Abstract

Phenolic compounds are a large, heterogeneous group of secondary metabolites found in various plants and herbal substances. From the perspective of dermatology, the most important benefits for human health are their pharmacological effects on oxidation processes, inflammation, vascular pathology, immune response, precancerous and oncological lesions or formations, and microbial growth. Because the nature of phenolic compounds is designed to fit the phytochemical needs of plants and not the biopharmaceutical requirements for a specific route of delivery (dermal or other), their utilization in cutaneous formulations sets challenges to drug development. These are encountered often due to insufficient water solubility, high molecular weight and low permeation and/or high reactivity (inherent for the set of representatives) and subsequent chemical/photochemical instability and ionizability. The inclusion of phenolic phytochemicals in lipid-based nanocarriers (such as nanoemulsions, liposomes and solid lipid nanoparticles) is so far recognized as a strategic physico-chemical approach to improve their in situ stability and introduction to the skin barriers, with a view to enhance bioavailability and therapeutic potency. This current review is focused on recent advances and achievements in this area.

Highlights

  • Phenolics are a large group of secondary metabolites comprising one or more phenolic rings in their chemical composition [1]

  • In terms of an ongoing oxidative stress-related autoimmune response against the melanocytes, phenolic compounds may exhibit a protective action toward melanogenesis [166,168]

  • Regulation of gene expression in cancer cells; to inhibit epidermal growth factor-induced neoplastic transformations in cell lines; to inhibit tyrosinase and melanogenesis; to inhibit the proteasome; an enzyme complex responsible for the degradation of essential proteins involved in cell development, and lead to subsequent suppression of cancer cell growth and spread, and to destabilize lysosomal membrane through permeabilization and cause cancer cell death

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Summary

Introduction

Phenolics are a large group of secondary metabolites comprising one or more phenolic rings in their chemical composition [1]. Since one or more of them are intrinsic for the majority of phenolic compounds, they do not always represent the best candidates for dermal transport [21,22] Another limitation is often set by insufficient chemical stability of particular representatives [23,24] (e.g., resveratrol [25,26,27], hypericin [28,29], hyperforin [30,31,32], quercetin [33,34,35], cathehin [36,37,38]), for which precise control over the selection of dermal vehicles and technological operations for drug introduction in preformulation stage is required. This is highly relevant, not widely discussed for the phenolic compounds and their introduction to lipid-based nanostructures

Phenolic Compounds
Fields of Application of Phenolic Compounds in Dermatology
Effects on Melanin Synthesis
Photosensitization
Antitumor Activity of Phenolics
Phenolics as Pro-Oxidants
Dermal Drug Delivery of Phenolic Compounds
Biopharmaceutical Considerations of the Dermal Drug Delivery
Stability of Phenolics
Lipid-Based Nanotechnologies
Liposomes
Solid Lipid Nanoparticles
Nanostructured Lipid Carriers
Nanoemulsions
Obtained Results
Conclusions
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