Co-carrier-based solid dispersion of celecoxib improves dissolution rate and oral bioavailability in rats

Abstract

This study aimed to prepare a co-carrier-based solid dispersion (SD) of celecoxib (CXB) to improve its dissolution and oral bioavailability. The CXB-loaded SD formulation was prepared using CXB, pol407, Aerosil 200, and Eudragit L100 at a weight ratio of 1:3:1.5:1. PXRD, DSC, and FTIR analyses were conducted to evaluate the structural behavior and interactions between the drug and carrier. The dissolution profile was studied to demonstrate superior CXB dissolution capacity of CXB-SD than that of the physical mixture and raw CXB, and the results showed that the dissolution efficiency (%) of optimized CXB-SD significantly (P < 0.05) increased compared to that of raw CXB. The mean dissolution times of CXB-SD at pH 1.2 and 6.8 were reduced by 2.4-fold and 2.5-fold, respectively, compared to that of raw CXB. The dissolution of CXB-SD fitted well with the zero-order model. The preparation of the CXB-SD formulation improved the bioavailability of CXB, as demonstrated by the increased AUClast (1.88-fold) and Cmax (2.24-fold) of CXB-SD compared to that of raw CXB. In conclusion, these results indicate that SDs can enhance the dissolution and oral bioavailability of poorly water-soluble CXB.