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化学交联的聚乙烯醇-共聚甲基丙烯酸水凝胶的共聚合成;5-氟尿嘧啶口服给药的潜在接枝聚合物载体。

Synthesis of chemically cross-linked polyvinyl alcohol-co-poly (methacrylic acid) hydrogels by copolymerization; a potential graft-polymeric carrier for oral delivery of 5-fluorouracil.

机构信息

Faculty of Pharmacy and Alternative Medicine, the Islamia University of Bahawalpur-63100, Punjab, Pakistan.

出版信息

Daru. 2013 May 30;21(1):44. doi: 10.1186/2008-2231-21-44.

Abstract

BACKGROUND OF THE STUDY

The propose of the present work was to develop chemically cross-linked polyvinyl alcohol-co-poly(methacrylic acid) hydrogel (PVA-MAA hydrogel) for pH responsive delivery of 5-Fluorouracil (5-FU).

METHODS

PVA based hydrogels were prepared by free radical copolymerization. PVA has been cross-linked chemically with monomer (methacrylic acid) in aqueous medium, cross-linking agent was ethylene glycol di-methacrylate (EGDMA) and benzoyl peroxide was added as reaction initiator. 5-FU was loaded as model drug. FTIR, XRD, TGA and DSC were performed for characterization of copolymer. Surface morphology was studied by SEM. pH sensitive properties were evaluated by swelling dynamics and equilibrium swelling ratio at low and higher pH.

RESULTS

FTIR, XRD, TGA and DSC studies confirmed the formation of new copolymer. Formulations with higher MAA contents showed maximum swelling at 7.4 pH. High drug loading and higher drug release has been observed at pH 7.4.

CONCLUSIONS

The current study concludes that a stable copolymeric network of PVA was developed with MAA. The prepared hydrogels were highly pH responsive. This polymeric network could be a potential delivery system for colon targeting of 5-FU in colorectal cancers.

摘要

研究背景

本研究旨在开发化学交联的聚乙烯醇-共聚(甲基丙烯酸)水凝胶(PVA-MAA 水凝胶),用于 pH 响应递药 5-氟尿嘧啶(5-FU)。

方法

通过自由基共聚制备基于 PVA 的水凝胶。PVA 在水介质中与单体(甲基丙烯酸)进行化学交联,使用的交联剂是乙二醇二甲基丙烯酸酯(EGDMA),并添加过氧化苯甲酰作为反应引发剂。将 5-FU 作为模型药物进行负载。采用傅里叶变换红外光谱(FTIR)、X 射线衍射(XRD)、热重分析(TGA)和差示扫描量热法(DSC)对共聚物进行了表征。通过扫描电子显微镜(SEM)研究了表面形态。通过低 pH 和高 pH 下的溶胀动力学和平衡溶胀比评估了 pH 敏感性。

结果

FTIR、XRD、TGA 和 DSC 研究证实了新共聚物的形成。含有更高 MAA 含量的配方在 7.4 pH 时表现出最大的溶胀。在 pH 7.4 时观察到高载药量和更高的药物释放。

结论

本研究得出结论,开发了具有 MAA 的 PVA 稳定共聚网络。所制备的水凝胶对 pH 具有高度响应性。这种聚合物网络可能是用于结直肠癌中 5-FU 结肠靶向的潜在递药系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fafc/3704659/5a05f3a82765/2008-2231-21-44-1.jpg

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