Usnea barbata CO2-supercritical extract in alkyl polyglucoside-based emulsion system: contribution of Confocal Raman imaging to the formulation development of a natural product

Pharm Dev Technol. 2016 Aug;21(5):563-75. doi: 10.3109/10837450.2015.1026606. Epub 2015 Jul 1.

Abstract

Topical treatment of skin infections is often limited by drawbacks related to both antimicrobial agents and their vehicles. In addition, considering the growing promotion of natural therapeutic products, our objective was to develop and evaluate naturally-based emulsion system, as prospective topical formulation for skin infections-treatment. Therefore, alkyl polyglucoside surfactants were used for stabilization of a vehicle serving as potential carrier for supercritical CO2-extract of Usnea barbata, lichen with well-documented antimicrobial activity, incorporated using two protocols and three concentrations. Comprehensive physicochemical characterization suggested possible involvement of extract's particles in stabilization of the investigated system. Raman spectral imaging served as the key method in disclosing extract's particles potential to participate in the microstructure of the tested emulsion system via three mechanisms: (1) particle-particle aggregation, (2) adsorption at the oil-water interface and (3) hydrophobic particle-surfactant interactions. Stated extract-vehicle interaction proved to be correlated to the preparation procedure and extract concentration on one hand and to affect the physicochemical and biopharmaceutical features of investigated system, on the other hand. Thereafter, formulation with the best preliminary stability and liberation profile was selected for further efficiency and in vivo skin irritation potential evaluation, implying pertinent in vitro antimicrobial activity against G+ bacteria and overall satisfying preliminary safety profile.

Keywords: Antimicrobial activity; biopharmaceutical characterization; colloidal structure; extract–vehicle interaction; physicochemical stability; skin performance.

MeSH terms

  • Biological Products / analysis*
  • Biological Products / pharmacology
  • Carbon Dioxide / chemistry
  • Chromatography, Supercritical Fluid / methods*
  • Emulsifying Agents / analysis*
  • Emulsifying Agents / pharmacology
  • Glucosides / analysis*
  • Glucosides / pharmacology
  • Humans
  • Organ Culture Techniques
  • Skin Absorption / drug effects
  • Skin Absorption / physiology
  • Spectrum Analysis, Raman / methods*
  • Usnea*
  • Young Adult

Substances

  • Biological Products
  • Emulsifying Agents
  • Glucosides
  • Carbon Dioxide