Topical retinoids represent a mainstay of acne treatment because they expel mature comedones, reduce microcomedone formation, and exert anti-inflammatory effects. The first-generation retinoid tretinoin (all-trans retinoic acid) and the synthetic third-generation polyaromatics adapalene and tazarotene are approved for acne treatment by the US FDA, whereas topical tretinoin, isotretinoin (13-cis retinoic acid), and adapalene are accredited in Canada and Europe. Topical retinoids have a favorable safety profile distinct from the toxicity of their systemic counterparts. Local adverse effects, including erythema, dryness, itching, and stinging, occur frequently during the early treatment phase. Their impact varies with the vehicle formation, skin type, frequency and mode of application, use of moisturizers, and environmental factors such as sun exposure or temperature. The broad anti-acne activity and safety profile of topical retinoids justifies their use as first-line treatment in most types of non-inflammatory and inflammatory acne. They are also suitable as long-term medications, with no risk of inducing bacterial resistance, for maintenance of remission after cessation of initial combination therapy.

Topical retinoids in acne vulgaris: update on efficacy and safety.

The emergence of oral and topical retinoids was a major advance in the clinical management of acne vulgaris. However, the benefits of these agents were somewhat limited by the degree of side effects caused by these drugs. Over the last 15 years, researchers have sought compounds that can provide the manifold therapeutic benefits obtained with tretinoin and isotretinoin while minimizing the potential for irritation and other unwanted effects. Adapalene, a naphthoic-acid derivative, is one result of this search, and it serves as an example of rational drug development: the formulation of a novel substance with specific pharmacological properties and clinical objectives in mind. These goals included enhancing stability, enhancing anti-inflammatory effects, maintaining effectiveness and minimizing cutaneous irritation. This paper reviews the history of the development of adapalene, its unique physical and biochemical properties, and the pharmacological studies that demonstrate a wide range of retinoid-receptor, genetic and anti-inflammatory effects, all of which contribute to the therapeutic efficacy and improved tolerability of adapalene observed in the clinical use of this agent for the treatment of acne.

Adapalene biochemistry and the evolution of a new topical retinoid for treatment of acne.

Adapalene, a naphthoic acid derivative with retinoid-like activity is used for the topical treatment of mild to moderate acne vulgaris. It binds to retinoic acid receptors found predominantly in the terminal differentiation zone of epidermis and is more active than tretinoin in modulating cellular differentiation. Adapalene exhibits anti-inflammatory activity in various in vitro and in vivo models. To dates adapalene 0.1% gel and lotion formulations have been compared only with tretinoin 0.025% gel. In these comparisons, adapalene 0.1% aqueous gel was at least as effective as tretinoin and in some studies was significantly better at reducing the numbers of non inflammatory, inflammatory and total facial lesions in patients with mild to moderate acne. In such comparisons, the cutaneous tolerability of adapalene aqueous gel was generally better than that of tretinoin. On the basis of published data, adapalene aqueous 0.1% gel is an effective and generally better tolerated alternative to tretinoin 0.025% gel for the topical treatment of patients with mild to moderate acne.

Adapalene. A review of its pharmacological properties and clinical potential in the management of mild to moderate acne.

Retinoids have increasingly gained acceptance for single agent or adjuvant therapy to treat dermatological diseases such as acne, photoageing, cutaneous neoplasia, psoriasis, disorders of keratinisation and various skin cancers. As potent biological modulators which regulate numerous cellular processes, retinoids have been administered as both chemotherapeutic and chemopreventive agents and offer a viable alternative to classical cancer chemotherapy. Although retinoid treatment has shown considerable promise, certain side-effects have limited chronic administration. As a result of recent discoveries regarding the biological function of retinoids and retinoid receptors, several new treatment strategies have been developed, including the application of receptor selective synthetic retinoids, combination therapies with other hormones or chemotherapeutic agents, and novel formulations. This has resulted in a new generation of retinoids and retinoid treatments which are in clinical development and which exhibi...

Section Review: Retinoids: Biological Function and Use in the Treatment of Dermatological Diseases: Pulmonary-Allergy, Dermatological, Gastrointestinal & Arthritis

BACKGROUND: Topical retinoids are highly effective treatments for acne vulgaris. The various formulations and concentrations available allow physicians to tailor therapies to individual patient's needs and minimize the cutaneous irritation that is often observed with the use of these drugs. OBJECTIVE: To compare the efficacy and safety of tretinoin gel microsphere 0.1% with adapalene gel 0.1% in the treatment of acne vulgaris. METHODS: A 12-week double-blind study was conducted, and patients were evaluated at baseline and at weeks 2, 3, 4, 6, 8, 10, and 12. RESULTS: Although the two drugs displayed similar efficacy in the resolution of acne lesions at 12 weeks, a significantly greater reduction in the number of comedones was seen at week 4 among patients treated with tretinoin gel microsphere ( p = 0.047). Patients receiving tretinoin gel microsphere had an increased incidence of dryness (weeks 8 and 10) and peeling (weeks 3, 6, 8, and 10) compared with those patients treated with adapalene gel, but the t...

A comparative trial of two retinoids commonly used in the treatment of acne vulgaris.

The histological and ultrastructural effects following 3 weeks' topical treatment with two agents (all-trans retinoic acid and a new synthetic retinoid-like substance, CD271) were evaluated on the epidermis and the epithelial wall of the pseudocomedones in rhino mouse skin. The comedolytic effects of these drugs were similar, and consisted of a reduction of the utricular diameter, with normalization of follicular units. Morphological examinations revealed a hyperplastic response with an increase in the number of cell layers of both epidermis and follicular epithelium, and modifications in keratinocyte differentiation. Ultrastructural changes in the epidermis and epithelial wall were observed mainly in the granular and horny layers, with increased desquamation, and a decrease in the cohesiveness of corneocytes. During the first week of treatment, some cutaneous toxic effects were noticed, but they normalized within two weeks. On the other hand, a fine granular material persisted in the intercellular spaces. It is confirmed that the skin of the rhino mouse is a good model for the evaluation of the comedolytic effects of drugs. Moreover, it reveals the specific effects of retinoids on epidermal differentiation. We have demonstrated that topically applied CD271 induces modifications similar to those obtained with all-trans retinoic acid. It is thus concluded that CD271 is a potentially effective anti-acne agent.

The rhino mouse model: the effects of topically applied all-trans retinoic acid and CD271 on the fine structure of the epidermis and utricle wall of pseudocomedones

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The rhino mouse model: the effects of topically applied all-trans retinoic acid and CD271 on the fine structure of the epidermis and utricle wall of pseudocomedones