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Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients
CU. Ogadah, K. Mrštná, L. Matysová, A. Müllertz, T. Rades, A. Niederquell, Z. Šklubalová, B. Vraníková
Language English Country Netherlands
Document type Journal Article
- MeSH
- X-Ray Diffraction MeSH
- Excipients * MeSH
- Porosity MeSH
- Solubility MeSH
- Water * MeSH
- Publication type
- Journal Article MeSH
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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- $a Ogadah, Chiazor Ugo $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: ogadahc@faf.cuni.cz
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- $a Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients / $c CU. Ogadah, K. Mrštná, L. Matysová, A. Müllertz, T. Rades, A. Niederquell, Z. Šklubalová, B. Vraníková
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- $a 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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- $a Mrštná, Kristýna $u Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; Department of Clinical Biochemistry and Diagnostics, University Hospital Hradec Králové, Sokolská 581, 50005 Hradec Králové, Czech Republic. Electronic address: arnoltok@faf.cuni.cz
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- $a Matysová, Ludmila $u Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: matysova@faf.cuni.cz
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- $a Müllertz, Anette $u Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen, Denmark. Electronic address: anette.mullertz@sund.ku.dk
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- $a Rades, Thomas $u Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen, Denmark. Electronic address: thomas.rades@sund.ku.dk
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- $a Niederquell, Andreas $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; Institute of Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences, Klingelbergstr. 50, 4056 Basel, Switzerland. Electronic address: andreas.niederquell@fhnw.ch
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- $a Šklubalová, Zdenka $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: sklubalova@faf.cuni.cz
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- $a Vraníková, Barbora $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: vranikovab@faf.cuni.cz
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