AAPS PharmSciTech

, Volume 10, Issue 3, pp 906–916

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

  • Ajeet K. Singh
  • Akash Chaurasiya
  • Anshumali Awasthi
  • Gautam Mishra
  • Dinesh Asati
  • Roop K. Khar
  • Rama Mukherjee
Research Article

DOI: 10.1208/s12249-009-9281-7

Cite this article as:
Singh, A.K., Chaurasiya, A., Awasthi, A. et al. AAPS PharmSciTech (2009) 10: 906. doi:10.1208/s12249-009-9281-7

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.

Key words

bioavailability enhancementexemestanemicroemulsionSMEDDS

Copyright information

© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  • Ajeet K. Singh
    • 1
    • 2
  • Akash Chaurasiya
    • 2
  • Anshumali Awasthi
    • 1
  • Gautam Mishra
    • 1
    • 2
  • Dinesh Asati
    • 3
  • Roop K. Khar
    • 2
  • Rama Mukherjee
    • 4
  1. 1.Dabur Research FoundationSahibabadIndia
  2. 2.Department of Pharmaceutics, Faculty of PharmacyJamia Hamdard (Hamdard University)New DelhiIndia
  3. 3.Department of DermatologyAll India Institute of Medical SciencesNew DelhiIndia
  4. 4.ARA Healthcare Pvt Ltd.GurgaonIndia