Lipid-based dispersions of exemestane for improved dissolution rate and intestinal permeability: in vitro and ex vivo characterization

Abstract

Current study aimed to develop lipid dispersions of poorly water soluble exemestane by employing lipid carriers such as Gelucire 44/14 and TPGS with porous calcium silicate (PCS) as an adsorbent carrier and formulate into a solid dosage form. The lipid dispersions at 1:5 ratio showed the highest solubility and dissolution compared to pure exemestane. Further, the ex vivo intestinal permeation studies showed improved apparent permeability (P_app, cm/s) of exemestane from the lipid dispersions (GLD_1:5 1.3 × 10⁻²cm/s; TLD_1:5 1.8 × 10⁻²cm/s) compared to pure exemestane (0.7 × 10⁻²cm/s). The optimized lipid dispersions (GLD_1:5 and TLD_1:5) were evaluated for scalability to develop into capsules.

Keywords:

• Dissolution
• exemestane
• Gelucire 44/14
• lipid dispersions
• permeability
• vitamin E TPGS

Acknowledgements

The authors are grateful to Dr. Reddy’s Laboratories, Hyderabad, India, for the gift sample of exemestane, Gattefosse and Isochem France for providing lipid carriers Gelucire 44/14 and vitamin E TPGS. The authors also thank Mr. T. Jayapal Reddy, Chairman, St. Peter’s Institute of Pharmaceutical Sciences, Hanamkonda for providing the necessary facilities.

Disclosure statement

The authors report no conflicts of interest.

Funding information

The corresponding author is thankful for financial support from Science & Engineering Research Board (File No. SB/YS/LS-119/2013), Department of Science and Technology, New Delhi, India.