Enhanced dissolution of valsartan-vanillin binary co-amorphous system loaded in mesoporous silica particles

Abstract

The study was aimed to prepare a co-amorphous system of valsartan (VAL) with vanillin (VAN) for improving its solubility and dissolution followed by its confinement in mesoporous silica particles (MSPs) to stabilise the co-amorphous system and prevent its recrystallization. Amorphous VAL and VAN were obtained through quench-cooling and VAL/VAN binary co-amorphous system (VAL/VAN-CAS) was prepared through solvent evaporation technique. The particle size and morphology of VAL/VAN-CAS-MSPs were studied using scanning electron microscopy (SEM) and solid-state characterisation was performed by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). The in vitro dissolution was investigated by dialysis bag diffusion method. SEM analysis revealed irregular shaped VAL/VAN-CAS-MSPs with a size range of 5–25 μm, while outcomes of DSC and XRPD confirmed the formation of VAL/VAN-CAS. The in vitro dissolution profiles demonstrated a significantly increased dissolution in first 60 minutes from VAL/VAN-CAS (∼68%) and VAL/VAN-CAS-MSPs (∼76%) compared to powder VAL (∼25%).

Keywords:

• Valsartan
• vanillin
• co-amorphous system
• mesoporous silica particles
• dissolution

Acknowledgements

We are grateful to Shaigan Pharmaceuticals Pvt. Ltd. Islamabad and National University of Science and Technology, Islamabad for providing drug sample and testing facilities, respectively.

Disclosure

The authors report no conflict of interest in this work.

Additional information

Funding

This work was partially supported by Riphah Academy of Research and Education through the seed money grant programme of Riphah International University.