口服环孢素A——其脂质体及其他递送系统的现状
Oral cyclosporine A--the current picture of its liposomal and other delivery systems.
作者信息
Czogalla Aleksander
机构信息
Research and Development Centre Novasome Sp. Z O.O., ul. Olsztyńska 5, 51-423 Wrocław, Poland.
出版信息
Cell Mol Biol Lett. 2009;14(1):139-52. doi: 10.2478/s11658-008-0041-6. Epub 2008 Nov 12.
Abstract
The discovery of cyclosporine A was a milestone in organ transplantation and the treatment of autoimmune diseases. However, developing an efficient oral delivery system for this drug is complicated by its poor biopharmaceutical characteristics (low solubility and permeability) and the need to carefully monitor its levels in the blood. Current research is exploring various approaches, including those based on emulsions, microspheres, nanoparticles, and liposomes. Although progress has been made, none of the formulations is flawless. This review is a brief description of the main pharmaceutical systems and devices that have been described for the oral delivery of cyclosporine A in the context of the physicochemical properties of the drug and the character of its interactions with lipid membranes.
摘要
环孢素A的发现是器官移植和自身免疫性疾病治疗领域的一个里程碑。然而，由于该药物生物药剂学特性不佳（低溶解度和低渗透性）以及需要仔细监测其血药浓度，开发一种高效的口服给药系统变得很复杂。目前的研究正在探索各种方法，包括基于乳剂、微球、纳米颗粒和脂质体的方法。尽管已经取得了进展，但没有一种制剂是完美无缺的。本综述简要介绍了在环孢素A的物理化学性质及其与脂质膜相互作用特点的背景下，已报道的用于环孢素A口服给药的主要药物系统和装置。
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