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

Chiazor Ugo Ogadah*, Kristýna Mrštná*, Ludmila Matysová*, Anette Müllertz*, Thomas Rades*, Andreas Niederquell*, Zdenka Šklubalová*, Barbora Vraníková*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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.

Original languageEnglish
Article number123702
JournalInternational Journal of Pharmaceutics
Volume650
Number of pages10
ISSN0378-5173
DOIs
Publication statusPublished - 2024

Bibliographical note

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Keywords

  • Co-milling
  • Cyclosporine A
  • Drug loading
  • Liquisolid systems
  • Mesoporous carrier

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