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Open AccessArticle

Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems

1
School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK
2
School of Human Sciences, London Metropolitan University, 166-220 Holloway Road, London N7 8DB, UK
3
GlaxoSmithKline Consumer Healthcare, St George’s Avenue, Weybridge KT13 0DE, UK
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2020, 88(2), 19; https://doi.org/10.3390/scipharm88020019
Received: 27 February 2020 / Revised: 27 March 2020 / Accepted: 30 March 2020 / Published: 1 April 2020
(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)
3-O-ethyl l-ascorbic acid (EA), an ether derivative of Vitamin C, is widely used in skincare formulations. Previously, we reported the effects of neat solvents on EA percutaneous absorption and observed that 0.6–7.5% of the applied EA was delivered through the skin over 24 h. In this work, we designed complex formulations using combinations of solvents that may act synergistically and examined their impact on EA permeation in porcine skin in vitro under finite dose conditions. Binary combinations of propylene glycol (PG) with propylene glycol monolaurate (PGML) were effective in enhancing skin permeation of EA compared with individual solvents (p < 0.05). Combining PGML with 1,2-hexanediol (HEX) did not result in significantly higher EA permeation compared with the neat solvents (p > 0.05). Addition of the volatile solvent isopropyl alcohol (IPA) to PG solutions also did not improve EA skin delivery compared with neat PG. Ternary solvent systems containing PG:PGML were subsequently prepared by the addition of a lipophilic solvent, either isopropyl myristate (IPM), medium-chain triglycerides (MCT) or isostearyl isostearate (ISIS). The optimum vehicle, PG:PGML:IPM, promoted up to 70.9% skin delivery of EA. The PG:PGML:ISIS vehicles also promoted EA permeation across the skin, but to a significantly lesser extent than the IPM-containing vehicles. No enhancement of EA delivery was noted for the PG:PGML:MCT mixtures. These results will inform the development of targeted formulations for EA in the future. View Full-Text
Keywords: in vitro; topical formulations; porcine skin permeation; cosmetic and pharmaceutical product technology; finite dose; 3-O-ethyl l-ascorbic acid; antioxidant; vitamin C in vitro; topical formulations; porcine skin permeation; cosmetic and pharmaceutical product technology; finite dose; 3-O-ethyl l-ascorbic acid; antioxidant; vitamin C
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MDPI and ACS Style

Iliopoulos, F.; Hossain, A.S.M.M.A.; Sil, B.C.; Moore, D.J.; Lucas, R.A.; Lane, M.E. Topical Delivery of 3-O-ethyl l-ascorbic Acid from Complex Solvent Systems. Sci. Pharm. 2020, 88, 19.

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