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Background <p>The low oral bioavailability of poorly water-soluble drugs poses a challenge during drug development. Fenofibrate has low aqueous solubility and poor oral absorption. The aim of the present work was to develop proliposome formulations of fenofibrate using lipid hydration and lyophilization techniques. The proliposome formulation was optimized by applying a 3<sup>2</sup> full factorial design by selecting the concentrations of phosphatidylcholine and cholesterol as independent variables and percent entrapment efficiency as the response variable. Tablet and capsule formulations of proliposomes were developed and compared with fenofibrate nanoparticulate tablets prepared by milling.</p> Results <p>The homogenized liposomal dispersion formulation (T8) and nanoparticulate tablet had final average median particle sizes (D50) of 151&#xa0;nm, 148&#xa0;nm and 224&#xa0;nm, respectively. There was significantly less drug release from the proliposome formulations than from the nanoparticulate tablet, which exhibited complete drug release in 60&#xa0;min. A pharmacokinetic study revealed that the proliposome-containing capsule formulation (T8-C) had greater bioavailability than did the proliposome tablet and nanoparticulate tablet.</p> Conclusion <p>The proliposome formulation was stable and could be developed into a solid dosage form, such as capsules, tablets, or powders, for oral suspension. Additionally, the proliposome formulation demonstrated greater absorption than the nanoparticulate fenofibrate tablet developed using wet milling/grinding technology.</p>

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Exploring proliposome-embedded solid fenofibrate formulations: a comparative study with nanoparticulate tablets to enhance oral absorption

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年12月28日

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  • Sachin Salampure,
  • Swaroop R. Lahoti

摘要

Background

The low oral bioavailability of poorly water-soluble drugs poses a challenge during drug development. Fenofibrate has low aqueous solubility and poor oral absorption. The aim of the present work was to develop proliposome formulations of fenofibrate using lipid hydration and lyophilization techniques. The proliposome formulation was optimized by applying a 32 full factorial design by selecting the concentrations of phosphatidylcholine and cholesterol as independent variables and percent entrapment efficiency as the response variable. Tablet and capsule formulations of proliposomes were developed and compared with fenofibrate nanoparticulate tablets prepared by milling.

Results

The homogenized liposomal dispersion formulation (T8) and nanoparticulate tablet had final average median particle sizes (D50) of 151 nm, 148 nm and 224 nm, respectively. There was significantly less drug release from the proliposome formulations than from the nanoparticulate tablet, which exhibited complete drug release in 60 min. A pharmacokinetic study revealed that the proliposome-containing capsule formulation (T8-C) had greater bioavailability than did the proliposome tablet and nanoparticulate tablet.

Conclusion

The proliposome formulation was stable and could be developed into a solid dosage form, such as capsules, tablets, or powders, for oral suspension. Additionally, the proliposome formulation demonstrated greater absorption than the nanoparticulate fenofibrate tablet developed using wet milling/grinding technology.