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Covalent polybenzimidazole-based triazine frameworks: A robust carrier for non-steroidal anti-inflammatory drugs

机译:基于共价的聚苯和咪唑的三嗪框架:用于非甾体类抗炎药的强大载体

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摘要

Covalent triazine-based polymers (CTPs) are a new class of porous materials that can be used for the intercalation of therapeutic agents. The main purposes of designing new drug carriers include protecting them from degradation, enhancing their poor aqueous solubility, and investigating their controlled release properties. In this context, a novel polybenzimidazole-based CTP (BZ-CTP) was prepared by a solvothermal reaction between 4,4',4 ''-((1,3,5-triazine-2,4,6-triy1) tris(azanediyl)) tribenzoic acid (TCA) and 3,3'-diaminobenzidine. Piroxicam (PRX) and mefenamic acid (MFA) were loaded thoroughly into the CTP by using ultrasonication to form MFA-loaded CTP (MFA@BZ-CTP) and PRX-loaded CTP (PRX@BZ-CTP) with drug loading efficiencies of 49% and 53%, respectively. We attribute the increased loading efficiencies to the formation of pi-pi stacking forces between the aromatic rings present in the CTP structure and drugs. The in vitro release experiments were assessed in simulated physiological conditions using the dialysis method. Moreover, the release mechanisms were evaluated by Korsmeyer-Peppas kinetic studies and the obtained results showed excellent sustained releases of 81% after 96 h and 87% after 24 h for the PRX@BZ-CTP and MFA@BZ-CTP hybrids, respectively.
机译:基于共价三嗪的聚合物(CTP)是一种新的多孔材料,可用于嵌入治疗剂。设计新药物载体的主要目的包括保护它们免于降解,增强其差的含水溶解度,并研究其控释性能。在这种情况下,通过4,4',4'' - ((1,3,5-三嗪-2,4,6-三毫米1)三((1,3,5-三嗪-2,4,6-Triy1)Tris的溶剂热反应制备基于新的聚苯咪唑基CTP(BZ-CTP) (氮杂噻吩))二苯甲酸(TCA)和3,3'-二氨基苯甲酸。通过使用超声波彻底将吡罗昔康(PRX)和MEFENAMIC酸(MFA)彻底加载到CTP中,以形成MFA加载的CTP(MFA @ BZ-CTP)和PRX负载的CTP(PRX @ BZ-CTP),其中药物负载效率为49 %和53%。我们将增加的加载效率归因于CTP结构和药物中存在的芳环之间的PI-PI堆叠力的形成。使用透析方法评估在模拟的生理条件下进行体外释放实验。此外,通过Korsmeyer-Peppas动力学研究评估了释放机制,并且所得结果分别在PRX @ BZ-CTP和MFA @ BZ-CTP杂种的24小时后显示出优异的81%和87%的优异持续释放。

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