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Preparation and evaluation of photocrosslinkable chitosan as a drug delivery matrix

机译:光可交联壳聚糖作为药物传递基质的制备与评价

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Epichlorohydrin (1-chloro-2,3-epoxypropane) was reacted with sodium azide in the presence of a phase transfer catalyst to obtain 1-cliloro-2-hydroxy-3-azidopropane, which was further coupled onto chitosan to prepare. a photocrosslinkable derivative of the biopolymer. Elemental analysis and infrared (IR) spectroscopy confirmed the incorporation of azide groups onto chitosan. Films were cast from an aqueous acetic acid solution of azidated chitosan containing a model drug, such as theophylline. Irradiation of the film with ultraviolet (UV) light led to crosslinking of the drug incorporated film. IR spectra indicated complete surface crosslinking within 2 h of irradiation. Release of theophylline from uncrosslinked and crosslinked films was examined in simulated gastric and intestinal fluids without enzymes at 37 degreesC. The release of the drug from the crosslinked films was slower than the release from uncrosslinked films. Although the system is far from being optimized to obtain sustained release of a pharmacologically active agent for long periods, the data obtained indicate the possibility of developing photocrosslinkable matrices of biopolymers, such as chitosan, for sustained drug delivery with many advantages over chemical crosslinking. (C) 2002 Wiley Periodicals, Inc. [References: 22]
机译:在相转移催化剂的存在下,使表氯醇(1-氯-2,3-环氧丙烷)与叠氮化钠反应,获得1-氯-2-羟基-3-叠氮基丙烷,将其进一步偶联到壳聚糖上制备。生物聚合物的光可交联衍生物。元素分析和红外(IR)光谱证实叠氮化物基团结合到壳聚糖上。从叠氮化的壳聚糖的乙酸水溶液中流延膜,其中所述叠氮化的壳聚糖含有模型药物,例如茶碱。用紫外线(UV)照射膜导致药物结合膜的交联。红外光谱表明在照射后2小时内表面完全交联。在没有酶的模拟胃液和肠液中,在37摄氏度下检查了茶碱从未交联和交联的膜中的释放。药物从交联膜的释放比未交联膜的释放慢。尽管该系统远未达到获得药理活性剂长期持续释放的最佳状态,但获得的数据表明,有可能开发生物聚合物(如壳聚糖)的光可交联基质,以实现持续药物输送,并且具有比化学交联更大的优势。 (C)2002 Wiley Periodicals,Inc. [参考:22]

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