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一种潜在的纳米药物,由负载肝素的多糖纳米载体组成,用于治疗哮喘。

A potential nanomedicine consisting of heparin-loaded polysaccharide nanocarriers for the treatment of asthma.

机构信息

Department of Pharmacy, Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Santiago de Compostela, Spain.

出版信息

Macromol Biosci. 2012 Feb;12(2):176-83. doi: 10.1002/mabi.201100102. Epub 2011 Nov 23.

Abstract

A new nanomedicine consisting of chitosan/carboxymethyl-β-cyclodextrin loaded with unfractioned or low-molecular-weight heparin is described and its potential in asthma treatment is evaluated. The nanoparticles are prepared by ionotropic gelation showing a size that between 221 and 729 nm with a positive zeta potential. The drug association efficiency is higher than 70%. Developed nanosystems are stable in Hank's balanced salt solution at pH = 6.4, releasing the drug slowly. Ex vivo assays show that nanocarriers lead to an improvement of heparin preventing mast cell degranulation. These results agree with the effective cellular internalization of the fluorescently labeled nanocarriers, and suggest these nanomedicines as promising formulations for asthma treatment.

摘要

一种新型的纳米药物由壳聚糖/羧甲基-β-环糊精负载未分级或低分子量肝素组成,评估其在哮喘治疗中的潜力。该纳米粒子是通过离子凝胶化制备的,其粒径在 221nm 到 729nm 之间,具有正的zeta 电位。药物结合效率高于 70%。在 pH = 6.4 的 Hank 平衡盐溶液中,所开发的纳米系统稳定,药物释放缓慢。体外实验表明,纳米载体可改善肝素对肥大细胞脱颗粒的抑制作用。这些结果与荧光标记的纳米载体的有效细胞内化一致,表明这些纳米药物是治疗哮喘的有前途的制剂。

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