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.

Highlights

  • Human skin can be affected by a broad range of disorders, spanning from inflammatory diseases to skin cancer, many of which did not find an efficacious therapy; there is an unmet need for effective strategies to treat dermatological pathologies [1,2,3,4]

  • In order to determine the caffeic acid (CA) stability in water, its content was evaluated in aqueous solution of the drug stored in different conditions

  • The mathematical modelling of CA residual content, obtained by fitting profiles with Equations (1) and (2), revealed that CA stability followed a zero order kinetic model, as indicated by the high coefficient correlation values reported in Table S1, suggesting that CA stability was independent from its concentration [29]

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Summary

Introduction

Human skin can be affected by a broad range of disorders, spanning from inflammatory diseases to skin cancer, many of which did not find an efficacious therapy; there is an unmet need for effective strategies to treat dermatological pathologies [1,2,3,4]. Ethanol is able to disorganize the stratum corneum barrier, opening spaces for ETHO crossing, while the peculiar structure of phospholipids, similar to skin lipids, promotes ETHO permeation [16,17,18] On this matter, some authors have demonstrated the presence of intact vesicles in the skin strata, suggesting that ETHOs can overcome the stratum corneum, allowing deep drug permeation [20,21,22]. Some authors have demonstrated the presence of intact vesicles in the skin strata, suggesting that ETHOs can overcome the stratum corneum, allowing deep drug permeation [20,21,22] In this context, the object of the present investigation is a pre-formulative study aimed at the development of ETHOs for CA solubilization and delivery through the skin. This electrochemical monitoring enables to obtain a reliable prediction of in-vivo cutaneous antioxidant administration [27]

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