脂蛋白作为环孢素A的药物载体：包封率的优化

Lipoproteins as Drug Carriers for Cyclosporine A: Optimization of the Entrapment.

作者信息

Abdel-Mottaleb Mona M A, Boi Lorenza, Barra Marina, Colin Julie, Berni Luisa, Béduneau Arnaud, Moulari Brice, Pellequer Yann

机构信息

Department of Pharmaceutics and Industrial Pharmacy, Ain Shams University, Cairo 11566, Egypt.

Department of Drug Science and Technology, University of Turin, 10125 Turin, Italy.

出版信息

Materials (Basel). 2023 Jan 29;16(3):1156. doi: 10.3390/ma16031156.

DOI:10.3390/ma16031156

PMID:36770166

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9918909/

Abstract

Lipoproteins are natural nanostructures responsible for the transport of cholesterol and other lipids in the blood. They are characterized by having a lipophilic core surrounded by an amphiphilic shell composed of phospholipids, cholesterol and one or more apolipoproteins. Being endogenous carriers makes them suitable for drug delivery purposes. Here, we investigate the effect of lipoproteins' intricate composition on the entrapment efficiency of a model drug "Cyclosporine A" into the different types of lipoproteins, namely, HDL, LDL and VLDL. It was observed that the protein content of the lipoproteins had the highest effect on the entrapment of the drug with a correlation coefficient of 0.80, 0.81 and 0.96 for HDL, LDL and VLDL respectively. This was even confirmed by the effect of plasma on the association rate of lipoproteins and the drug. The second effective factor is the cholesterol concentration, while triglycerides and phospholipids had a negligible effect.

摘要

脂蛋白是负责在血液中运输胆固醇和其他脂质的天然纳米结构。它们的特征是具有一个亲脂性核心，周围是由磷脂、胆固醇和一种或多种载脂蛋白组成的两亲性外壳。作为内源性载体使它们适用于药物递送目的。在此，我们研究了脂蛋白复杂组成对模型药物“环孢素A”在不同类型脂蛋白（即高密度脂蛋白（HDL）、低密度脂蛋白（LDL）和极低密度脂蛋白（VLDL））中的包封效率的影响。据观察，脂蛋白的蛋白质含量对药物包封的影响最大，HDL、LDL和VLDL的相关系数分别为0.80、0.81和0.96。血浆对脂蛋白与药物结合速率的影响甚至证实了这一点。第二个有效因素是胆固醇浓度，而甘油三酯和磷脂的影响可忽略不计。