title: Lemon (Citrus limon, Burm.f.) essential oil enhances the trans-epidermal release of lipid-(A, E) and water-(B6, C) soluble vitamins from topical emulsions in reconstructed human epidermis.
abstract: Topical bioavailability of lipid- and water-soluble vitamins is a critical issue for protecting or anti-ageing formulations. Using 17-day-old SkinEthic(®) reconstructed human epidermis, we investigated (at 34°C) the role of lemon EO in enhancing the penetration of α-tocopherol (E) and retinyl acetate (A), pyridoxine (B(6)) and ascorbic acid (C), released from O/W or W/O emulsions. D-limonene, α-pinene and p-cymene (65.9, 2.2 and 0.5%w/w of the oil) had skin permeability coefficients Ps (10(-3) cm h(-1)) of 0.56 ± 0.03 (or 0.73 ± 0.02), 0.72 ± 0.05 (or 0.98 ± 0.05) and 0.84 ± 0.04 (or 1.14 ± 0.04), respectively, when incorporated in a W/O (or O/W) emulsion. Vitamins B6, C and A had Ps values of (3.0 ± 0.4) × 10(-3), (7.9 ± 0.6) × 10(-3) and (0.37 ± 0.02) × 10(-5) cm h(-1), respectively, and their flux through the skin was enhanced by a factor of 4.1, 3.4 and 5.8, respectively, in the presence of lemon EO. The penetration of vitamin E was nine-fold enhanced. Lemon EO produced only reversible modification of TEWL, and it is a safe and effective penetration enhancer for topical administration of lipid- and water-soluble vitamins.
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, University of Bologna, Bologna, Italy. luca.valgimigli@unibo.it
authors.forename: L
authors.initials: L
authors.lastname: Valgimigli
authors.forename: S
authors.initials: S
authors.lastname: Gabbanini
authors.forename: E
authors.initials: E
authors.lastname: Berlini
authors.forename: E
authors.initials: E
authors.lastname: Lucchi
authors.forename: C
authors.initials: C
authors.lastname: Beltramini
authors.forename: Y L
authors.initials: YL
authors.lastname: Bertarelli
mesh_terms: D000279:Administration, Cutaneous; D001205:Ascorbic Acid / Q000008:administration & dosage; D004224:Diterpenes; D004655:Emulsions / Q000008:administration & dosage; D004817:Epidermis / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D016014:Linear Models; D010938:Plant Oils / Q000008:administration & dosage*; D011736:Pyridoxine / Q000008:administration & dosage; D000084562:Retinyl Esters; D012869:Skin Absorption / Q000187:drug effects*; D014801:Vitamin A / Q000008:administration & dosage / Q000031:analogs & derivatives; D024502:alpha-Tocopherol / Q000008:administration & dosage
chemical_list: D004224:Diterpenes; D004655:Emulsions; D010938:Plant Oils; D000084562:Retinyl Esters; D014801:Vitamin A; C009166:retinol acetate; D024502:alpha-Tocopherol; C501365:lemon oil; D011736:Pyridoxine; D001205:Ascorbic Acid