Development and statistical optimization of alginate-Neusilin US2 micro-composite beads to elicit gastric stability and sustained action of hesperidin

The Alginate-Neusilin US2 micro-composite (MC) beads were fabricated and optimized for oral delivery of hesperidin (HES). A 3(2) full factorial design encompassing independent variables (factors) such as the concentration of sodiumalginate (X-1), and Neusilin US2 (X-2) and dependant variables (response) such as particle size (Y-1), entrapment efficiency (Y-2), and swelling degree (Y-3). Nine batcheswere prepared by formulation designemploying statistical software JMP 13.2.1. The multiple regression analysis (MLRA) was carried to explore the influence of factor over responses. Further, a prediction profiler was used to trace the optimum concentration of factors based on desirable responses. The optimized beads (OF) were characterized for their morphology and size by moticmicroscopy and scanning electron microscopy. In vitro release, kinetic studieswere performed in simulated gastric and intestinal fluids. In vivo pharmacokinetic studies revealed better absorption of HES from optimized beads (OF) compared to HES suspension which could be due to the prevention of acidic degradation of HES in the stomach. The estimated shelf life of OF formulation was found to be 3.86 years suggested better stability after fabrication. In a nutshell, the developed micro-composite beads of HES could be a better alternative for promising oral sustained delivery of HES. (C) 2021 Elsevier B.V. All rights reserved.

Automated summary

The study fabricated and optimized Alginate-Neusilin US2 micro-composite beads for oral delivery of hesperidin. Through experimental designs and analyses, the characteristics, release kinetics, and pharmacokinetics of the optimized beads were determined. The results suggest that the optimized beads could be a promising alternative for sustained oral delivery of hesperidin.