title: Effect of borneol on the transdermal permeation of drugs with differing lipophilicity and molecular organization of stratum corneum lipids.
abstract: The aim of the present paper was to investigate the promoting activity of borneol on the transdermal permeation of drugs with differing lipophilicity, and probe its alterations in molecular organization of stratum corneum (SC) lipids. The toxicity of borneol was evaluated in epidermal keratinocyte HaCaT and dermal fibroblast CCC-HSF-1 cell cultures and compared to known enhancers, and its irritant profile was also assessed by transepidermal water loss (TEWL) evaluation. The promoting effect of borneol on the transdermal permeation of five model drugs, namely 5-fluorouracil, antipyrine, aspirin, salicylic acid and ibuprofen, which were selected based on their lipophilicity denoted by logp value, were performed using in vitro skin permeation studies. Attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) was employed to monitor the borneol-induced alteration in molecular organization of SC lipids. The enhancer borneol displayed lower cytotoxicity or irritation in comparison to the well-established and standard enhancer Azone. Borneol could effectively promote the transdermal permeation of five model drugs, and its enhancement ratios were found to be parabolic curve with the logp values of drugs, which exhibited the optimum permeation activity for relatively hydrophilic drugs (an estimated logp value of -0.5 ∼0.5). The molecular mechanism studies suggested that borneol could perturb the structure of SC lipid alkyl chains, and extract part of SC lipids, resulting in the alteration in the skin permeability barrier.
authors.affiliation: a Xiang Ya Nursing School of Central South University , Changsha , China ;|b Nursing Department , the Third Xiangya Hospital of Central South University , Changsha , China ;
authors.forename: Qi-Feng
authors.initials: QF
authors.lastname: Yi
authors.affiliation: a Xiang Ya Nursing School of Central South University , Changsha , China ;|b Nursing Department , the Third Xiangya Hospital of Central South University , Changsha , China ;
authors.forename: Jin
authors.initials: J
authors.lastname: Yan
authors.affiliation: a Xiang Ya Nursing School of Central South University , Changsha , China ;
authors.forename: Si-Yuan
authors.initials: SY
authors.lastname: Tang
authors.affiliation: b Nursing Department , the Third Xiangya Hospital of Central South University , Changsha , China ;
authors.forename: Hui
authors.initials: H
authors.lastname: Huang
authors.affiliation: c Department of Dermatology , the Third Xiangya Hospital of Central South University , Changsha , China.
authors.forename: Li-Yang
authors.initials: LY
authors.lastname: Kang
mesh_terms: D000818:Animals; D001892:Camphanes / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D005347:Fibroblasts / Q000187:drug effects; D006801:Humans; D015603:Keratinocytes / Q000187:drug effects; D050356:Lipid Metabolism / Q000187:drug effects; D008055:Lipids / Q000737:chemistry; D008297:Male; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D014677:Pharmaceutical Vehicles / Q000737:chemistry* / Q000633:toxicity; D017207:Rats, Sprague-Dawley; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption; D014867:Water / Q000378:metabolism; D014870:Water Loss, Insensible / Q000187:drug effects
chemical_list: D001892:Camphanes; D008055:Lipids; D004364:Pharmaceutical Preparations; D014677:Pharmaceutical Vehicles; D014867:Water; C022871:isoborneol
keywords: Borneol; infrared spectroscopy; penetration enhancer; stratum corneum