Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients

Type
01A - Journal article
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Parent work
International Journal of Pharmaceutics
Special issue
DOI of the original publication
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Series
Series number
Volume
650
Issue / Number
Pages / Duration
123702
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Publisher / Publishing institution
Elsevier
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Abstract
Drug loading into mesoporous carriers may help to improve the dissolution of poorly aqueous-soluble drugs. However, both preparation method and carrier properties influence loading efficiency and drug release. Accordingly, this study aimed to compare two preparation methods: formulation into liquisolid systems (LSS) and co-milling for their efficiency in loading the poorly soluble model drug cyclosporine A (CyA) into mesoporous magnesium aluminometasilicate Neusilin® US2 (NEU) or functionalized calcium carbonate (FCC). Scanning electron microscopy was used to visualize the morphology of the samples and evaluate the changes that occurred during the drug loading process. The solid-state characteristics and physical stability of the formulations, prepared at different drug concentrations, were determined using X-ray powder diffraction. In vitro release of the drug was evaluated in biorelevant media simulating intestinal fluid. The obtained results revealed improved drug release profiles of the formulations when compared to the milled (amorphous) CyA alone. The dissolution of CyA from LSS was faster in comparison to the co-milled formulations. Higher drug release was achieved from NEU than FCC formulations presumably due to the higher pore volume and larger surface area of NEU.
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ISBN
ISSN
0378-5173
1873-3476
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
Open access category
Closed
License
Citation
Ogadah, C. U., Mrštná, K., Matysová, L., Müllertz, A., Rades, T., Niederquell, A., Šklubalová, Z., & Vraníková, B. (2024). Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients. International Journal of Pharmaceutics, 650, 123702. https://doi.org/10.1016/j.ijpharm.2023.123702