Transdermal delivery of valsartan: I. Effect of various terpenes.
The objective of the present study was to investigate the effect of various terpenes, including a diterpene, forskolin (FSK; a putative penetration enhancer), on skin permeation of valsartan. Permeation studies were carried out with Automated Transdermal Diffusion Cells Sampling System (SFDC 6, LOGAN Instruments Corp., NJ, USA) through rat skin and human cadaver skin (HCS) using ethanol: IPB (pH 7.4) (40:60) as vehicle. The efficacy of the study terpenes for permeation of valsartan across rat skin and human cadaver skin was found in the order of cineole > d-limonene > l-menthol > linalool > FSK and cineole > d-limonene > linalool > l-menthol > FSK, respectively. No apparent skin irritation (erythema, edema) was observed on treatment of skin with terpenes including FSK. FT-IR, DSC, and histopathological studies revealed that FSK enhanced the skin permeation of the active drug by disruption and extraction of lipid bilayers of SC in consonance with other terpenes.
Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi, India.
Mohammad
M
Rizwan
Mohammed
M
Aqil
Abdul
A
Ahad
Yasmin
Y
Sultana
Mushir M
MM
Ali
D000277:Adjuvants, Pharmaceutic / Q000737:chemistry / Q000494:pharmacology*; D000279:Administration, Cutaneous; D047228:Angiotensin II Type 1 Receptor Blockers / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D000959:Antihypertensive Agents / Q000737:chemistry / Q000493:pharmacokinetics*; D002102:Cadaver; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010539:Permeability; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption / Q000187:drug effects*; D017550:Spectroscopy, Fourier Transform Infrared; D013729:Terpenes / Q000737:chemistry / Q000494:pharmacology*; D013777:Tetrazoles / Q000737:chemistry / Q000493:pharmacokinetics*; D014633:Valine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D000068756:Valsartan
D000277:Adjuvants, Pharmaceutic; D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D004337:Drug Carriers; D013729:Terpenes; D013777:Tetrazoles; D000068756:Valsartan; D014633:Valine