Enhanced dissolution and physical stability of cefdinir via mesoporous silica (SBA-15) inclusion: A novel approach for BCS Class IV drugs

Title : Enhanced dissolution and physical stability of cefdinir via mesoporous silica (SBA-15) inclusion: A novel approach for BCS Class IV drugs

Abstract:

Cefdinir, a BCS class IV cephalosporin antibiotic, suffers from poor oral bioavailability due to its low solubility and permeability. This study aimed to improve the dissolution rate and physical stability of cefdinir by incorporating it into mesoporous silica SBA-15 using the solvent immersion method. Multiple solvents were evaluated for optimal drug loading, with n-hexane demonstrating the highest loading efficiency (37%) due to its non-polar nature, minimizing competitive interactions with silica surfaces. The optimized formulation (F3) was comprehensively characterized using Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), and Scanning Electron Microscopy (SEM). Characterization confirmed the transformation of cefdinir into an amorphous state and the formation of stabilizing hydrogen bonds with the silica matrix. In vitro dissolution studies conducted at pH 1.2, 4.5, and 6.8 revealed significantly enhanced release profiles for the mesoporous formulation compared to pure crystalline cefdinir. Notably, at pH 1.2, over 65% of cefdinir was released within 5 minutes from the SBA-15 formulation versus 40% from the pure drug. Stability testing under varying temperature and humidity conditions (25?C/0%RH, 40?C/0%RH, and 40?C/75%RH) demonstrated the robust ability of SBA-15 to preserve the amorphous form and prevent recrystallization over six months. Release kinetics were best described by the Weibull model for the loaded formulation across most conditions. This mesoporous silica-based strategy presents a promising approach for improving both dissolution and stability of poorly soluble oral drugs.

Biography:

Prof. Raghad studied Pharmacy at Damascus University, Syria, and completed her Master’s degree in 2015. She then enrolled in the PhD program in Industrial Pharmacy at the Faculty of Pharmacy, Damascus University, where she obtained her PhD degree in 2022. Two years later, she participated in the Erasmus+ UNIMED program as a visiting lecturer at Pavia University, delivering lectures to postgraduate students on solid-state properties, strategies for enhancing drug solubility, and stabilization approaches for amorphous drug forms. She is currently conducting research focused on the development of nanotechnology-based drug delivery systems.