A New Concept of Drug Delivery for Acne

Abstract

Adapalene is a stable naphthoic acid derivative that displays a strong retinoid agonist pharmacology. This drug controls cell proliferation and differentiation, and possesses significant anti-inflammatory action. The retinoid action of adapalene are mediated by the ligand-activated gene transcription factors retinoic acid receptors RARβ and RARγ. We describe here how an aqueous gel containing adapalene was selected for the topical treatment of acne.

Adapalene 0.1%/Benzoyl Peroxide 2.5% Gel

“…[17,18,20] Adapalene also showed antiproliferative effects and comedolytic activity in animal models. [17,18,20] Adapalene also modulates the epidermal immune system, decreasing the expression of the transcription factor AP-1, decreasing Toll-like receptor-2 (TLR2) expression (P. acnes triggers proinflammatory cytokine production by activating TLR2), increasing CD1d expression and decreasing interleukin (IL)-10 expression by keratinocytes. [17,18,20] Adapalene also modulates the epidermal immune system, decreasing the expression of the transcription factor AP-1, decreasing Toll-like receptor-2 (TLR2) expression (P. acnes triggers proinflammatory cytokine production by activating TLR2), increasing CD1d expression and decreasing interleukin (IL)-10 expression by keratinocytes.…”

“…[16][17][18] RARg is predominantly expressed in the epidermis. [13,17,20] Given that the development of microcomedones is the initial step in all acne lesions, the fact that adapalene inhibits microcomedone formation leads to a reduction in both comedones and inflammatory lesions. [13,17,20] Given that the development of microcomedones is the initial step in all acne lesions, the fact that adapalene inhibits microcomedone formation leads to a reduction in both comedones and inflammatory lesions.…”

“…[13,17,20] Given that the development of microcomedones is the initial step in all acne lesions, the fact that adapalene inhibits microcomedone formation leads to a reduction in both comedones and inflammatory lesions. [17,18,20] Adapalene also showed antiproliferative effects and comedolytic activity in animal models. [17,18,20] Adapalene also showed antiproliferative effects and comedolytic activity in animal models.…”

“…[5,21] In vitro, adapalene had antiproliferative effects and modulated cell differentiation, as well as inhibiting transglutaminase type I (an enzyme involved in the final stages of keratinocyte differentiation). [17,18,20] The anti-inflammatory activity of adapalene reflects inhibition of chemotactic and chemokine responses in human polymorphonuclear leukocytes, inhibition of lipoxygenase pathways, and inhibition of cyclo-oxygenase activity. [17,18,20] The anti-inflammatory activity of adapalene reflects inhibition of chemotactic and chemokine responses in human polymorphonuclear leukocytes, inhibition of lipoxygenase pathways, and inhibition of cyclo-oxygenase activity.…”