Quercetin topical application, from conventional dosage forms to nanodosage forms

• Published in: European journal of pharmaceutics and biopharmaceutics 2016-11, Vol.108, p.41-53
• Main Authors: Hatahet, T., Morille, M., Hommoss, A., Devoisselle, J.M., Müller, R.H., Bégu, S.
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Anti-Inflammatory Agents - administration & dosage; Anti-Inflammatory Agents - chemistry; Antiinflammatory activity; Antioxidant activity; Antioxidants - administration & dosage; Antioxidants - chemistry; Cell Line; Emulsions - chemistry; Female; Franz cells; Humans; In vitro skin penetration; In vivo skin penetration; Keratinocytes - cytology; Life Sciences; Male; Mice; Nanomedicine - methods; Nanoparticles - administration & dosage; Nanoparticles - chemistry; Particle Size; Pharmaceutical sciences; Quercetin; Quercetin - administration & dosage; Quercetin - chemistry; Rats; Reactive Oxygen Species - chemistry; Skin - drug effects; Skin Absorption; Skin antiaging; Solubility; Swine; Water - chemistry; Wound Healing
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2016.08.011

[Display omitted] 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.