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用于胰岛素递送的聚氧乙烯烷基醚脂质体的体外研究

In vitro study of polyoxyethylene alkyl ether niosomes for delivery of insulin.

作者信息

Pardakhty Abbas, Varshosaz Jaleh, Rouholamini Abdolhossein

机构信息

Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Kerman University of Medical Sciences, PO Box 76175-493, Kerman, Iran.

出版信息

Int J Pharm. 2007 Jan 10;328(2):130-41. doi: 10.1016/j.ijpharm.2006.08.002. Epub 2006 Aug 12.

Abstract

In this study, niosomes of polyoxyethylene alkyl ethers (Brij) were prepared for encapsulation of insulin by film hydration method. Without cholesterol, brij 35 and brij 58 did not form niosomes, apparently because of relatively large polar head groups in comparison with their alkyl chains. The size of vesicles depended on the cholesterol content, charge incorporation or hydrophilicity of surfactants. Entrapment of insulin in bilayer structure of niosomes protected it against proteolytic activity of alpha-chymotrypsin, trypsin and pepsin in vitro. The maximum protection activity was seen in brij 92/cholesterol (7:3 molar ratios) in which only 26.3+/-3.98% of entrapped insulin was released during 24h in simulated intestinal fluid (SIF). The kinetic of drug release for most formulations could be best described by Baker and Lonsdale equation indicating diffusion based delivery mechanism. These results indicate that niosomes could be developed as sustained release oral dosage forms for delivery of peptides and proteins such as insulin.

摘要

在本研究中,采用薄膜水化法制备了聚氧乙烯烷基醚(Brij)脂质体用于包封胰岛素。在没有胆固醇的情况下,Brij 35和Brij 58不能形成脂质体,显然是因为与其烷基链相比,其极性头部基团相对较大。囊泡的大小取决于胆固醇含量、电荷掺入或表面活性剂的亲水性。胰岛素包封在脂质体的双层结构中,在体外可保护其免受α-糜蛋白酶、胰蛋白酶和胃蛋白酶的蛋白水解活性影响。在Brij 92/胆固醇(摩尔比7:3)中观察到最大保护活性,在模拟肠液(SIF)中24小时内仅有26.3±3.98%的包封胰岛素释放。大多数制剂的药物释放动力学可用Baker和Lonsdale方程最好地描述,表明其基于扩散的递送机制。这些结果表明,脂质体可开发为用于递送胰岛素等肽和蛋白质的缓释口服剂型。

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