Caffeine is a methylxanthine-class alkaloid with the chemical structure known as 1,3,7-trimethylxanthine. Its INCI (International Nomenclature of Cosmetic Ingredients) name is "Caffeine," and it is listed with Fragrance and Skin Conditioning functions in cosmetic ingredient databases. [3] Caffeine inhibits phosphodiesterase (PDE), the enzyme that breaks down cyclic adenosine monophosphate (cAMP) within adipocytes, thereby raising cAMP levels; as a result, a mechanism promoting the lipolysis pathway has been reported, and at the same time it is described as inducing capillary constriction and microcirculation stimulation through adenosine receptor antagonism. [1][2] In cosmetics, these multiple activities serve as the basis for its use across various areas, such as eye contour care and antioxidant and sun-support formulations.
Caffeine is an alkaloid first isolated and purified from coffee beans in 1820 by the German chemist Friedlieb Ferdinand Runge; following its study in pharmacology and food science, it began to be researched in earnest in the field of dermatology from the 1980s–1990s onward. [1] From the late 1990s, caffeine's PDE inhibition and cAMP elevation mechanisms were applied to research on topical cellulite products [7], and from the 2000s onward, quantitative studies on the human skin penetration kinetics of topical caffeine followed. [4] In the 2010s, clinical studies on care for dark circles and puffiness around the eyes [6] and clinical studies evaluating caffeine as an adjuvant in sunscreen formulations [9] were reported, expanding the research field beyond a simple stimulant ingredient to an eye-zone, antioxidant, and microcirculation-support ingredient. It is listed as a methylxanthine-class active ingredient in the European cosmetic ingredient database (COSMILE Europe) [3], and the U.S. PCPC guide information also compiles cases of its use in the cosmetics and OTC areas. [11]