Chemical ultraviolet absorbers topically applied in a skin barrier mimetic formulation remain in the outer stratum corneum of porcine skin

Int J Pharm. 2016 Aug 20;510(1):250-4. doi: 10.1016/j.ijpharm.2016.06.041. Epub 2016 Jun 16.

Abstract

The objective of the present study was to evaluate the fate of three chemical sunscreens, isoamyl p-methoxycinnamate (IPMC), diethylamino hydroxybenzoyl hexyl benzoate (DHHB), and bis-ethylhexylphenol methoxyphenyl triazine (BEMT), topically applied to mammalian skin from a skin barrier mimetic oil-in-water formulation. High Performance Liquid Chromatography (HPLC) methods were developed for the analysis of each molecule and validated. Franz cell permeation studies were conducted following application of finite doses of the formulations to excised porcine skin. A vehicle formulation containing no sunscreens was evaluated as a control. Permeation studies were conducted for 12h after which full mass balance studies were carried out. Analysis of individual UV sunscreens was achieved with HPLC following application of the formulation to the skin with no interference from the vehicle components. No skin permeation of any of the chemical sunscreens was evident after 12h. While sunscreens were detected in up to 12 tape strips taken from the SC, 87% or more of the applied doses recovered in the first 5 tape strips. When corrected for the amount of protein removed per tape strip this corresponded to a penetration depth in porcine stratum corneum of ∼1.7μm. Mass balance studies indicated total recovery values were within accepted guidelines for cosmetic formulations. Overall, only superficial penetration into the SC was observed for each compound. These findings are consistent with the physicochemical properties of the selected UV absorbing molecules and their formulation into an ordered biomimetic barrier formulation thus support their intended use in topical consumer formulations designed to protect from UV exposure. To our knowledge this is the first report of depth profiling of chemical sunscreens in the SC that combines tape stripping and protein determination following in vitro Franz cell studies.

Keywords: Mass balance; Permeation studies; Porcine skin; Sunscreens; Tape stripping; Topical.

MeSH terms

  • Administration, Topical
  • Animals
  • Biomimetic Materials / administration & dosage*
  • Biomimetic Materials / metabolism
  • Drug Compounding
  • Epidermis / drug effects*
  • Epidermis / metabolism
  • Organ Culture Techniques
  • Skin Absorption / drug effects*
  • Skin Absorption / physiology
  • Sunscreening Agents / administration & dosage*
  • Sunscreening Agents / metabolism
  • Swine
  • Ultraviolet Rays*

Substances

  • Sunscreening Agents