Rosacea Topical Treatment and Care: From Traditional to New Drug Delivery Systems

Abstract

Rosacea is a multifactorial chronic inflammatory dermatosis characterized by flushing, nontransient erythema, papules and pustules, telangiectasia, and phymatous alterations accompanied by itching, burning, or stinging, the pathophysiology of which is not yet fully understood. Conventional topical treatments usually show limited efficacy due to the physical barrier property of the skin that hinders skin penetration of the active ingredients, thereby hampering proper drug skin delivery and the respective therapeutic or cosmetic effects. New advances regarding the physiopathological understanding of the disease and the underlying mechanisms suggest the potential of new active ingredients as promising therapeutic and cosmetic approaches to this dermatosis. Additionally, the development of new drug delivery systems for skin delivery, particularly the potential of nanoparticles for the topical treatment and care of rosacea, has been described. Emphasis has been placed on their reduced nanometric size, which contributes to a significant improvement in the attainment of targeted skin drug delivery. In addition to the exposition of the known pathophysiology, epidemiology, diagnosis, and preventive measures, this Review covers the topical approaches used in the control of rosacea, including skin care, cosmetics, and topical therapies, as well as the future perspectives on these strategies.

Keywords: Cosmetic; Drug Delivery System; Nanoparticle; Rosacea; Skin; Therapy.

Figure 1

Summary representation of the main aspects involved in the development and manifestation of signals of rosacea (produced with Biorender).

Figure 2

(A) Schematization of MTZ in vitro permeation studies through pig skin. (B) Comparison of the amount of MTZ retained in the skin when applied at a dose of 1 mg through NNE and commercial gel. (C) AUC–time profiles and (D) plasma concentration of MTZ after administration via NNE and commercial gel. Adapted from Yu et al. with permission from Elsevier. Copyright 2014 Elsevier B.V.

Figure 3

(A) Schematic representation of the prepared ZnO nanorods, with a transmission electron microscopy image. (B) Scanning electron microscopy image of the developed cross-linked hydrogel containing ZnO nanorods. (C) Characterization of the developed transdermal system, in terms of porosity, density, and mechanical properties (tensile strength, elastic modulus, and elongation at break). Adapted from Radwan-Praglowska et al. with permission from Elsevier. Copyright 2020 The Authors.

Figure 4

(A) Schematic representation of the developed PGZ NNE, including performed characterization assays. (B) Tolerance study results in humans involving TEWL measurement. (C) Tolerance study results in humans involving skin hydration measurements. (D) Relative expression of inflammatory cytokines IL-6, TNF-α, and IL-1β in mice. Adapted from Espinoza et al. with permission from Elsevier. Copyright 2019 Elsevier Inc.

Figure 5

Efficacy end points after treatment regarding (A) inflammatory lesion count, (B) IGA end points, and (C) percent reduction in inflammatory lesions. Adapted from Gold et al. with permission from Elsevier. Copyright 2020 American Academy of Dermatology, Inc.

Figure 6

(A) Schematic representation of the developed hybrid lipid–polymer nanocarriers, with respective composition. (B) In vitro rat skin permeation results. (C) In vivo assay representation, with hematoxylin and eosin histological staining images. Adapted from Desai et al. with permission from Elsevier. Copyright 2013 Elsevier B.V.

Figure 7

Representative rosacea management scheme: nontherapeutic measures, cosmetics/skin care, topical pharmacological measures, and future challenges (produced with Biorender).