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基于天然聚合物的pH响应性交联聚合物基质:工艺变量对溶胀特性和药物递送性能的影响。

pH responsive cross-linked polymeric matrices based on natural polymers: effect of process variables on swelling characterization and drug delivery properties.

作者信息

Naeem Fahad, Khan Samiullah, Jalil Aamir, Ranjha Nazar Muhammad, Riaz Amina, Haider Malik Salman, Sarwar Shoaib, Saher Fareha, Afzal Samrin

机构信息

Faculty of Pharmacy, Bahauddin Zakariya University, Multan-60800 Pakistan.

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

出版信息

Bioimpacts. 2017;7(3):177-192. doi: 10.15171/bi.2017.21. Epub 2017 Aug 16.

DOI:10.15171/bi.2017.21
PMID:29159145
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5684509/
Abstract

The current work was aimed to design and synthesize novel crosslinked pH-sensitive gelatin/pectin (Ge/Pec) hydrogels using different polymeric ratios and to explore the effect of polymers and degree of crosslinking on dynamic, equilibrium swelling and in vitro release behavior of the model drug (Mannitol). The Ge/Pec based hydrogels were prepared using glutaraldehyde as the crosslinker. Various structural parameters that affect their release behavior were determined, including swelling study, porosity, sol-gel analysis, average molecular weight between crosslinks (Mc), volume fraction of polymer (V2,s), solvent interaction parameter (χ) and diffusion coefficient. The synthesized hydrogels were subjected to various characterization tools like Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD) and DSC differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). The hydrogels show highest water uptake and release at lower pH values. The FTIR spectra showed an interaction between Ge and Pec, and the drug-loaded samples also showed the drug-related peaks, indicating proper loading of the drug. DSC and TGA studies confirmed the thermal stability of hydrogel samples, while SEM showed the porous nature of hydrogels. The drug release followed non-Fickian diffusion or anomalous mechanism. Aforementioned characterizations reveal the successful formation of copolymer hydrogels. The pH-sensitive swelling ability and drug release behavior suggest that the rate of polymer chain relaxation and drug diffusion from these hydrogels are comparable which also predicts their possible use for site-specific drug delivery.

摘要

当前的工作旨在使用不同的聚合物比例设计并合成新型交联的pH敏感明胶/果胶(Ge/Pec)水凝胶,并探究聚合物和交联度对模型药物(甘露醇)的动力学、平衡溶胀及体外释放行为的影响。以戊二醛作为交联剂制备了基于Ge/Pec的水凝胶。测定了影响其释放行为的各种结构参数,包括溶胀研究、孔隙率、溶胶-凝胶分析、交联点间的平均分子量(Mc)、聚合物的体积分数(V2,s)、溶剂相互作用参数(χ)和扩散系数。对合成的水凝胶进行了各种表征手段,如傅里叶变换红外光谱(FTIR)、X射线衍射(XRD)、差示扫描量热法(DSC)和扫描电子显微镜(SEM)。水凝胶在较低pH值下表现出最高的吸水量和释放量。FTIR光谱显示Ge和Pec之间存在相互作用,载药样品也显示出与药物相关的峰,表明药物负载良好。DSC和TGA研究证实了水凝胶样品的热稳定性,而SEM显示了水凝胶的多孔性质。药物释放遵循非菲克扩散或反常机制。上述表征揭示了共聚物水凝胶的成功形成。pH敏感的溶胀能力和药物释放行为表明,聚合物链松弛速率和药物从这些水凝胶中的扩散速率相当,这也预示了它们在定点给药方面的潜在用途。

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