Abstract
Caffeic acid is a natural antioxidant, largely distributed in plant tissues and food sources, possessing anti-inflammatory, antimicrobial, and anticarcinogenic properties. The object of this investigation was the development of a formulation for caffeic acid cutaneous administration. To this aim, caffeic acid has been loaded in solid lipid nanoparticles by hot homogenization and ultrasonication, obtaining aqueous dispersions with high drug encapsulation efficiency and 200 nm mean dimension, as assessed by photon correlation spectroscopy. With the aim to improve the consistence of the aqueous nanodispersions, different types of polymers have been considered. Particularly, poloxamer 407 and hyaluronic acid gels containing caffeic acid have been produced and characterized by X-ray and rheological analyses. A Franz cell study enabled to select poloxamer 407, being able to better control caffeic acid diffusion. Thus, a nanoparticulate gel has been produced by addition of poloxamer 407 to nanoparticle dispersions. Notably, caffeic acid diffusion from nanoparticulate gel was eight-fold slower with respect to the aqueous solution. In addition, the spreadability of nanoparticulate gel was suitable for cutaneous administration. Finally, the antioxidant effect of caffeic acid loaded in nanoparticulate gel has been demonstrated by ex-vivo evaluation on human skin explants exposed to cigarette smoke, suggesting a protective role exerted by the nanoparticles.
Highlights
Caffeic acid (CA) is a naturally occurring hydroxycinnamic acid amply present in coffee, fruits, plants, oils, grapes, and tea [1,2]
Solvents were of high-performance liquid chromatography (HPLC) grade and all other chemicals were of analytical grade
Solid Lipid Nanoparticles (SLN) dispersions were prepared emulsifying a fused lipid phase constituted of tristearin with an aqueous solution constituted of p188 by hot homogenization, followed by ultrasonication in order to decrease the droplet size
Summary
Caffeic acid (CA) is a naturally occurring hydroxycinnamic acid amply present in coffee, fruits, plants, oils, grapes, and tea [1,2]. CS is considered responsible for multiple, highly diverse effects on human health, including tumors, noncancerous lung diseases, atherosclerosis, and disorders of male and female reproductive systems [8,9,10]. The skin can counteract the CS toxic effect by natural mechanisms of defense, acting as antioxidants or oxidant-degrading systems. This homeostatic protection can unsuccessfully increase cutaneous reactive oxygen species (ROS), leading to the onset of dermatological diseases [12]. In this respect, the cutaneous administration of antioxidants represents an approach to restore homeostasis, preventing ROS-mediated disorders
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