Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients
Research output: Contribution to journal › Journal article › Research › peer-review
Standard
Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients. / Ogadah, Chiazor Ugo; Mrštná, Kristýna; Matysová, Ludmila; Müllertz, Anette; Rades, Thomas; Niederquell, Andreas; Šklubalová, Zdenka; Vraníková, Barbora.
In: International Journal of Pharmaceutics, Vol. 650, 123702, 2024.Research output: Contribution to journal › Journal article › Research › peer-review
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients
AU - Ogadah, Chiazor Ugo
AU - Mrštná, Kristýna
AU - Matysová, Ludmila
AU - Müllertz, Anette
AU - Rades, Thomas
AU - Niederquell, Andreas
AU - Šklubalová, Zdenka
AU - Vraníková, Barbora
N1 - Publisher Copyright: Copyright © 2023 Elsevier B.V. All rights reserved.
PY - 2024
Y1 - 2024
N2 - 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.
AB - 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.
KW - Co-milling
KW - Cyclosporine A
KW - Drug loading
KW - Liquisolid systems
KW - Mesoporous carrier
U2 - 10.1016/j.ijpharm.2023.123702
DO - 10.1016/j.ijpharm.2023.123702
M3 - Journal article
C2 - 38086492
AN - SCOPUS:85181845443
VL - 650
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
M1 - 123702
ER -
ID: 380200940