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

Int J Biol Macromol. 2021 Dec 1:192:958-966. doi: 10.1016/j.ijbiomac.2021.10.054. Epub 2021 Oct 14.

Abstract

The current study was conducted to evaluate and analyze the effect of alginate, itaconic acid, and N,N'-methylene 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 deprotonation 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.

Keywords: Alginate; Microgels; Pharmacokinetic study.

MeSH terms

  • Alginates / chemistry*
  • Animals
  • Chemical Phenomena
  • Chromatography, High Pressure Liquid
  • Delayed-Action Preparations
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Drug Delivery Systems*
  • Drug Liberation
  • Kinetics
  • Male
  • Microgels / chemistry*
  • Molecular Structure
  • Polymers
  • Rabbits
  • Spectrum Analysis
  • Thermogravimetry

Substances

  • Alginates
  • Delayed-Action Preparations
  • Drug Carriers
  • Microgels
  • Polymers