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Stimuli-responsive chitosan-graft-poly(N-vinylcaprolactam) as a promising material for controlled hydrophobic drug delivery

机译:刺激响应的壳聚糖接枝聚(N-乙烯基己内酰胺)作为一种有望用于控制疏水性药物输送的材料

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摘要

A novel type of pH- and thermo-responsive copolymer, chitosan-graft-poly(N-vinylcaprolactam) (chitosan-g-PNVCL), was prepared by grafting carboxyl-terminated poly(N- vinylcaprolactam) (PNVCL-COOH) chains onto a chitosan backbone as a drug-delivery carrier. The formation of chitosan-g-PNVCL was confirmed by FT-IR and H-1 NMR techniques. Chitosan-g-PNVCL showed a definite phase transition at 32 degrees C as occurs in pure PNVCL. The swelling degree of the chitosan-g-PNVCL beads was found to be higher at pH 2.2 than at pH 7.4. Moreover, the swelling degree of the beads decreased with increased environmental temperature. Compared to the chitosan beads, the release profile of chitosan-g-PNVCL beads showed a slower and more controlled release of the entrapped ketoprofen. The release behavior of the chitosan-g-PNVCL beads was influenced by both the pH and temperature of the medium. The MTT assay showed no obvious cytotoxicity of chitosan-g-PNVCL against a human endothelial cell line over a concentration range of 0-400 mu g center dot mL(-1). These results suggest that chitosan-g-PNVCL could be a potential stimuli-responsive material for controlled drug delivery, and it may improve the bioavailability, efficacy, and compliance of the encapsulated drugs.
机译:通过将羧基封端的聚(N-乙烯基己内酰胺)(PNVCL-COOH)链接枝到壳中,制备了一种新型的pH和热敏共聚物,即壳聚糖-接枝-聚(N-乙烯基己内酰胺)(壳聚糖-g-PNVCL)。壳聚糖骨架作为药物递送载体。通过FT-IR和H-1 NMR技术证实了壳聚糖-g-PNVCL的形成。壳聚糖-g-PNVCL与纯PNVCL一样,在32摄氏度时显示出确定的相变。发现壳聚糖-g-PNVCL珠的溶胀度在pH 2.2下比在pH 7.4下更高。而且,珠粒的溶胀度随着环境温度的升高而降低。与壳聚糖珠相比,壳聚糖-g-PNVCL珠的释放曲线显示,被包裹的酮洛芬的释放较慢且受控程度更高。壳聚糖-g-PNVCL珠的释放行为受培养基的pH和温度影响。 MTT分析显示,在0-400μg中心点mL(-1)的浓度范围内,壳聚糖-g-PNVCL对人内皮细胞系没有明显的细胞毒性。这些结果表明,壳聚糖-g-PNVCL可能是控制药物输送的潜在刺激反应材料,它可以改善包封药物的生物利用度,功效和顺应性。

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