Development, physico-chemical characterization and in-vitro studies of hydrogels containing rosmarinic acid-loaded nanoemulsion for topical application

J Pharm Pharmacol. 2019 Aug;71(8):1199-1208. doi: 10.1111/jphp.13102. Epub 2019 May 24.

Abstract

Objectives: Natural sources with antioxidant activity, such as rosmarinic acid (RA), have been considered as an interesting approach for the development of new anti-ageing skin products. In this context, this study aimed to develop hydrogels containing RA-loaded nanoemulsions and evaluate the effect of the addition of Tween® 80 (a nonionic cosurfactant) in formulations intended to be used for topical application.

Methods: Physico-chemical characterization, in-vitro release and skin retention/permeation from hydrogels of RA-loaded nanoemulsions (containing or not Tween® 80) were evaluated. The RA-loaded nanoemulsion safety profiles were also investigated in keratinocytes (HaCaT cells).

Key findings: It was observed that all formulations presented adequate physico-chemical characterization for topical application. Furthermore, the results also demonstrated that the presence of Tween® 80 decreased the droplet size and polydispersity index of nanoemulsions and hydrogels. An extended RA release was noted for the hydrogels. However, when comparing the hydrogels, a positive effect of the presence of Tween® 80 on RA retention/permeation in total skin was seen. The RA-loaded nanoemulsion safety profiles demonstrated a good tolerability (3.125-100 μm) in HaCaT cells.

Conclusions: The overall results demonstrated that the formulations developed in this study can be considered as a suitable carrier for RA in a topical application targeting new anti-ageing skin care products.

Keywords: HaCaT; cytotoxicity; hydrogel; in-vitro studies; nanoemulsion; rosmarinic acid.

MeSH terms

  • Administration, Cutaneous
  • Administration, Topical
  • Animals
  • Cell Line
  • Cinnamates / administration & dosage*
  • Cinnamates / chemistry*
  • Depsides / administration & dosage*
  • Depsides / chemistry*
  • Drug Compounding / methods
  • Emulsions / administration & dosage*
  • Emulsions / chemistry*
  • Humans
  • Hydrogels / administration & dosage*
  • Hydrogels / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Particle Size
  • Polysorbates / chemistry
  • Rosmarinic Acid
  • Skin / metabolism
  • Skin Absorption / drug effects
  • Swine

Substances

  • Cinnamates
  • Depsides
  • Emulsions
  • Hydrogels
  • Polysorbates