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接枝环糊精作为载体用于控制药物释放和高效细胞杀伤。

Grafted cyclodextrin as carrier for control drug delivery and efficient cell killing.

机构信息

School of Materials Science and Technology, Indian Institute of Technology, Banaras Hindu University, Varanasi, 221005, India.

Department of Chemistry, Institute of Science, Banaras Hindu University, Varanasi, 221005, India.

出版信息

J Biomed Mater Res A. 2019 Feb;107(2):434-444. doi: 10.1002/jbm.a.36560. Epub 2018 Nov 22.

Abstract

The presence of hydroxyl groups in cyclodextrin (CD) makes it highly hydrophilic and simultaneously allows its chemical modification to graft polyurethane to control the drug release for longer period of time by maintaining the hydrophobic-hydrophilic balance through varying extent of grafting. Grafting of polyurethane on CD is confirmed through H NMR and molecular weight measurement while FTIR and UV visible studies further support grafting and emphasize the interaction among polymer chains as a whole. Degree of grafting is evaluated from the integrated peak area in NMR spectra. Thermal and mechanical measurements show improved stability and strength of the graft polymers with respect to pure CD. The conversion of particle nature of CD to strip-like morphology in graft copolymers is evident from atomic force microscopy. Sustained drug release has been achieved using graft copolymer against burst release from pure CD and specific interactions, as observed through spectroscopy and thermal measurements, are responsible for sustained release of drug. Biocompatibility of graft copolymers has been checked using cellular studies through MTT assay and cell adhesion. Importantly, the cell killing efficiency has been demonstrated by embedding anticancer drug in polymer matrices causing mortality rate of 75% using graft copolymer against scanty 25% using pure drug or drug embedded in CD and the result is understood from the sustained release of drug from the graft copolymer vis-à-vis burst release in other systems. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 107A: 434-444, 2019.

摘要

环糊精(CD)中存在的羟基使其具有高度的亲水性,同时允许对其进行化学修饰,以接枝聚氨酯,通过保持疏水性-亲水性平衡来控制药物更长时间的释放,接枝程度不同。通过 H NMR 和分子量测量来确认 CD 上的聚氨酯接枝,而 FTIR 和 UV 可见研究进一步支持接枝,并强调聚合物链作为一个整体之间的相互作用。接枝度通过 NMR 光谱中的积分峰面积进行评估。与纯 CD 相比,热重和力学测量显示接枝聚合物的稳定性和强度得到提高。从原子力显微镜可以明显看出,CD 的颗粒性质转化为接枝共聚物中的条状形态。通过光谱和热测量观察到的特定相互作用,使用接枝共聚物实现了药物的持续释放,而不是纯 CD 的突释。通过 MTT 测定和细胞黏附,使用细胞研究检查了接枝共聚物的生物相容性。重要的是,通过将抗癌药物嵌入聚合物基质中,接枝共聚物显示出 75%的细胞杀伤效率,而纯药物或药物嵌入 CD 中的细胞杀伤效率仅为 25%,这可以从接枝共聚物中药物的持续释放与其他系统中的突释来理解。 © 2018 威利父子公司。生物医学材料研究杂志 A 部分:107A:434-444,2019.

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