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奥贝胆酸结合到人血清白蛋白纳米粒中:为开发稳定制剂优化制备参数。

Incorporation of obidoxime into human serum albumin nanoparticles: optimisation of preparation parameters for the development of a stable formulation.

机构信息

Institute of Pharmaceutical Technology, Goethe University, Frankfurt am Main, Germany.

出版信息

J Microencapsul. 2010;27(7):594-601. doi: 10.3109/02652048.2010.501395.

Abstract

Intoxication with organophosphorous nerve agents such as paraoxon requires immediate administration of antidotes such as oximes. However, the oximes lack sufficient activity in the central nervous system as they are unable to rapidly penetrate the blood-brain barrier (BBB) in therapeutically relevant concentrations. Human serum albumin (HSA) nanoparticles represent a promising drug carrier system for the transport of drugs across the BBB. This study focussed on the development of an obidoxime-loaded nanoparticles prepared by desolvation using an incorporation technique. The nanoparticle preparation parameters, i.e. drug amount, pH value, ethanol volume and crosslinking degree, were optimised. The in vitro release study showed a sustained release profile, indicating the suitability of the developed formulation for the transport of oximes across the BBB.

摘要

有机磷神经毒剂如对氧磷中毒需要立即给予解毒剂,如肟类。然而,肟类由于无法快速穿透血脑屏障(BBB)以达到治疗相关浓度,因此在中枢神经系统中的活性不足。人血清白蛋白(HSA)纳米粒是一种很有前途的药物载体系统,可用于将药物输送穿过 BBB。本研究集中于通过去溶剂化作用使用包埋技术制备负载羟肟酸的纳米粒。优化了纳米粒制备参数,如药物用量、pH 值、乙醇体积和交联度。体外释放研究显示出持续释放的特征,表明所开发的制剂适合将肟类药物输送穿过 BBB。

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