Mechanistic approach for the development of ultrafine o/w emulsions using blends medium and long chain triglycerides: solubility and bioavailability enhancement of perphenazine

  • Sanjula Baboota Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi-110062, INDIA.
  • Abdullah Abdullah Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi-110062, INDIA.
  • Gulam Mustafa Dept. Pharmaceutics F/O Pharmacy Jamia Hamdard New Delhi-110062
  • Jasjeet Kaur Sahni Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi-110062, INDIA.
  • Javed Ali Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi-110062, INDIA.

Abstract

A thermodynamically stable ultrafine (o/w) emulsion containing perphenazine for solubility and oral bioavailability enhancement using blends of long and medium chain triglyceride was developed. Formulation was prepared using low energy emulsification phase titration method. The optimized formulations consisted of blend of linseed and sefsol 218 (1:1), polysorbate 40, polyethylene glycol 400 and distilled water as an oil, surfactant, cosurfactant and dispersion phase respectively. The formulations were characterized on the basis of viscosity, refractive index, particle size distribution, spectral transmittance and surface morphology. Formulations were evaluated for release study by everted gut sac using intestinal mucosa. The ex vivo release data showed that nanoemulsions significantly increased the permeation rate of perphenazine over the simple suspension. Following oral administration of nanoemulsion in wistar rats, both AUC and Cmax of perphenazine increased by 2.9 fold and 2.54-fold respectively compared with the perphenazine suspension. The resultant bioavailability might be due to increased solubility, bypassing the first-pass metabolism through lymphatic absorption and enhanced permeation potential of perphenazine.

Published
2013-03-29
How to Cite
BABOOTA, Sanjula et al. Mechanistic approach for the development of ultrafine o/w emulsions using blends medium and long chain triglycerides: solubility and bioavailability enhancement of perphenazine. Journal of Excipients and Food Chemicals, [S.l.], v. 4, n. 1, p. 12-24, mar. 2013. ISSN 21502668. Available at: <https://ojs.abo.fi/ojs/index.php/jefc/article/view/196>. Date accessed: 27 oct. 2021.
Section
Original Research Articles

Keywords

Perphenazine, Nanoemulsion, Phase diagram, Lymphatic delivery, Thermodynamic study, Pharmacokinetic.