Quercetin topical application, from conventional dosage forms to nanodosage forms

Eur J Pharm Biopharm. 2016 Nov:108:41-53. doi: 10.1016/j.ejpb.2016.08.011. Epub 2016 Aug 24.

Abstract

Skin is a multifunctional organ with activities in protection, metabolism and regulation. Skin is in a continuous exposure to oxidizing agents and inflammogens from the sun and from the contact with the environment. These agents may overload the skin auto-defense capacity. To strengthen skin defense mechanisms against oxidation and inflammation, supplementation of exogenous antioxidants is a promising strategy. Quercetin is a flavonoid with very pronounced effective antioxidant and antiinflammatory activities, and thus a candidate of first choice for such skin supplementation. Quercetin showed interesting actions in cellular and animal based models, ranging from protecting cells from UV irradiation to support skin regeneration in wound healing. However, due to its poor solubility, quercetin has limited skin penetration ability, and various formulation approaches were taken to increase its dermal penetration. In this article, the quercetin antioxidant and antiinflammatory activities in wound healing and supporting skin against aging are discussed in detail. In addition, quercetin topical formulations from conventional emulsions to novel nanoformulations in terms of skin penetration enhancement are also presented. This article gives a comprehensive review of quercetin for topical application from biological effects to pharmaceutical formulation design for the last 25 years of research.

Keywords: Antiinflammatory activity; Antioxidant activity; Franz cells; In vitro skin penetration; In vivo skin penetration; Quercetin; Skin antiaging; Wound healing.

Publication types

  • Review

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry
  • Cell Line
  • Emulsions / chemistry
  • Female
  • Humans
  • Keratinocytes / cytology
  • Male
  • Mice
  • Nanomedicine / methods*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Particle Size
  • Quercetin / administration & dosage
  • Quercetin / chemistry*
  • Rats
  • Reactive Oxygen Species / chemistry
  • Skin / drug effects*
  • Skin Absorption
  • Solubility
  • Swine
  • Water / chemistry
  • Wound Healing

Substances

  • Anti-Inflammatory Agents
  • Antioxidants
  • Emulsions
  • Reactive Oxygen Species
  • Water
  • Quercetin