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Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS)

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Abstract

Limited aqueous solubility of exemestane leads to high variability in absorption after oral administration. To improve the solubility and bioavailability of exemestane, the self-microemulsifying drug delivery system (SMEDDS) was developed. SMEDDS comprises of isotropic mixture of natural or synthetic oil, surfactant, and cosurfactant, which, upon dilution with aqueous media, spontaneously form fine o/w microemulsion with less than 100 nm in droplet size. Solubility of exemestane were determined in various vehicles. Ternary phase diagrams were plotted to identify the efficient self-emulsification region. Dilution studies, droplet size, and zeta potential of the formulations were investigated. The release of exemestane from SMEDDS capsules was studied using USP dissolution apparatus in different dissolution media and compared the release of exemestane from a conventional tablet. Oral pharmacokinetic study was performed in female Wistar rats (n = 8) at the dose of 30 mg kg−1. The absorption of exemestane from SMEDDS form resulted in about 2.9-fold increase in bioavailability compared with the suspension. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as exemestane by the oral route.

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Authors and Affiliations

  1. Dabur Research Foundation, Plot No. 22 Site IV, Sahibabad, 201010, Ghaziabad Uttar Pradesh, India

    Ajeet K. Singh, Anshumali Awasthi & Gautam Mishra

  2. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), 110062, New Delhi, India

    Ajeet K. Singh, Akash Chaurasiya, Gautam Mishra & Roop K. Khar

  3. Department of Dermatology, All India Institute of Medical Sciences, 110029, New Delhi, India

    Dinesh Asati

  4. ARA Healthcare Pvt Ltd., Plot No. 10 Electronic City, Sector 18, 122015, Gurgaon, Haryana, India

    Rama Mukherjee

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  1. Ajeet K. Singh
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  2. Akash Chaurasiya
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  4. Gautam Mishra
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Correspondence to Ajeet K. Singh.

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Singh, A.K., Chaurasiya, A., Awasthi, A. et al. Oral Bioavailability Enhancement of Exemestane from Self-Microemulsifying Drug Delivery System (SMEDDS). AAPS PharmSciTech 10, 906–916 (2009). https://doi.org/10.1208/s12249-009-9281-7

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  • DOI: https://doi.org/10.1208/s12249-009-9281-7

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