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

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. Key finding: The oxidative coupling assembly of quercetin resulted in microspheres of 10-20µm 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.

Oxidative Coupling and Self-Assembly of Polyphenols for the Development of Novel Biomaterials

“…These microspheres were loaded with diclofenac sodium in the space of the microspheres. 15 The quercetin microspheres loaded with diclofenac showed in vivo gastrosparing anti-inflammatory activity better than diclofenac sodium in rodents.…”

“…The nucleophilic addition involving a quinone is responsible for inter-flavan oligo/polyphenol successive coupling and formation. In this reaction, the formation of microparticles is mediated through quinone or semiquinone, and Cu 2+ acts as a catalyst in this process . The formation of oligomeric/polymeric polyphenols takes place with the reduction of temperature and the aggregation into spherical precipitates via noncovalent interaction.…”

“…Recently, we have synthesized quercetin microspheres using oxidative coupling assembly in the presence of Cu 2+ . These microspheres were loaded with diclofenac sodium in the space of the microspheres . The quercetin microspheres loaded with diclofenac showed in vivo gastrosparing anti-inflammatory activity better than diclofenac sodium in rodents.…”

“…In this reaction, the formation of microparticles is mediated through quinone or semiquinone, and Cu 2+ acts as a catalyst in this process. 15 The formation of oligomeric/polymeric polyphenols takes place with the reduction of temperature and the aggregation into spherical precipitates via noncovalent interaction. These polymeric polyphenols can be biodegraded by a thiolysis reaction and can be easily cleaved in the presence of glutathione (GSH).…”