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载布洛芬的壳聚糖-脂质纳米共轭水凝胶与阿拉伯胶:绿色合成、表征、体外动力学机制释放研究及前列腺素E2生成测试

Ibuprofen-Loaded Chitosan-Lipid Nanoconjugate Hydrogel with Gum Arabic: Green Synthesis, Characterisation, In Vitro Kinetics Mechanistic Release Study and PGE2 Production Test.

作者信息

Mahmood Syed, Almurisi Samah Hamed, Al-Japairai Khater, Hilles Ayah Rebhi, Alelwani Walla, Bannunah Azzah M, Alshammari Farhan, Alheibshy Fawaz

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Universiti Malaya, Kuala Lumpur 50603, Malaysia.

Centre for Natural Products Research and Drug Discovery (CENAR), Universiti Malaya, Kuala Lumpur 50603, Malaysia.

出版信息

Gels. 2021 Dec 8;7(4):254. doi: 10.3390/gels7040254.

DOI:10.3390/gels7040254
PMID:34940313
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8701348/
Abstract

Ibuprofen is a well-known non-steroidal anti-inflammatory (NSAID) medicine that is often used to treat inflammation in general. When given orally, it produces gastrointestinal issues which lead to lower patient compliance. Ibuprofen transdermal administration improves both patient compliance and the efficacy of the drug. Nanoconjugation hydrogels were proposed as a controlled transdermal delivery tool for ibuprofen. Six formulations were prepared using different compositions including chitosan, lipids, gum arabic, and polyvinyl alcohol, through ionic interaction, maturation, and freeze-thaw methods. The formulations were characterised by size, drug conjugation efficiency, differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). Further analysis of optimised hydrogels was performed, including X-ray diffraction (XRD), rheology, gel fraction and swelling ability, in vitro drug release, and in vitro macrophage prostaglandin E2 (PGE) production testing. The effects of ibuprofen's electrostatic interaction with a lipid or polymer on the physicochemical and dissolution characterisation of ibuprofen hydrogels were evaluated. The results showed that the S3 (with lipid conjugation) hydrogel provided higher conjugation efficiency and prolonged drug release compared with the S6 hydrogel.

摘要

布洛芬是一种著名的非甾体抗炎药,常用于治疗一般性炎症。口服时,它会引发胃肠道问题,导致患者依从性降低。布洛芬经皮给药可提高患者依从性和药物疗效。纳米共轭水凝胶被提议作为布洛芬的一种可控经皮给药工具。通过离子相互作用、熟化和冻融法,使用包括壳聚糖、脂质、阿拉伯胶和聚乙烯醇在内的不同成分制备了六种制剂。通过尺寸、药物共轭效率、差示扫描量热法(DSC)和傅里叶变换红外光谱法(FTIR)对这些制剂进行了表征。对优化后的水凝胶进行了进一步分析,包括X射线衍射(XRD)、流变学、凝胶分数和溶胀能力、体外药物释放以及体外巨噬细胞前列腺素E2(PGE)生成测试。评估了布洛芬与脂质或聚合物的静电相互作用对布洛芬水凝胶的物理化学和溶解特性的影响。结果表明,与S6水凝胶相比,S3(脂质共轭)水凝胶具有更高的共轭效率和更长的药物释放时间。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54c/8701348/97a2aa7e8b80/gels-07-00254-g010.jpg
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