岩黄连碱是广西壮族民间常用保肝药材岩黄连中的主要有效成分之一，又名脱氢卡维丁，是一种重要的生物碱类化合物，药理研究表明其具有抗肝纤维化、抗病毒、抗肿瘤、抗菌等生物活性。本课题组前期研究表明，岩黄连碱具有较好的抗肝纤维化作用，但因其水中溶解度欠佳，口服给药后首过效应明显，以致其生物利用度低下，从而限制了其临床应用。纳米结构脂质载体是以一种可将难溶性药物包裹于类脂核中的新型纳米给药系统，为第二代脂质纳米粒，具有高效载药能力和良好稳定性，并能调整药物释放曲线，且具有缓控释作用。本研究以岩黄连碱为模型药物，将具有肝细胞靶向作用的半乳糖-胆固醇配体结合甘草次酸配体共同修饰于包载有抗肝纤维化药物岩黄连碱的纳米结构脂质载体，以此构建一种高效低毒的新型肝靶向岩黄连碱纳米递药系统，并评价其肝靶向性和药效活性。研究为民族药岩黄连碱新制剂的研发及临床应用提供实验依据，也为肝靶向纳米药物载体的研究提供一种新思路。

Dehydrocavidine is an important alkaloid compound, and it is also one of the main active ingredients in Yanhuanglian(Corydalis saxicola Bunting), a commonly used liver-protecting medicinal herb of Zhuang nationality in Guangxi.Modern pharmacological studies have shown that it has many biological activities such as anti-hepatic fibrosis, anti-virus, anti-tumor, anti-bacterial and so on.Preliminary research of our group shows dehyrocavidine has significant anti-hepatic fibrosis activity,however, due to its poor solubility in water and obvious first-pass effect after oral administration, its bioavailability is low, which limits its clinical application.Nanostructured lipid carriers are the second generation lipid nanoparticles, which are a new nano-drug delivery system that can encapsulate insoluble drugs in lipoid nuclei.It has high drug loading capacity and good stability, and can adjust drug release curve, and has sustained and controlled release effect.In this study, the liver-targeting galactose-cholesterol ligand and glycyrrhetinic acid ligand were co-modified on the surface of nanostructured lipid carriers containing dehydrocavidine to construct a novel liver-targeting dehydrocavidine Nanodelivery system with high efficiency and low toxicity, and to evaluate its liver targeting and pharmacodynamic activity.This study provides an experimental basis for the development and clinical application of new preparations of folk medicine dehydrocavidine, as well as a new idea for the study of liver-targeting nano-drug carriers.