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用于药物持续释放的聚乙烯吡咯烷酮/聚乙二醇环糊精修饰水凝胶

Cyclodextrin modified hydrogels of PVP/PEG for sustained drug release.

作者信息

Nielsen Anne Louise, Madsen Flemming, Larsen Kim Lambertsen

机构信息

Department of Biotechnology, Chemistry and Environmental Engineering, Aalborg University, Aalborg, Denmark.

出版信息

Drug Deliv. 2009 Feb;16(2):92-101. doi: 10.1080/10717540802605129.

Abstract

Hydrogels are water swollen networks of polymers and especially hydrogels consisting of poly vinylpyrrolidone/poly ethyleneglycol-dimethacrylate (PVP/PEG-DMA) blends show promising wound care properties. Enhanced functionality of the hydrogels can be achieved by incorporating drugs and other substances that may assist wound healing into the gel matrix. Controlling the release of active compounds from the hydrogels may be possible by carefully modifying the polymer matrix. For this purpose, cyclodextrins (CD) were grafted to the polymer matrix in 4-5 w/w% in an attempt to retard the release of water-soluble drugs. Ibuprofenate (IBU) was chosen as model drug and loaded in IBU/CD ratios of 0.6, 1.2, and 2.5. Vinyl derivatives of alpha-, beta- and gamma-CD were produced, added to the prepolymer blend and cured by UV-light. During this curing process the CD derivatives were covalently incorporated into the hydrogel matrix. The modified hydrogels were loaded with ibuprofenate by swelling. The release of the model drug from CD modified hydrogels show that especially covalently bonded beta-cyclodextrin can change both the release rate and the release profile of ibuprofen.

摘要

水凝胶是聚合物的水溶胀网络,特别是由聚乙烯吡咯烷酮/聚乙二醇二甲基丙烯酸酯(PVP/PEG-DMA)共混物组成的水凝胶显示出有前景的伤口护理特性。通过将药物和其他可能有助于伤口愈合的物质掺入凝胶基质中,可以实现水凝胶功能的增强。通过仔细修饰聚合物基质,有可能控制水凝胶中活性化合物的释放。为此,将环糊精(CD)以4-5 w/w%的比例接枝到聚合物基质上,试图延缓水溶性药物的释放。选择布洛芬酯(IBU)作为模型药物,并以0.6、1.2和2.5的IBU/CD比例载入。制备了α-、β-和γ-CD的乙烯基衍生物,添加到预聚物共混物中并通过紫外光固化。在该固化过程中,CD衍生物共价掺入水凝胶基质中。通过溶胀将模型药物载入改性水凝胶中。模型药物从CD改性水凝胶中的释放表明,特别是共价键合的β-环糊精可以改变布洛芬的释放速率和释放曲线。

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