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Design and characterization of ethosomes for transdermal delivery of caffeic acid

DOI: 10.3390/pharmaceutics12080740 DOI Help

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

Open Access Open Access

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


Discipline Tags:

Drug Delivery Health & Wellbeing Biochemistry Chemistry Life Sciences & Biotech

Technical Tags:

Scattering Small Angle X-ray Scattering (SAXS)