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巯基改性辣木胶-一种有潜力的生物粘附聚合物。

Thiol modified Moringa gum - A potential bioadhesive polymer.

机构信息

Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, 125001, India.

Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, 125001, India.

出版信息

Carbohydr Polym. 2019 Apr 1;209:400-408. doi: 10.1016/j.carbpol.2018.12.100. Epub 2019 Jan 2.

DOI:10.1016/j.carbpol.2018.12.100
PMID:30732824
Abstract

In the present study Moringa gum was modified by thiolation to enhance its mucoadhesive potential. Thiolation was accomplished by esterification with thioglycolic acid. Thiolated Moringa gum was characterized by FT-IR, TGA, DSC, XRD and SEM-EDX studies. Modified gum was found to have 0.956 ± 0.024 mM of thiol groups/g as determined by Ellman's method. The greater force of detachment of polymer compacts of modified gum from the mucin discs as compared to native gum indicates its enhanced mucoadhesive potential. The thiolated Moringa gum was formulated into buccal tablets using metronidazole benzoate as the test drug. A comparative evaluation of buccal tablets revealed 1.5-fold higher ex vivo bioadhesion time of buccal tablets of modified gum than the native gum. The results of in vitro release studies showed that modified gum tablets provided a sustained release of metronidazole over 24 h of the study following First-order kinetics with diffusion mechanism of release.

摘要

在本研究中,通过与巯基乙酸酯化来对辣木胶进行硫醇化修饰,以增强其黏膜黏附潜力。通过傅里叶变换红外光谱(FT-IR)、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-能谱分析(SEM-EDX)对硫醇化辣木胶进行了表征。通过 Ellman 法测定,改性胶的巯基含量为 0.956±0.024mM。与天然胶相比,改性胶聚合物压片从黏蛋白盘上的分离力更大,表明其黏膜黏附潜力增强。将硫醇化辣木胶制成依托硝唑苯甲酸的颊片剂。对颊片剂的比较评估表明,与天然胶相比,改性胶颊片剂的体外生物黏附时间延长了 1.5 倍。体外释放研究结果表明,改性胶片剂在研究的 24 小时内,按照一级动力学和释放的扩散机制,提供了依托硝唑的持续释放。

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