基于淀粉糖的非那根酸类非甾体抗炎药酯原药的合成和释放研究。

IF 3 Q2 PHARMACOLOGY & PHARMACY Therapeutic delivery Pub Date : 2024-01-01 Epub Date: 2024-09-17 DOI:10.1080/20415990.2024.2400041
Shraddha Chugh, Mousmee Sharma, Garima Chandrasen, Harish Mudila, Parteek Prasher
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引用次数: 0

摘要

材料与方法:通过酯联淀粉原药实现甲灭酸的结肠靶向释放:通过 1H NMR 和 IR 光谱对原药进行表征。在富含酶的模拟生理介质中,通过紫外可见光谱对药物的活化和释放曲线进行了研究,并通过高效液相色谱分析进行了验证。酶联免疫吸附试验(ELISA)用于评估不同浓度的原药与酯和/或淀粉水解酶预孵育时对 COX-1 和 COX-2 的抑制率。扫描电镜研究进一步验证了原药在模拟生理条件下的性能:结果:胰蛋白酶是 SIM 中原药活化的关键,它使原药中的酯键容易被酯酶水解。这一证据通过药物释放研究、高效液相色谱分析、酶联免疫吸附试验和扫描电镜研究得到了证实,在这些研究中,酯结合原药在生理介质中表现出明显的稳定性,只有在淀粉降解酶存在时才会被激活:结论:酯类连接的淀粉-甲灭酸共轭物在 SIM 中表现出酶反应性激活和释放。
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Synthesis and release studies on amylose-based ester prodrugs of fenamic acid NSAIDs.

Aim: To achieve colon-targeted release of mefenamic acid from its ester-linked amylose prodrugs.Materials & methods: The prodrug was characterized by 1H NMR and IR spectroscopy. Drug activation and release profile was studied in enzyme enriched simulated physiological media via UV-vis spectroscopy and was validated with HPLC analysis. ELISA assay was employed for evaluating the % inhibition of COX-1 and COX-2 inhibition at different concentrations of the prodrug preincubated with ester and/ or amylose hydrolyzing enzymes. SEM studies further validated the performance of the prodrug under simulated physiological conditions.Results: Pancreatin was essential for the prodrug activation in SIM to make the ester bonds in prodrug vulnerable to hydrolysis by esterase. This evidence was confirmed by drug release studies, HPLC analysis, ELISA assay and SEM investigation where the ester conjugated prodrug showed marked stability in physiological media only to get activated in the presence of amylose degrading enzyme.Conclusion: Ester linked amylose-mefenamic acid conjugate showed both enzyme responsive activation and release in SIM.

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来源期刊
Therapeutic delivery
Therapeutic delivery PHARMACOLOGY & PHARMACY-
CiteScore
5.50
自引率
0.00%
发文量
25
期刊介绍: Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.
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