Evaluation of Extended-release of Piroxicam-loaded Pectin-zein Hydrogel Microspheres: In vitro, Ex vivo, and In vivo Studies

Abstract

Objective: This study evaluated drug delivery systems based on Pectin (P) and Zein (Z) hydrogel microspheres. Piroxicam (Px) loaded P/Z hydrogel microspheres (P/Z HM) were developed, and their extended-release pharmacokinetic properties were evaluated.

Methods: Experiments were executed under three different conditions: in vitro, ex vivo, and in vivo. Then, the in vitro-in vivo correlations (IVIVC) and ex vivo-in vivo correlations (EVIVC) were examined.

Results: Analysis of drug release mechanisms were evaluated by fitting the in vitro data into the Ritger- Peppas equation, showing the contribution of both polymers' relaxation and drug diffusion from the hydrogel microspheres. The fraction absorbed in vivo was determined by the deconvolution of plasma concentration data using the Loo-Riegelman method. After oral single-dose administration of the two formulations, their basic independent model parameters were calculated.

Conclusion: P/Z HM had different drug release behaviors in in vitro and in vivo conditions. However, the ex vivo and in vivo characteristics were similar (R² = 0.99). It seemed reasonable to use the ex vivo method to predict the in vivo drug absorption behavior during the polymeric drug delivery system developmental studies. The P/Z HM formulation maintained the drug dose at the colon site for a long duration and could be applied for delivery of active pharmaceutical and food ingredients to the colon site.

Keywords: IVIVC; Pectin; ex vivo-in vivo correlation; extended-release; piroxicam; zein.