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载姜黄素和汉防己甲素的纳米脂质体的双重载药：制备、表征、肝毒性和抗肿瘤作用。

Nano-Liposomes Double Loaded with Curcumin and Tetrandrine: Preparation, Characterization, Hepatotoxicity and Anti-Tumor Effects.

机构信息

State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

出版信息

Int J Mol Sci. 2022 Jun 20;23(12):6858. doi: 10.3390/ijms23126858.

DOI:10.3390/ijms23126858
PMID:35743311
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9224699/
Abstract

(1) Background: Curcumin (CUR) and tetrandrine (TET) are natural compounds with various bioactivities, but have problems with low solubility, stability, and absorption rate, resulting in low bioavailability, and limited applications in food, medicine, and other fields. It is very important to improve the solubility while maintaining the high activity of drugs. Liposomes are micro-vesicles synthesized from cholesterol and lecithin. With high biocompatibility and biodegradability, liposomes can significantly improve drug solubility, efficacy, and bioavailability. (2) Methods: In this work, CUR and TET were encapsulated with nano-liposomes and g DSPE-MPEG 2000 (DP)was added as a stabilizer to achieve better physicochemical properties, biosafety, and anti-tumor effects. (3) Results: The nano-liposome (CT-DP-Lip) showed stable particle size (under 100 nm) under different conditions, high solubility, drug encapsulation efficiency (EE), loading capacity (LC), release rate in vitro, and stability. In addition, in vivo studies demonstrated CT-DP-Lip had no significant toxicity on zebrafish. Tumor cytotoxicity test showed that CT-DP-Lip had a strong inhibitory effect on a variety of cancer cells. (4) Conclusions: This work showed that nano-liposomes can significantly improve the physical and chemical properties of CUR and TET and make them safer and more efficient.

摘要

（1）背景：姜黄素（CUR）和汉防己甲素（TET）是具有多种生物活性的天然化合物，但存在溶解度、稳定性和吸收率低的问题，导致生物利用度低，在食品、医药等领域的应用受到限制。提高药物的溶解度而保持其高活性非常重要。脂质体是由胆固醇和卵磷脂合成的微型囊泡。脂质体具有高生物相容性和可生物降解性，可以显著提高药物的溶解度、疗效和生物利用度。（2）方法：在这项工作中，CUR 和 TET 被包裹在纳米脂质体中，并添加 g-DSPE-MPEG 2000（DP）作为稳定剂，以实现更好的物理化学性质、生物安全性和抗肿瘤效果。（3）结果：纳米脂质体（CT-DP-Lip）在不同条件下表现出稳定的粒径（小于 100nm）、高溶解度、药物包封效率（EE）、载药量（LC）、体外释放率和稳定性。此外，体内研究表明 CT-DP-Lip 对斑马鱼没有明显的毒性。肿瘤细胞毒性试验表明，CT-DP-Lip 对多种癌细胞具有强烈的抑制作用。（4）结论：这项工作表明，纳米脂质体可以显著改善 CUR 和 TET 的物理化学性质，使其更安全、更有效。

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