Enhanced vitamin C skin permeation from supramolecular hydrogels, illustrated using in situ ToF-SIMS 3D chemical profiling

• Published in: International journal of pharmaceutics Vol. 563; pp. 21 - 29
• Main Authors: Starr, Nichola J., Abdul Hamid, Khuriah, Wibawa, Judata, Marlow, Ian, Bell, Mike, Pérez-García, Luïsa, Barrett, David A., Scurr, David J.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 30.05.2019
• Subjects: Administration, Topical; Animals; Ascorbic Acid - administration & dosage; Depth profiling; Hydrogels - administration & dosage; Permeation enhancer; Skin - metabolism; Skin Absorption; Skin permeation; Spectrometry, Mass, Secondary Ion; Supramolecular hydrogel; Swine; ToF-SIMS; Vitamin C; Vitamins - administration & dosage; Supramolecular hydrogel; Permeation enhancer; ToF-SIMS; Depth profiling; Skin permeation; Vitamin C
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2019.03.028

[Display omitted] Vitamin C (ascorbic acid) is a naturally occurring, powerful anti-oxidant with the potential to deliver numerous benefits to the skin when applied topically. However, topical use of this compound is currently restricted by an instability in traditional formulations and the delivery and eventual fate of precursor compounds has been largely unexplored. Time of flight secondary ion mass spectrometry (ToF-SIMS) is an emerging technique in the field of skin research and offers detailed chemical analysis, with high mass and spatial resolution, as well as profiling capabilities that allow analysis as a function of sample depth. This work demonstrates the successful use of ToF-SIMS to obtain, in situ, accurate 3D permeation profiles of both ascorbic acid and a popular precursor, ascorbyl glucoside, from ex vivo porcine skin. The significant permeation enhancing effect of a supramolecular hydrogel formulation, produced from an amphiphilic gemini imidazolium-based surfactant, was also demonstrated for both compounds. Using ToF-SIMS, it was also possible to detect and track the breakdown of ascorbyl glucoside into ascorbic acid, elucidating the ability of the hydrogel formulation to preserve this important conversion until the targeted epidermal layer has been reached. This work demonstrates the potential of ToF-SIMS to provide 3D permeation profiles collected in situ from ex vivo tissue samples, offering detailed analysis on compound localisation and degradation. This type of analysis has significant advantages in the area of skin permeation, but can also be readily translated to other tissue types.