Abstract

Mesoporous silica (MS) is a promising material as a drug carrier that is used in pharmaceutical applications. It was discovered that the incorporation of drugs into MS has the potential to improve their dissolution and bioavailability due to the large specific surface area. This study aimed to characterize the drugs with various molecular weights in MS as well as to elucidate their impact on the loading amount and the amorphization within MS. The solvent evaporation method was used to encapsulate itraconazole (ITZ), nifedipine (NIF), and nicotinamide (NIC), respectively, into MS. The result shows the absence of glass transition and the melting peak of ITZ, NIF, and SAC within MS signifying the successful encapsulation. A hallo pattern was found in ITZ and NIF within MS indicating the amorphization. The high molecular weight and the interaction between the drug with the silica surface is reportedly contributed to the formation of the amorphous state. Meanwhile, the characteristic diffraction peaks of NIC crystal were observed for NIC within MS. In conclusion, the molecular weight of the drug has a significant effect on the loading amount and the amorphization of the drug within MS.

Highlights

  • The aqueous solubility of active pharmaceutical ingredient (API) has a strong influence on its bioavailability when orally administrated (Budiman et al, 2021)

  • The resulting powder was dried at 30 C for 48h using a vacuum dryer to obtain ITZ encapsulated into Mesoporous silica (MS) (ITZ/MS), NIF encapsulated into MS (NIF/MS), and NIC encapsulated into MS (NIC/MS)

  • This study clearly explains the characterization of ITZ, NIF, and NIC encapsulated into MS using the solvent evaporation method

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Summary

Introduction

The aqueous solubility of active pharmaceutical ingredient (API) has a strong influence on its bioavailability when orally administrated (Budiman et al, 2021). About 90% of drug candidates, currently under development, possess low aqueous solubility and high hydrophobicity characteristics (Dening and Taylor, 2018). Formulation strategies are required to enhance drug solubility and. Some of the strategies adopted to improve oral bioavailability include the use of additives such as surfactants or complexing agents, salts (Takano et al, 2010), and amorphous solid dispersions (Almeida E Sousa et al, 2016)

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