Key Laboratory for Biomechanics and Mechanobiology (Beihang University) of Ministry of Education, Beijing Advanced Innovation Center for Biomedical Engineering, School of Biological Science and Medical Engineering, Beihang University, Beijing 100083, P.R. China.
School of Life Sciences and Technology, Harbin Institute of Technology, Harbin, Heilongjiang 150001, P.R. China.
Mater Sci Eng C Mater Biol Appl. 2021 Dec;131:112527. doi: 10.1016/j.msec.2021.112527. Epub 2021 Oct 27.
Quercetin (Que) has been proved to have various biological activities, including anti-oxidation, anti-inflammation and anti-virus, showing great potential in liver protection. However, its water insolubility leads to low bioavailability. Therefore, the development of a suitable drug delivery fashion is imminent. In recent years, liposomes have been widely used in the fields of drug delivery and gene transfer thanks to the cell membrane like structure, easy surface-modification and high encapsulation efficiency. Herein, we fabricated Que loaded anionic liposomes. Galactosylated chitosan (GC) was simply attached to the surfaces of liposomes through electrostatic adsorption to achieve targeted delivery by binding to asialoglycoprotein receptor (ASGPR). The results showed that Que loaded liposomes modified with GC (GC-Que-Lipo) could enrich the liver in mice through tail vein injection. Liposomes could achieve sustained drug release and GC-Que-Lipo promoted M2 polarization of macrophages. More importantly, it could maintain low content of AST, ALT, ALP and high level of GSH while reducing lipid oxidation, thereby protecting the liver from damage in acute liver injury model. In general, we expect to be able to acquire targeted and efficient delivery of quercetin through a facile approach, thus fulfill the prevention and treatment of liver diseases.
槲皮素 (Que) 已被证明具有多种生物活性，包括抗氧化、抗炎和抗病毒作用，在肝脏保护方面具有很大的潜力。然而，其水溶性差导致生物利用度低。因此，开发合适的药物输送方式迫在眉睫。近年来，由于具有类似细胞膜的结构、易于表面修饰和高包封效率，脂质体在药物输送和基因转导领域得到了广泛应用。本文制备了载有槲皮素的阴离子脂质体。通过静电吸附将半乳糖化壳聚糖 (GC) 简单地附着在脂质体表面，通过与去唾液酸糖蛋白受体 (ASGPR) 结合实现靶向递送。结果表明，通过尾静脉注射，载有 Que 的脂质体经 GC 修饰（GC-Que-Lipo）后可在小鼠肝脏中富集。脂质体可以实现药物的持续释放，GC-Que-Lipo 促进了巨噬细胞的 M2 极化。更重要的是，它可以保持低的 AST、ALT、ALP 含量和高的 GSH 水平，同时减少脂质氧化，从而在急性肝损伤模型中保护肝脏免受损伤。总的来说，我们期望通过一种简便的方法获得槲皮素的靶向和高效递送，从而实现对肝脏疾病的预防和治疗。
