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Melt-extruded formulations of fenofibrate with various grades of hydrogenated phospholipid exhibit promising in-vitro biopharmaceutical behavior. | LitMetric

AI Article Synopsis

  • The study investigates the use of different grades of hydrogenated phospholipids (HPL) as excipients in solid dispersions for the drug fenofibrate (FEN), showing that both binary and ternary blends can enhance the drug's solubility.
  • X-ray diffraction analysis confirmed that ternary blends achieved complete conversion of crystalline FEN to an amorphous state, leading to better drug release compared to binary blends and marketed formulations.
  • Results indicated that the formulations containing higher levels of phosphatidylcholine demonstrated improved drug permeation, suggesting that HPL blends created via hot melt extrusion could be a promising option for formulating poorly water-soluble drugs like FEN.

Article Abstract

In the current study, it was demonstrated that three commercially available grades of hydrogenated phospholipids (HPL) differing in their content of phosphatidylcholine may be used as components for hot melt-extruded binary (HPL as sole excipient) or ternary (in combination with copovidone) solid dispersions of fenofibrate (FEN) at mass fractions between 0.5 and 20% (ternary) or 80% (binary). X-ray powder diffraction indicated complete conversion of crystalline fenofibrate into the amorphous state by hot melt extrusion for all ternary blends. In contrast, both the binary blends (HPL- and copovidone-based) contained minor remaining crystallites. Irrespectively, all solid dispersions induced during dissolution studies a supersaturated state of FEN, where the ternary ASDs showed enhanced and more complete release of FEN as compared to the binary blends and, even more pronounced, in comparison to the marketed micronized and nano-milled formulations. In terms of the cumulated amount permeated, there were marginal differences between the various formulations when combined dissolution/permeation was done using FeSSIF as donor medium; with FaSSIF as donor medium, the binary HPL-ASD containing the grade with the highest phosphatidylcholine fraction performed best in terms of permeation, even significantly better than the marketed nano-crystal formulation. Otherwise, no significant differences were seen between the various grades of HPL when FEN dissolution and permeation were analyzed for ternary solid dispersions. In conclusion, the in-vitro biopharmaceutical behaviour of hydrogenated phospholipid-containing blends manufactured by hot melt extrusion appears promising. They can be a viable formulation option for poorly water-soluble and lipophilic drug compounds like FEN.

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Source
http://dx.doi.org/10.1016/j.ejps.2024.106936DOI Listing

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