The impact of drug-loading factors on the solid-state form of ritonavir-mesoporous silica systems

Abstract

Among the formulation techniques used to enhance the solubility and dissolution rate of poorly, aqueous-soluble drugs, mesoporous silica drug delivery systems have shown promise. A range of processes are employed to load drugs onto silica and solvent-based approaches are widely employed. This study aims to understand the influence of drug concentration insolvent and drug-silica ratio on drug solid-state form and amorphization within silica. Ritonavir which belongs to  BCS Class II was used as a model drug. Ritonavir was loaded into Syloid®244FP using a solvent evaporation method. Ritonavir loading percentage was calculated based on the assumption that the entire specific surface area of silica is exposed and available for drug adsorption. Ethanol solutions with 3 different ritonavir concentrations; 70%, 32% and 20% saturated solubility at 25°C were employed. Ritonavir was loaded into silica at 1:1, 1:2and 1:3 ritonavir: silica ratios. All systems included ritonavir loaded beyond monolayer surface coverage. Ritonavir- Syloid®244 FP formulations were characterised using DSC, PXRD, FT-IR, and TGA. The results showed that all ritonavir-Syloid®244 FP systems prepared contained ritonavir in a non-crystalline state.

Keywords

mesoporous silica, Ritonavir, Solid-state

How to Cite

Al-Dagamin, T., O'Shea, J. P. & Crean, A., (2022) “The impact of drug-loading factors on the solid-state form of ritonavir-mesoporous silica systems”, British Journal of Pharmacy 7(2). doi: https://doi.org/10.5920/bjpharm.1150

Funding

  • Science Foundation Ireland
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Tanweer Al-Dagamin (University College Cork)
Joseph P O'Shea (University College Cork)
Abina Crean (University College Cork)

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Creative Commons Attribution 4.0

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This article has been peer reviewed.

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