Abstract
Adapalene (ADP) is a representative of the third retinoids generation and successfully used in first-line acne treatment. ADP binds to retinoic acid nuclear receptors. The comedolytic, anti-inflammatory, antiproliferative, and immunomodulatory are the known ADP effects. Its safety profile is an advantage over other retinoids. ADP recently was found to be effective in the treatment of several dermatological diseases and photoaging besides the utility in the treatment of acne vulgaris. New biological effects of adapalene with therapeutic potential are highlighted in this review paper. Thus, adapalene could be a valuable therapeutic drug into the treatment of several types of cancer. Additionally, some neurodegenerative diseases could be treated with a suitable formulation for intravenous administration. The antibacterial activity against methicillin-resistant Staphylococcus aureus of an analogue of ADP has been proven. In different therapeutic schemes, ADP is more effective in combination with other active substances. New topical combinations with adapalene include ketoconazole (antifungal), mometasone furoate (anti-inflammatory corticosteroid), nadifloxacin (fluoroquinolone), and alfa and beta hydroxy acids. Combination with oral drugs is a new trend that enhances the properties of topical formulations with adapalene. Several studies have investigated the effects of ADP in co-administration with azithromycin, doxycycline, faropenem, isotretinoin, and valganciclovir. Innovative formulations of ADP also aim to achieve a better bioavailability, increased efficacy, and reduced side effects. In this review, we have highlighted the current studies on adapalene regarding biological effects useful in various treatment types. Adapalene has not been exploited yet to its full biological potential.
Highlights
The modern history of the retinoids begins in 1909, with the discovery of vitamin A in the egg yolk lipid extract
The antiproliferative effects of ADP were examined in vivo on xenograft tumors derived from human colorectal cancer cells subcutaneously [89]
One analogue of ADP shows antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA), probably due to adamantane that intercalates into the lipidic bacterial membrane [32]
Summary
The modern history of the retinoids begins in 1909, with the discovery of vitamin A in the egg yolk lipid extract. The first retinoids used in the treatment of acne and keratinization diseases were limited by the toxicity and adverse effects of first retinoids generation. Tretinoin was the first retinoid used topically in the treatment of acne, but with a high incidence of adverse effects. Adapalene (ADP) is a retinoid approved in 1996 by the U.S Food and Drug Administration (FDA) for the treatment of acne (trade name Differin, producer Galderma) with fewer side effects than tretinoin [2,3]. The structure of this paper comprises the updated data regarding ADP in the frame of retinoid class, mechanism of action, and structure–activity relationships (SAR) of ADP, biological effects, and the potential to treat numerous diseases, adverse reactions, and toxicity. Recent studies were analyzed to highlight the enhanced therapeutic potential of ADP in different combinations with other APIs and innovative pharmaceutical formulations.
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