Antibacterial PEGylated Solid Lipid Microparticles for Cosmeceutical Purpose: Formulation, Characterization, and Efficacy Evaluation

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.

The Acne-treatment Potential of Cinnamomum Camphora Chvar. Borneol Essential Oil in Vitro and in Vivo

“…BEO signi cantly reduces expression of TNF-α in serum and tissues with xylene-induced auricular in ammation in mice [9], and its main component, borneol, can inhibit TNF-α and PTGS2 [21] production in tissues of mice with acute in ammations. Limonene has been reported to have anti-in ammatory effects by reducing the content of serum TNF-α and down-regulating the expression of NF-κB in in ammatory rats, and has been used in the treatment of acne [22]. The β-caryophyllene signi cantly reduces the mRNA expression levels of ESR1 in the Alzheimer's disease cell injury model [23], indicating that the above target genes and components are of great signi cance in BEO treatment of acne.…”

The Use of Micro- and Nanocarriers for Resveratrol Delivery into and across the Skin in Different Skin Diseases—A Literature Review

“…To counteract skin infections caused by pathogen bacterial strains (i.e., Staphylococcus aureus and Propionibacterium acnes ), lipid microparticles containing resveratrol and R-(+)-limonene have been developed [ 114 ]. It has been shown that encapsulating resveratrol in an amorphous state in microspheres prolongs its half-life and avoids inactivation due to isomerization phenomena.…”

Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

“…This is particularly true for resveratrol (RSV), a nutraceutical that exhibits interesting and broad-spectrum pharmacological activities that make it a promising candidate for potential applications in different fields [ 1 , 2 , 3 ]. RSV (active form: 3,4′,5-trihydroxy-trans-stilbene) is a phenolic phytoalexin obtained from red grapes, red wine and wild berries, as well as by both chemical and biotechnological synthesis [ 4 ]. Thanks to its molecular structure, RSV is able to bind different biomolecules, thus causing a wide range of potential therapeutic effects [ 5 ].…”