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以盐酸二甲双胍为模型药物的基于瓜尔胶的新型聚合基质的制备、表征及控释性能的体外评价。

Development, characterization and In-vitro evaluation of guar gum based new polymeric matrices for controlled delivery using metformin HCl as model drug.

机构信息

College of Pharmacy and Health Sciences, Ajman University, Ajman, United Arab Emirates.

Medical and Bio-allied Health Sciences Research Centre, Ajman University, Ajman, United Arab Emirates.

出版信息

PLoS One. 2022 Jul 28;17(7):e0271623. doi: 10.1371/journal.pone.0271623. eCollection 2022.

DOI:10.1371/journal.pone.0271623
PMID:35901085
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9333214/
Abstract

Currently, hydrogels are considered as ideal biomaterials due to their unique structure and characteristics that facilitates considerable hydrophilicity, swelling, drug loading and release. In this study, we report pH-responsive GG-MAA-AMPS hydrogel delivery system prepared via free radical polymerization technique. Hydrogels were loaded with Metformin HCl as a model drug. Hydrogels were characterized through Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). FTIR confirmed the successful crosslinking of reactants, hydrogel network formation and drug loading. TGA and DSC proved the higher thermal stability of reactants after crosslinking and drug loading. XRD analysis showed decrease in crystallinity of drug after loading into the hydrogels. SEM revealed smooth and glassy appearance of both loaded and unloaded hydrogels. Gel content was increased with increase in concentration of reactants. Drug entrapment was decreased by increasing concentration of GG and AMPS while MAA acted inversely. Hydrogels displayed pH-dependent swelling and drug release behavior being high at pH 6.8 and 7.4 while low at acidic pH (1.2). Oral tolerability in rabbits showed that hydrogels were safe without causing any hematological or histopathological changes in healthy rabbits. Based on the obtained results, GG-MAA-AMPS can be considered as potential carrier for metformin HCl as well as other hydrophilic drugs.

摘要

目前,水凝胶因其独特的结构和特性而被认为是理想的生物材料,这些特性包括相当的亲水性、溶胀性、药物负载和释放能力。在本研究中,我们报告了一种通过自由基聚合技术制备的 pH 响应 GG-MAA-AMPS 水凝胶输送系统。水凝胶中负载了盐酸二甲双胍作为模型药物。通过傅里叶变换红外光谱(FTIR)、热重分析(TGA)、差示扫描量热法(DSC)、X 射线衍射(XRD)和扫描电子显微镜(SEM)对水凝胶进行了表征。FTIR 证实了反应物的成功交联、水凝胶网络的形成和药物负载。TGA 和 DSC 证明了反应物交联和药物负载后的热稳定性更高。XRD 分析表明,药物在负载到水凝胶后结晶度降低。SEM 显示了负载和未负载水凝胶的光滑和玻璃状外观。凝胶含量随反应物浓度的增加而增加。药物包封率随 GG 和 AMPS 浓度的增加而降低,而 MAA 的作用则相反。水凝胶表现出 pH 依赖性溶胀和药物释放行为,在 pH 值为 6.8 和 7.4 时较高,而在酸性 pH 值(1.2)时较低。兔子的口服耐受性研究表明,水凝胶是安全的,不会在健康兔子中引起任何血液学或组织病理学变化。基于获得的结果,GG-MAA-AMPS 可被视为盐酸二甲双胍以及其他亲水性药物的潜在载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/e100a37b3586/pone.0271623.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/f59ffd2138c2/pone.0271623.g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/cab5c93beb6d/pone.0271623.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/dfa18318469c/pone.0271623.g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/8de29d12c54c/pone.0271623.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/e100a37b3586/pone.0271623.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/f59ffd2138c2/pone.0271623.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/533eda0ceaca/pone.0271623.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/d556b8b08921/pone.0271623.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/cab5c93beb6d/pone.0271623.g004.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/8de29d12c54c/pone.0271623.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ef13/9333214/e100a37b3586/pone.0271623.g007.jpg

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