Design and Optimization of Quercetin-Loaded Polymeric Eudragit L-100 Nanoparticles for Anti-diabetic Activity with Improved Oral Delivery: In-Vitro and In-Vivo Evaluation

To design and develop a nanoformulation from isolated quercetin (QT) from the Annona reticulata Linn leaves to enhance therapeutic index, solubility, bioavailability, toxicity mitigation, pharmacological activity improvement, and prevention of physical and chemical degradation of antidiabetic lead compounds. Bio-flavonoids are gaining popularity in diabetes and other therapeutic research due to their various pharmacological and biological effects. QT is one of several beneficial flavonoids, has amazing hypoglycemic effects, with significant improvement, stabilization of long-term insulin secretion, and regeneration of human islets in the pancreas without causing severe health risks. However, poor solubility, biological milieu instability, limited permeation, short biological half-life, and low bioavailability prevent its widespread use in anti-diabetic research. This novel approach of polymeric nanoformulation of QT will improve the bioavailability and enhance its antidiabetic activity. The effectiveness of QT-loaded Eudragit L-100 (EDL) nanoparticles (NPs) against hyperglycemia in streptozotocin-induced type 2 diabetic rats was investigated in this work. QT/EDLNPs were designed by Box-Behnken Design and prepared by a sonication-assisted emulsification solvent evaporation process. The optimized QT/EDLNPs formulation was administered orally for 21 days to streptozotocin-induced diabetic rats. The QT/EDLNPs demonstrated significant antidiabetic effects comparable to the currently available anti-diabetic drug Glibenclamide. Thus, the approach provides an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. These findings suggest that QT/EDLNPs is an effective oral medicine for diabetes management with a lower dose and dosing frequency that is also patient compliant. This study also investigates a fantastic alternative method for creating brand-new polymeric NPs that serve as bioactive compound delivery systems.Journal instruction requires a city for affiliations; however, these are missing in affiliation 2. Please verify if the provided city is correct and amend if necessary.City for affiliation 2 is Dibrugarh.It is correctPlease confirm if the author names are presented accurately and in the correct sequence (given name, middle name/initial, family name). Author Given name: [Mohammad Zaki], Last name [Ahmad], Given name: [Ratna Jyoti], Last name [Das].The author names are presented accurately.It is confirmed

Automated summary

This study aimed to design and develop a nanoformulation using isolated quercetin from Annona reticulata Linn leaves to improve therapeutic index, solubility, bioavailability, toxicity mitigation, pharmacological activity, and prevention of degradation of antidiabetic compounds. Quercetin has hypoglycemic effects but its poor solubility and low bioavailability limit its use. The polymeric nanoformulation of quercetin was found to enhance its antidiabetic activity. The optimized formulation demonstrated significant antidiabetic effects, making it an effective oral medicine for diabetes management. Rating: 9 out of 10.