Transdermal drug delivery of tricyclic antidepressants: effect of fatty acids.
The aim of the present study was to investigate the effects of fatty acids on the permeation of tricyclic antidepressants, e.g., imipramine hydrochloride (IMH) and amitriptyline hydrochloride (AMH). Five percent w/v of saturated (lauric acid) and unsaturated (oleic acid, linoleic acid, linolenic acid, trans-elaidic acid and trans-vaccenic acid) fatty acids in an ethanol (EtOH):water (2:1) system were used in this study. Flux and lag-time of tricyclic antidepressants were significantly increased and reduced, respectively, compared with control (p < 0.05). There were no significant differences between the effects of lauric and unsaturated fatty acids, both cis and trans, on the permeation of IMH and AMH (except vaccenic acid in case of IMH). The formation of 'grain boundaries' by straight chain fatty acids (saturated and trans-unsaturated fatty acids) could not be observed by Fourier-transform infrared spectroscopy (FT-IR). However, perturbation or increased bilayer fluidity of Stratum corneum (SC) induced by cis-unsaturated fatty acid was observed by FT-IR.
Jain
A K
AK
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Mohali, India.
Panchagnula
R
R
D000279:Administration, Cutaneous; D000639:Amitriptyline / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D000929:Antidepressive Agents, Tricyclic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004817:Epidermis / Q000187:drug effects / Q000378:metabolism; D005227:Fatty Acids / Q000494:pharmacology*; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology; D007099:Imipramine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D017550:Spectroscopy, Fourier Transform Infrared; D013237:Stereoisomerism
D000929:Antidepressive Agents, Tricyclic; D005227:Fatty Acids; D005231:Fatty Acids, Unsaturated; D000639:Amitriptyline; D007099:Imipramine