Abstract
The development of efficacious means of delivering antioxidant polyphenols from natural sources for the treatment of skin diseases is of great interest for many cosmetic and pharmaceutical companies. Resveratrol (RSV) and Limonene (LIM) have been shown to possess good anti-inflammatory and antibacterial properties against Staphylococcus aureus infections responsible for many skin disorders, such as acne vulgaris. In this study, solid lipid microparticles are designed as composite vehicles capable of encapsulating a high amount of trans-RSV and enhancing its absorption through the stratum corneum. A microparticulate system based on mixture of PEGylate lipids, long-chain alcohols and LIM is able to entrap RSV in an amorphous state, increasing its half-life and avoiding inactivation due to isomerization phenomena, which represents the main drawback in topical formulations. Particles have been characterized in term of shape, size distribution and drug loading. Antimicrobial tests against S. aureus have highlighted that empty microspheres possess per se antimicrobial activity, which is enhanced by the presence of LIM, demonstrating that they can represent an interesting bactericide vehicle for RSV administration on the skin.
Highlights
Skincare is one of the major concerns of modern society, since having healthy skin is synonymous with beauty, health, and youth
A nanocomposite system consisting of solid lipid microparticles containing Resveratrol and R-(+)-limonene, dispersed internally at the nanometric level in its amorphous state, was developed and studied to unveil its ability to counteract common skin infections caused by pathogen bacterial strains (i.e., Staphylococcus aureus and Propionibacterium acnes)
Microparticles have proven their suitability as a drug-delivery vehicle for skin administration of RSV, allowing its high encapsulation efficiency within solid lipid microparticles (SLM) in an amorphous state, as well as promoting its absorption through the stratum corneum of porcine epidermis
Summary
Skincare is one of the major concerns of modern society, since having healthy skin is synonymous with beauty, health, and youth. The look of the facial skin influences interpersonal relationships, because those who have skin with imperfections and blemishes are seen as unappealing, compared to those who have smooth skin [1] Some of these imperfections are due to bacterial infections; for instance, acne vulgaris is the most common of all skin diseases. Cellulitis, erysipelas, impetigo, folliculitis, furuncles, and carbuncles are common skin diseases caused by Staphylococcus aureus infection [3]. These infections are treated with both oral and topical antibacterial agents. RSV has been shown to be active against a wide spectrum of bacterial strains (i.e., Neisseria gonorrhoeae, Neisseria meningitidis, Helicobacter pylori, Staphylococcus aureus, Enterococcus faecalis, Pseudomonas aeruginosa, Proteus mirabilis, and Propionibacterium acnes) [11,12]. RSV reduces the pro-inflammatory signal, avoiding adenosine release from activated platelets and inhibiting protease-activated (PAR) and P2 receptors by interfering with mitogen-activated protein (MAPK) and c-Jun (JNK) kinases [13]
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