Research on Ternary Solid Dispersions of Celecoxib with Surfactant: Preparation, Characterization, and Solubility Property

Celecoxib (CXB) is a nonsteroidal anti-inflammatory drug (NSAID). However, the application of CXB has been compromised by its poor aqueous solubility and low oral bioavailability. We developed a series of ternary solid dispersions (SDs) of CXB to increase its solubility. In this study, the polymers were screened to determine that they have the potential to increase the solubility of CXB in the solution. A hydrophilic polymer-hydroxypropyl methylcellulose (HPMC) and a surfactant Tween80 were employed as matrix respectively in the optimized formulations. Experimental data revealed that CXB was molecularly distributed within all dispersions in amorphous form by using Differential Scanning Calorimetry (DSC), Polarizing Light Microscopy (PLM), and X-ray powder diffraction (XRD). Fourier Transform Infrared Spectroscopy (FTIR) results showed that the characteristic peaks of CXB have shifted. Compared with pure CXB, the addition of excipients can reduce the contact angle, and improve the solubility of CXB. Ternary SDs were dissolved in PBS (pH 6.8) and formed drug-carrying nanoparticles. In vitro dissolution results indicated that the dissolution amount of HPMC-CXB 5 : 1 SD (32.08±1.56% for 120 min) was higher than pure CXB (3.09±0.29%). In particular, the greatest dissolution enhancement was obtained from the test of which the result was HPMC/Tween80-CXB 3 : 2 : 1 SD (44.12±2.01% for 120 min). This study showed that ternary SDs could be a promising strategy for improving CXB dissolution.