Development of omega-3 phospholipid-based solid dispersion of fenofibrate for the enhancement of oral bioavailability

Liang Yang, Yating Shao, Hyo Kyung Han

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

Abstract This research aimed to develop the omega-3 phospholipids based solid dispersion to improve the oral bioavailability of fenofibrate. The omega-3 phospholipids based solid dispersion formulation (OPSD) was prepared by an antisolvent precipitation with immediate freeze-drying and the optimal composition of the formulation was determined as the ratios of sucrose to krill oil of 5:1 (w/w), krill oil to fenofibrate of 1.5:1 (w/w), and antisolvent to solvent of 6:4 (v/v). The developed OPSD formulation was characterized by using scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC), which indicated the crystalline state of fenofibrate in the OPSD. The drug release profiles were also examined at different pHs. The OPSD achieved almost complete dissolution within 15 min, while the untreated powder and physical mixture exhibited minimal dissolution (less than 10% even after 2 h). Furthermore, this formulation effectively increased the oral drug exposure in rats, as the Cmax and AUC of fenofibric acid (an active metabolite) were enhanced by approximately 6-7 folds. These results suggest that the OPSD formulation should be promising for improving the oral bioavailability of fenofibrate.

Original languageEnglish
Article number3317
Pages (from-to)103-110
Number of pages8
JournalEuropean Journal of Pharmaceutical Sciences
Volume78
DOIs
StatePublished - 17 Jul 2015

Keywords

  • Antisolvent
  • Bioavailability
  • Dissolution
  • Fenofibrate
  • Omega-3 phospholipids

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