫羊藿苷为评价指标,采用Franz扩散池法对凝胶剂的体外释放及体外透皮行为进行研究;采用Wistar大鼠建立奥沙利铂诱导的周围神经毒性模型(oxaliplatin-induced peripheral neuropathy, OIPN),通过给药后的行为学测定和背根神经节、坐骨神经的组织病理学检测,评价淫羊藿富集部位微乳凝胶对化疗药物损伤周围神经的保护作用。淫羊藿富集部位微乳凝胶剂制备工艺稳定,5种成分的释放最符合Hixson-crowell动力学模型;行为学指标直观地显示了药物可以有效地缓解奥沙利铂引起的机械异常性疼痛,进一步的组织病理学研究发现,药物可以改善奥沙利铂引起的背根神经节神经元损伤、轴突变性和脱髓鞘现象。因此,淫羊藿富集部位微乳凝胶制备工艺可行,释药稳定,对化疗所致周围神经病变(chemotherapy-induced peripheral neuropathy, CIPN)具有一定的治疗作用。
On the basis of previous studies, this study prepared and evaluated microemulsion gel loading enriched ingredients of Epimedii Folium and investigated its protective effect against peripheral nervous system damage caused by chemotherapeutics. The preparation method and the type and dosage of the matrix were investigated from rheology, preparation difficulty, and drug loading. Then the optimal prescription was determined and the microemulsion gel loading enriched ingredients of Epimedii Folium was prepared. The in vitro release and transdermal behaviors of the gel were investigated in the Franz diffusion cell with epimedin A1,A,B,C, and icariin as evaluation indicators. The oxaliplatin-induced peripheral neuropathy(OIPN) model was established in Wistar rats. The protective effect of the microemulsion gel loading enriched ingredients of Epimedii Folium against peripheral nervous system damage caused by chemotherapeutics was evaluated by behavioral measurement after drug administration and histopathological examination of dorsal root ganglia and sciatic nerve. The preparation process of the microemulsion gel loading enriched ingredients of Epimedii Folium was stable, and the release of the five components was consistent with the Hixson-Crowell cube root law. Behavioral indicators intuitively showed that the drug could effectively relieve mechanical allodynia caused by oxaliplatin. The histopathological examination showed that the drug can improve neuron damage in the dorsal root ganglia, axon degeneration, and demyelination caused by oxaliplatin. Therefore, the preparation process of the microemulsion gel loading enriched ingredients of Epimedii Folium is feasible, which can achieve stable drug release. It has a certain therapeutic effect on chemotherapy-induced peripheral neuropathy(CIPN).

关键词(KeyWords): 淫羊藿富集部位;微乳凝胶剂;体外释放;体外透皮;化疗所致周围神经病变
enriched ingredients of Epimedii Folium;microemulsion gel;release in vitro;transdermal behavior in vitro;chemotherapy-induced peripheral neuropathy

Abstract:

Keywords:

基金项目(Foundation): 北京市自然科学基金项目(7192109)

作者(Authors): 刘玉娟;刘欣妍;李婷婷;李鑫;梅凯;王昕怡;王灵敏;吴清;
LIU Yu-juan;LIU Xin-yan;LI Ting-ting;LI Xin;MEI Kai;WANG Xin-yi;WANG Ling-min;WU Qing;Beijing University of Chinese Medicine;

DOI: 10.19540/j.cnki.cjcmm.20211104.302

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