Design and Characterization of Ethosomes for Transdermal Delivery of Caffeic Acid

Supandeep Singh Hallan, Maddalena Sguizzato, Paolo Mariani, Rita Cortesi (Coresponding Author), Nicolas Huang, Fanny Simelière, Nicola Marchetti, Markus Drechsler, Tautgirdas Ruzgas (Coresponding Author), Elisabetta Esposito (Coresponding Author)

Research output: Contribution to journalArticlepeer-review

19 Citations (Scopus)

Abstract

The present investigation describes a formulative study aimed at designing ethosomes for caffeic acid transdermal administration. Since caffeic acid is characterized by antioxidant potential but also high instability, its encapsulation appears to be an interesting strategy. Ethosomes were produced by adding water into a phosphatidylcholine ethanol solution under magnetic stirring. Size distribution and morphology of ethosome were investigated by photon correlation spectroscopy, small-angle X-ray spectroscopy, and cryogenic transmission electron microscopy, while the entrapment capacity of caffeic acid was evaluated by high-performance liquid chromatography. Caffeic acid stability in ethosome was compared to the stability of the molecule in water, determined by mass spectrometry. Ethosome dispersion was thickened by poloxamer 407, obtaining an ethosomal gel that was characterized for rheological behavior and deformability. Caffeic acid diffusion kinetics were determined by Franz cells, while its penetration through skin, as well as its antioxidant activity, were evaluated using a porcine skin membrane–covered biosensor based on oxygen electrode. Ethosome mean diameter was ≈200 nm and almost stable within three months. The entrapment of caffeic acid in ethosome dramatically prolonged drug stability with respect to the aqueous solution, being 77% w/w in ethosome after six months, while in water, an almost complete degradation occurred within one month. The addition of poloxamer slightly modified vesicle structure and size, while it decreased the vesicle deformability. Caffeic acid diffusion coefficients from ethosome and ethosome gel were, respectively, 137-and 33-fold lower with respect to the aqueous solution. At last, the caffeic acid permeation and antioxidant power of ethosome were more intense with respect to the simple solution.

Original languageEnglish
Article number740
Number of pages18
JournalPharmaceutics
Volume12
Issue number8
DOIs
Publication statusPublished - Aug 2020
Externally publishedYes

Keywords*

  • Caffeic acid
  • Ethosome
  • In vitro diffusion
  • Oxygen electrode
  • Penetration enhancers

Field of Science*

  • 1.4 Chemical sciences
  • 3.1 Basic medicine

Publication Type*

  • 1.1. Scientific article indexed in Web of Science and/or Scopus database

Fingerprint

Dive into the research topics of 'Design and Characterization of Ethosomes for Transdermal Delivery of Caffeic Acid'. Together they form a unique fingerprint.

Cite this