A cosmeceutical should be represented a topical preparation sold as a cosmetic but with an observable pharmaceutical action. Retinoids define a class of substances comprising vitamin A (retinol) and its naturally and synthetic derivatives. Retinoic acid is oxidized to a less active metabolite, 4-oxoretinoic acid, or converted to retinoyl glucuronide, whereas retinol is converted to retinyl glucuronide. Vitamin A is present in the epidermis as free and esterified retinol at an average concentration of 1–2 nmol/g. Natural retinoids may be efficient when used in topical application, but they are irritant and unstable following exposure to the sunlight. The genomic effects of topical retinoids are the consequence of the modulation of gene expression following their binding to nuclear retinoic acid receptor or retinoid X receptors. Retinol and retinyl esters have been incorporated into many skin products. Cosmeceutical retinoids may be useful in the treatment of skin aging, acne, and pigmentation disorders.