Hydrogenated phospholipid, a promising excipient in amorphous solid dispersions of fenofibrate for oral delivery: Preparation and in-vitro biopharmaceutical characterization

Mikołaj Czajkowski, Ann Christin Jacobsen, Annette Bauer-Brandl, Martin Brandl, Paulina Skupin-Mrugalska*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

Amorphous solid dispersions (ASD) represent a viable formulation strategy to improve dissolution and bioavailability of poorly soluble drugs. Our study aimed to evaluate the feasibility and potential role of hydrogenated phospholipid (HPL) as a matrix material and solubilizing additive for binary (alone) or ternary (in combination with polymers) solid dispersions, using fenofibrate (FEN) as the model drug. FEN, incorporated within ASDs by melting or freeze-drying (up to 20% m/m), stayed amorphous during short-term stability studies. The solubility enhancing potential of HPL depended on the dissolution medium. In terms of enhancing in vitro permeation, solid dispersions with HPL were found equally or slightly more potent as compared to the polymer-based ASD. For studied ASD, in vitro permeation was found substantially enhanced as compared to a suspension of crystalline FEN and at least equal compared to marketed formulations under comparable conditions (literature data). Additionally, while the permeation of neat FEN and FEN in binary solid dispersions was affected by the dissolution medium (i.e., the “prandial state”), for ternary solid dispersions the permeation was independent of the “prandial state” (FaSSIF = FeSSIF). This suggests that ternary solid dispersions containing both polymer and HPL may represent a viable formulation strategy to mitigate fenofibrate's food effect.

Original languageEnglish
Article number123294
JournalInternational Journal of Pharmaceutics
Volume644
ISSN0378-5173
DOIs
Publication statusPublished - 25. Sept 2023

Keywords

  • Amorphous solid dispersions
  • Enabling formulations
  • Fenofibrate
  • Hydrogenated phospholipids
  • Polymers
  • Supersaturation

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