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包虫囊肿膜的研究:模型分子的渗透及与载药纳米颗粒的相互作用

Study on the hydatid cyst membrane: permeation of model molecules and interactions with drug-loaded nanoparticles.

作者信息

Truong Cong Tri, Faivre Vincent, Nguyen Tien Thanh, Heras Hernan, Pirot Fabrice, Walchshofer Nadia, Sarciron Marie-Elisabeth, Falson Françoise

机构信息

Laboratoire de Pharmacie Galénique Industrielle, ISPB Université Lyon I, Lyon Cedex 08, France.

出版信息

Int J Pharm. 2008 Apr 2;353(1-2):223-32. doi: 10.1016/j.ijpharm.2007.11.040. Epub 2007 Nov 29.

Abstract

The success of the chemotherapeutic treatment of hydatid disease is based upon the drug ability to operate on the germinal layer and on the protoscolices of the hydatid cyst interior at adequate concentrations for sufficient periods. The goal of this study was to evaluate the ability of the drug diffusion through the cyst membrane from sheep hydatid cysts and the increase of drug concentration in the cyst environment. In the first part of this work, the permeation behaviour through the hydatid cyst membrane was studied with five model molecules, having different molecular descriptors (logP, molecular weight, polar surface area ...) onto static Franz glass diffusion cells. A good correlation has been observed between the permeation coefficient and the partition coefficient, log P (r=0.951). In the second part, albendazole-loaded nanoparticles (about 300 nm) prepared by the emulsion solvent evaporation method have shown a sufficient entrapment efficiency (36.4 +/- 6.4%) to raise the apparent solubility of albendazole. The diffusion of drug from the nanoparticles across the hydatid cyst membrane was also improved compare to albendazole suspension. These results have shown the interest of the albendazole-loaded nanoparticles for the treatment of hydatid cysts in the future.

摘要

包虫病化疗治疗的成功基于药物在足够长的时间内以足够的浓度作用于生发层和包虫囊肿内部原头节的能力。本研究的目的是评估药物从绵羊包虫囊肿通过囊肿膜的扩散能力以及囊肿环境中药物浓度的增加情况。在这项工作的第一部分,使用五个具有不同分子描述符(logP、分子量、极性表面积……)的模型分子,在静态Franz玻璃扩散池中研究了通过包虫囊肿膜的渗透行为。观察到渗透系数与分配系数log P之间有良好的相关性(r = 0.951)。在第二部分中,通过乳液溶剂蒸发法制备的载阿苯达唑纳米颗粒(约300 nm)显示出足够的包封效率(36.4 +/- 6.4%),以提高阿苯达唑的表观溶解度。与阿苯达唑悬浮液相比,纳米颗粒中药物通过包虫囊肿膜的扩散也得到了改善。这些结果表明载阿苯达唑纳米颗粒在未来治疗包虫囊肿方面具有应用前景。

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