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Design and characterization of ethosomes for transdermal delivery of caffeic acid
DOI:
10.3390/pharmaceutics12080740
Authors:
Supandeep Singh
Hallan
(University of Ferrara; Malmö University)
,
Maddalena
Sguizzato
(University of Ferrara)
,
Paolo
Mariani
(Polytechnic University of Marche)
,
Rita
Cortesi
(University of Ferrara)
,
Nicolas
Huang
(CNRS, Institut Galien Paris-Saclay, Université Paris-Saclay)
,
Fanny
Simelière
(CNRS, Institut Galien Paris-Saclay, Université Paris-Saclay)
,
Nicola
Marchetti
(University of Ferrara)
,
Markus
Drechsler
(Bavarian Polymer Institute (BPI) Keylab “Electron and Optical Microscopy” University of Bayreuth)
,
Tautgirdas
Ruzgas
(Malmö University)
,
Elisabetta
Esposito
(University of Ferrara)
Co-authored by industrial partner:
No
Type:
Journal Paper
Journal:
Pharmaceutics
, VOL 12
State:
Published (Approved)
Published:
August 2020
Diamond Proposal Number(s):
21035

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.
Journal Keywords: ethosome; caffeic acid; penetration enhancers; in vitro diffusion; oxygen electrode
Subject Areas:
Chemistry,
Biology and Bio-materials,
Medicine
Instruments:
B21-High Throughput SAXS
Added On:
20/08/2020 08:48
Documents:
pharmaceutics-12-00740-v2.pdf
Discipline Tags:
Drug Delivery
Health & Wellbeing
Biochemistry
Chemistry
Life Sciences & Biotech
Technical Tags:
Scattering
Small Angle X-ray Scattering (SAXS)