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用于自我调节无突释长效释放的碘响应性聚(甲基丙烯酸羟乙酯-聚乙烯吡咯烷酮)水凝胶

Iodine-responsive poly (HEMA-PVP) hydrogel for self-regulating burst-free extended release.

作者信息

Xu Jinku, Zhao Peili, Zhang Yongchun

机构信息

a Biomaterials and Drug Delivery System Laboratory , School of Chemistry and Pharmaceutical Engineering, Qilu University of Technology , Jinan , China.

出版信息

J Biomater Sci Polym Ed. 2017 Apr;28(5):470-485. doi: 10.1080/09205063.2017.1279533. Epub 2017 Jan 30.

DOI:10.1080/09205063.2017.1279533
PMID:28077032
Abstract

Swollen hydrogels with extended iodine release kinetics is highly desirable for burn and scald treatment. In this paper semi-interpenetrating poly (HEMA-PVP) hydrogels were prepared by radical polymerization followed by thermo-treatment to crosslink its PVP component. Incorporation of PVP component endows the hydrogels responsive to loaded iodine undergoing a reversible shrunken/swollen volume transition. This resulted in a self-regulating iodine release model, in which shrunken hydrogel at high iodine loading decreased drug diffusion thereby reducing burst release, and then gradually swollen hydrogel as drug release ensures rapid release of dissociated drug from strong affinity sites on hydrogel backbone, achieving a burst-free extended release. The hydrogels demonstrated 11.5-fold higher iodine loading than pure pHEMA hydrogel and showed a highest 40% volume shrink. Initial burst release of iodine was efficiently decreased from 12,894 μg/day of pure pHEMA hydrogel to 2570 μg/day of pHEMA/PVP hydrogel with 37% PVP content. Iodine-loaded hydrogels showed zero-order release at three time periods of 0-15 h, 15 h-3.5 days and 3.5-23.5 days corresponding to release rate of 2570, 776 and 493 μg/day. The work gained a new insight into swollen hydrogel drug delivery system with burst-free extended drug release kinetics.

摘要

具有延长碘释放动力学的肿胀水凝胶对于烧伤和烫伤治疗非常理想。本文通过自由基聚合制备了半互穿聚(HEMA-PVP)水凝胶,随后进行热处理以交联其PVP组分。PVP组分的加入使水凝胶对负载的碘产生响应,经历可逆的收缩/肿胀体积转变。这产生了一种自调节碘释放模型,其中在高碘负载下收缩的水凝胶减少了药物扩散,从而减少了突释,然后随着药物释放水凝胶逐渐肿胀,确保解离的药物从水凝胶主链上的强亲和位点快速释放,实现无突释的延长释放。该水凝胶的碘负载量比纯pHEMA水凝胶高11.5倍,体积收缩率最高可达40%。碘的初始突释从纯pHEMA水凝胶的12894μg/天有效降低到PVP含量为37%的pHEMA/PVP水凝胶的2570μg/天。负载碘的水凝胶在0-15小时、15小时-3.5天和3.5-23.5天三个时间段显示零级释放,对应释放速率分别为2570、776和493μg/天。这项工作为具有无突释延长药物释放动力学的肿胀水凝胶药物递送系统提供了新的见解。

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