Topical Rosacea Therapy: The Importance of Vehicles for Efficacy, Tolerability and Compliance

June 2011 | Volume 10 | Issue 6 | Original Article | 627 | Copyright © 2011

J. Mark Jackson MDa and Michelle Pelle MDb

aUniversity of Louisville, Division of Dermatology, Louisville, KY bMedDerm Associates, San Diego, CA; Division of Dermatology, University of San Diego Medical Center, San Diego, CA

Abstract

Many topical medications are available for the treatment of papulopustular rosacea. While treatments contain metronidazole, azelaic acid, or sodium sulfacetamide-sulfur as the active ingredient, the composition of the vehicle formulations varies widely. These vehicles come in gels, creams, lotions and foams; some ingredients are common to many vehicles, while some vehicles contain unique ingredients designed to optimize skin penetration and delivery of the active drug to its target. Vehicles can also influence tolerability, which is always a concern in patients with heightened skin sensitivity, and compliance, which is typically lower for topical treatments than oral treatments. Ideally, the vehicle of any rosacea treatment should enhance drug delivery, be nonirritating and be easy to use. Ingredients that help repair barrier function are also desirable. This review will focus on the key components of the vehicles from the most commonly used topical therapies for papulopustular rosacea and how vehicle formulations influence the delivery of active ingredient, skin barrier repair, tolerability and compliance.

J Drugs Dermatol. 2011;10(6):627-633.

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INTRODUCTION

Rosacea is a common facial disorder affecting approximately 16 million people in the United States.1 The facial skin of patients with rosacea is characterized by persistent erythema, visible blood vessels and often papules and pustules.2 Rosacea sufferers frequently experience skin sensitivity characterized by physical discomfort, burning sensation, facial itching, stinging and swelling.3 The lactic acid test involving application of a solution of lactic acid to the skin and assessing the subject's reaction is a validated test for determining skin sensitivity. Approximately 75 percent of patients with rosacea have a positive reaction to this test compared with <20 percent of normal subjects,4 demonstrating the prevalence of sensitive skin among rosacea sufferers. There are four main subtypes of rosacea: erythematotelangiectactic, papulopustular, phymatous and ocular.5 Available topical treatments are indicated for the treatment of papules, pustules and erythema.6

Topical medications comprise a major component of therapy for papulopustular rosacea. Currently, only one oral medication is approved by the Food and Drug Administration for the treatment of papulopustular rosacea, a subantimicrobial dose of doxycycline (Oracea®). In contrast, there are many topical medications to choose from that vary in active ingredient and vehicle, providing dermatologists with a wide array of treatment options. Ideally, treatment should not only deliver the active ingredient to its site of action but should not further irritate the skin, and medications that are potentially acnegenic should be avoided. Formulations that calm and soothe the skin are preferable. Emollient and barrier repair ingredients are important, as these may help repair inherent barrier dysfunction.

Other features that are important when choosing a therapy are its ease of application and its effect on the appearance of the skin when used with the patients' regular skin care routines, particularly the application of cosmetics. The ease of application and appearance of both the medication and patients' usual cosmetic regimens have been shown to influence patients' ratings of their overall appearance.7 Ideally, topical therapies should be well tolerated on oily and/or dry skin, as many patients display findings of both. A vehicle that is tolerated on both skin types allows for more flexibility of application.

It has been suggested that the vehicle of a topical therapy may account for 50 percent to 75 percent of its efficacy.8 A vehicle must allow penetration of the active ingredient, without damaging the skin barrier. It must deliver the correct dose, while being easy to use and well tolerated. This review will focus on commonly used topical therapies for papulopustular rosacea and the key components of their respective vehicles that influence the delivery of the active ingredient and repair of the skin barrier, and maximize tolerability. How these formulations are accepted in clinical practice will also be discussed.

Topical Rosacea Treatments and Their Vehicles

Three main active ingredients are found in topical rosacea therapies: metronidazole, azelaic acid, or sodium sulfacetamide-

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