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聚(乙烯-乙烯醇)/聚(δ-戊内酯)/阿司匹林复合材料:一种新型药物载体系统的模型

Poly(ethylene--vinylalcohol)/Poly(δ-valerolactone)/Aspirin Composite: Model for a New Drug-Carrier System.

作者信息

Alghamdi Abdulaziz Ali, Saeed Waseem Sharaf, Al-Odayni Abdel-Basit, Alharthi Fahad A, Semlali Abdelhabib, Aouak Taieb

机构信息

Chemistry Department, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

Groupe de Recherche en Écologie Buccale, Faculté de Médecin Dentaire, Université Laval, G1V 0A6, QC, Canada.

出版信息

Polymers (Basel). 2019 Mar 6;11(3):439. doi: 10.3390/polym11030439.

Abstract

The release dynamics of aspirin(ASP), used as a drug model, from the poly(ethylene--vinyl alcohol)/poly(δ-valerolactone) (PE--VAL/Pδ-VL) hydrogel blend was controlled by varying the blend's degree of swelling through a gradual loading of Pδ-VL (hydrophobic polymer) in this copolymer matrix. To achieve this goal, a series of PE--VAL/Pδ-VL blends with different ratios was prepared through the solvent casting method, and the miscibility of this polymer blend was evaluated by using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and scanning electronic microscopy methods. The tests of cell adhesion and growth on the PE--VAL/Pδ-VL specimens were performed using the 3-(4,5-demethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and the results obtained were the best performance in terms of cell viability, cell adhesion, and growth of the PE--VAL/Pδ-VL50 material. The dynamic mechanical properties of the prepared material were also examined by dynamic mechanical analysis; the results obtained showed a material having intermediary mechanical properties between those of the two components. On the basis of these characterizations, the blend showing the best performance, such as the PE--VAL/Pδ-VL50 system, was chosen as a carrier to study the in vitro control of the release dynamics of ASP from the ASP/PE--VAL/Pδ-VL drug-carrier system when administered orally, in which the influences of the ASP content and the degree of swelling of the PE--VAL/Pδ-VL blend were investigated. Based on the data obtained and the gastrointestinal transit time reported by Beltzer et al., it was possible to estimate the distribution of the in vitro cumulative ASP released in different digestive system organs regardless of the actions of any enzymes and microorganisms and select the best-performing drug-carrier system.

摘要

以阿司匹林(ASP)作为药物模型,通过在该共聚物基质中逐步加入聚(δ-戊内酯)(Pδ-VL,疏水性聚合物)来改变聚(乙烯-乙烯醇)/聚(δ-戊内酯)(PE-VAL/Pδ-VL)水凝胶共混物的溶胀度,从而控制阿司匹林从该共混物中的释放动力学。为实现这一目标,采用溶液浇铸法制备了一系列不同比例的PE-VAL/Pδ-VL共混物,并通过傅里叶变换红外光谱、差示扫描量热法、X射线衍射和扫描电子显微镜等方法对该聚合物共混物的混溶性进行了评估。使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐(MTT)法对PE-VAL/Pδ-VL样品进行细胞黏附与生长测试,结果表明PE-VAL/Pδ-VL50材料在细胞活力、细胞黏附及生长方面表现最佳。还通过动态力学分析对所制备材料的动态力学性能进行了检测;结果表明该材料具有介于两种组分之间的中间力学性能。基于这些表征,选择表现最佳的共混物,如PE-VAL/Pδ-VL50体系,作为载体来研究口服给药时ASP/PE-VAL/Pδ-VL药物载体系统中ASP释放动力学的体外控制,其中研究了ASP含量和PE-VAL/Pδ-VL共混物溶胀度的影响。根据所获得的数据以及Beltzer等人报道的胃肠道转运时间,无需考虑任何酶和微生物的作用,就有可能估算出体外累积释放的ASP在不同消化系统器官中的分布,并选择性能最佳的药物载体系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f24a/6473899/51c78e766d47/polymers-11-00439-g001.jpg

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