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甲基-β-环糊精修饰的血管假体:修饰程度对不同介质中药物传递性能的影响。

Methyl-β-cyclodextrin modified vascular prosthesis: Influence of the modification level on the drug delivery properties in different media.

机构信息

Université Lille Nord de France, France.

出版信息

Acta Biomater. 2011 Jan;7(1):304-14. doi: 10.1016/j.actbio.2010.09.002. Epub 2010 Sep 9.

Abstract

A textile polyester vascular graft was modified with methyl-β-cyclodextrin (MeβCD) to obtain a new implant capable of releasing antibiotics directly in situ at the site of operation over a prolonged period and thereby prevent post-operative infections. We investigated the influence of the curing parameters (time and temperature) that allow control of the degree of functionalization (DF) of the support by MeβCD. The inclusion of ciprofloxacin (CFX) in the MeβCD cavity was observed in solution by two-dimensional (1)H NMR spectroscopy. The amount of CFX loaded on the modified graft increased with DF. Depending on the release medium (water, phosphate-buffered saline, or human plasma) and the DF of the prostheses, different kinetic profiles of release of CFX were obtained. The sustained release of CFX in human plasma was shown by microbiological assays that indicated prolonged antimicrobial activity against Staphylococcus aureus and Escherichia coli. Viability tests demonstrated the non-toxicity of MeβCD to an epithelial cell line (HPMEC), although a decrease in endothelial cell number was observed on the functionalized prosthesis, probably due to the roughness of the coating and also to the nature of the MeβCD polymer present on the surface of the fibers.

摘要

一种纺织聚酯血管移植物用甲基-β-环糊精(MeβCD)进行了改性,得到了一种新的植入物,能够在手术部位原位长时间直接释放抗生素,从而预防术后感染。我们研究了固化参数(时间和温度)对支持物的功能化程度(DF)的影响,这些参数可以控制支持物的功能化程度。在溶液中通过二维(1)H NMR 光谱观察到环糊精腔内包含环丙沙星(CFX)。负载在改性移植物上的 CFX 量随 DF 的增加而增加。根据释放介质(水、磷酸盐缓冲盐水或人血浆)和假体的 DF,获得了 CFX 释放的不同动力学曲线。通过微生物学分析表明 CFX 在人血浆中的持续释放具有延长的抗金黄色葡萄球菌和大肠杆菌的抗菌活性。细胞活力测试表明 MeβCD 对上皮细胞系(HPMEC)没有毒性,尽管在功能化假体上观察到内皮细胞数量减少,这可能是由于涂层的粗糙度以及纤维表面存在的 MeβCD 聚合物的性质所致。

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