Effect of hydrophobic permeation enhancers on the release and skin permeation kinetics from matrix type transdermal drug delivery system of ketotifen fumarate

• Published in: Acta Poloniae pharmaceutica Vol. 58; no. 2; pp. 101 - 105
• Main Authors: Bhattacharya, A, Ghosal, S K
• Format: Journal Article
• Language: English
• Published: Poland 01-03-2001
• Subjects: Administration, Cutaneous; Animals; Diffusion; Drug Delivery Systems; Histamine H1 Antagonists - administration & dosage; Ketotifen - administration & dosage; Ketotifen - pharmacokinetics; Mice; Permeability; Skin - metabolism
• ISSN: 0001-6837

Ketotifen fumarate is effective in low doses in the treatment of bronchial asthma particularly of allergic origin. However, it is substantially metabolized in the liver when administered orally. Hence transdermal patches of combination of ethylcellulose/polyvinylpyrrolidone and Eudragits RS 100/RL 100 were prepared and their drug release kinetics and skin permeation profiles were evaluated. However, the skin permeation profiles were found to be low and subtherapeutic. Hence three hydrophobic biocompatible substances, viz, isopropyl myristate, isopropyl palmitate and linoleic acid and also combination of isopropyl myristate and linoleic acid were used as permeation enhancers in the film. It was found that isopropyl myristate and linoleic acid combination and isopropyl myristate alone produced promising results compared to isopropyl palmitate and linoleic acid.