Oxidative Coupling Assembly Induced Bio-engineered Quercetin Microspheres for the Gastrosparing Delivery of Diclofenac Sodium.

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY Current drug delivery Pub Date : 2024-01-01 DOI:10.2174/1567201820666230308100040

Vishal Sharma, Girdhari Lal Gupta, Manu Sharma

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Abstract

Objective: The study aimed to develop microspheres of quercetin by oxidative coupling assembly and these microspheres were used to deliver diclofenac sodium without causing gastrotoxicity.

Methods: The oxidative coupling assembly of quercetin was carried out in the presence of copper sulfate to yield quercetin microspheres. The microsphere of quercetin was loaded with diclofenac sodium (QP-Diclo). The carrageenan induced paw edema in rats was used for anti-inflammatory action was studied by using and acetic acid-induced writhing in mice was used to study the analgesic potential of the QP loaded microspheres. The ulcerogenecity and gastrotoxicity comparison was made between diclofenac and QP-Diclo.

Results: The oxidative coupling assembly of quercetin resulted in microspheres of 10-20 μm in size, which were loaded with diclofenac sodium (QP-Diclo). The marked anti-inflammatory activity was observed by QP-Diclo treatment using carrageenan induced paw edema (in rats) and better analgesic activity than diclofenac sodium in mice. The administration of QP-Diclo significantly elevated the diminished overall nitrite/nitrate extent and thiobarbituric acid reactive and significantly increased the diminished superoxide dismutase activity in comparison to diclofenac sodium in gastric mucosa.

Conclusion: The results suggested that dietary polyphenol quercetin can be converted to microspheres by oxidative coupling assembly and can be used to deliver diclofenac sodium without causing gastrotoxicity.

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氧化偶联组装诱导的生物工程槲皮素微球用于双氯芬酸钠的胃保护递送。

目的:通过氧化偶联组装法制备槲皮素微球，制备的槲皮素微球可用于双氯芬酸钠的递送，且无胃毒性。方法:在硫酸铜存在下，对槲皮素进行氧化偶联组装，得到槲皮素微球。用双氯芬酸钠(QP-Diclo)负载槲皮素微球。以卡拉胶致大鼠足跖水肿为研究对象，以醋酸致小鼠扭体为研究对象。比较双氯芬酸与qp -双氯芬酸的溃疡性和胃毒性。结果:槲皮素的氧化偶联组装得到了10 ~ 20 μm大小的微球，并负载双氯芬酸钠(QP-Diclo)。用卡拉胶诱导大鼠足跖水肿的QP-Diclo治疗后，其抗炎活性显著，镇痛活性优于双氯芬酸钠。与双氯芬酸钠相比，QP-Diclo显著提高了胃粘膜亚硝酸盐/硝酸盐总体降低程度和硫代巴比妥酸活性，显著提高了胃粘膜超氧化物歧化酶活性。结论:膳食多酚槲皮素可通过氧化偶联组装转化为微球，可用于递送双氯芬酸钠而不引起胃毒性。

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来源期刊

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.