Fabrication of alginate based microgels for drug-sustained release: In-vitro and in-vivo evaluation

The current study was conducted to evaluate and analyze the effect of alginate, itaconic acid, and N,N '-meth-ylene bisacrylamide in formulation of a novel alginate based microgels for sustained release of theophylline. The fabricated microgels were characterized by PXRD, SEM, FTIR, TGA and DSC respectively. FTIR revealed that alginate reacted with itaconic acid during polymerization reaction and confirmed the overlapping of itaconic acid on the backbone of alginate. TGA and DSC depicted high thermal stability of the fabricated microgels as compared to pure unreacted polymer and monomer. Likewise, dynamic swelling and percent drug release studies were carried out at different pH media i.e., pH 1.2, 4.6 and 7.4 respectively. Greater dynamic swelling and percent drug release was observed at higher pH 7.4 as compared to lower pH 4.6 and 1.2 due to the deproto-nation of COOH groups of both alginate and itaconic acid respectively. The drug release mechanism from the fabricated microgels could be described by first order model. In-vivo pharmacokinetic study was performed on rabbits and exhibited sustained release in rabbits. Hence, the developed microgels indicated higher potential as the delivery system for the sustained delivery of theophylline.

Automated summary

This study evaluated the effect of alginate, itaconic acid, and N,N'-meth-ylene bisacrylamide in fabricating alginate based microgels for sustained release of theophylline. Characterization studies showed high thermal stability of the microgels and pH-dependent drug release mechanism described by a first order model. In vivo pharmacokinetic study in rabbits demonstrated sustained release properties of the developed microgels.