Topical delivery of retinyl ascorbate co-drug - 1. synthesis, penetration into and permeation across human skin

Abdulmajed, Kasem and Heard, Charles Martin ORCID: https://orcid.org/0000-0001-9703-9777 2004. Topical delivery of retinyl ascorbate co-drug - 1. synthesis, penetration into and permeation across human skin. International Journal of Pharmaceutics 280 (1-2) , pp. 113-124. 10.1016/j.ijpharm.2004.05.008

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Abstract

A novel synthetic technique was used to synthesise the co-drug retinyl ascorbate (RA-AsA) ester from all-trans-retinyl chloride (RA) and l-ascorbic acid (AsA) suspended in ethanol at low temperature. Its log P, solubility in a Me:PBS, 50/50 at pH 4.8 and degradation constant were determined. The flux and permeation coefficient were determined using heat separated human skin membrane, and skin penetration was determined by tape stripping using full thickness human. All experiments were performed in parallel with retinyl palmitate (Rol-Pal) and ascorbyl palmitate (AsA-Pal), which are used in commercial topical formulations. RA-AsA exhibited favourable log P (2.2), with stability much greater than RA and AsA, but similar stability to Rol-Pal and AsA-Pal. The flux of RA-AsA was lower than for Rol-Pal and AsA-Pal. RA-AsA also demonstrated higher skin retention than the other two esters, but delivered more RA and AsA to the viable epidermis than retinol from Rol-Pal and ascorbic acid from AsA-Pal. Overall, the data suggest the potential value of RA-AsA co-drug for the purpose of treating damage to skin resulting from UV-induced production of free radicals.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Subjects:	R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords:	Co-drug; Retinoic acid; Retinyl ascorbate; Anti-oxidant; Skin permeation; Tape stripping; Ascorbic acid.
Publisher:	Elsevier
ISSN:	0378-5173
Last Modified:	27 Oct 2022 09:43
URI:	https://orca.cardiff.ac.uk/id/eprint/67487

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