Comparison of the liquisolid technique and co-milling for loading of a poorly soluble drug in inorganic porous excipients
Jazyk angličtina Země Nizozemsko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
38086492
DOI
10.1016/j.ijpharm.2023.123702
PII: S0378-5173(23)01124-9
Knihovny.cz E-zdroje
- Klíčová slova
- Co-milling, Cyclosporine A, Drug loading, Liquisolid systems, Mesoporous carrier,
- MeSH
- difrakce rentgenového záření MeSH
- pomocné látky * MeSH
- poréznost MeSH
- rozpustnost MeSH
- voda * MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- pomocné látky * MeSH
- voda * 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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