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Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect

Archives of Pharmacal Research volume 38, pages 1850–1856 (2015)Cite this article

Abstract

Megestrol acetate (MGA) belongs to the BCS class II drugs with low solubility and high permeability, and its oral absorption in conventional dosage form MGA microcrystal suspension (MGA MS) is very limited and greatly affected by food. In this study, MGA nanoemulsion (MGA NE) was formulated based on solubility, phase-diagram and release studies. Then oral bioavailability of MGA NE and MGA MS was evaluated. A randomized two-way crossover trial was conducted on six male dogs under fed and fasting conditions. Blood concentrations of MGA were analyzed using LC–MS/MS. MGA NE yielded 5.00-fold higher oral bioavailability in fasting conditions and displayed more stable absorption profiles after food intake compared with MGA MS.

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Acknowledgments

This work was supported by INHA UNIVERSITY Research Grant.

Conflict of interest

The authors declare that they have no conflicts of interest to disclose.

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    Affiliations

    1. Department of New Drug Development and NCEED, School of Medicine, Inha University, Incheon, 400-712, South Korea

      Yixian Li, Chung Kil Song, Min-Kyoung Kim, Hyosang Lim, Qingbo Shen & Su-Geun Yang

    2. Division of Gastroenterology & Hepatology, Inha University Hospital, Incheon, 400-712, South Korea

      Don Haeng Lee

    Authors
    1. Yixian Li
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    2. Chung Kil Song
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    3. Min-Kyoung Kim
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    4. Hyosang Lim
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    5. Qingbo Shen
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    7. Su-Geun Yang
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    Corresponding author

    Correspondence to Su-Geun Yang.

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    Yixian Li and Chung Kil Song have equally contributed to this paper.

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    Cite this article

    Li, Y., Song, C.K., Kim, MK. et al. Nanomemulsion of megestrol acetate for improved oral bioavailability and reduced food effect. Arch. Pharm. Res. 38, 1850–1856 (2015). https://doi.org/10.1007/s12272-015-0604-9

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    • DOI: https://doi.org/10.1007/s12272-015-0604-9

    Keywords

    • Megestrol acetate
    • Nanoemulsion
    • Food-effect
    • BCS class II drugs
    • Oral bioavailability