Arbutin, a naturally occurring hydroquinone, has gained attention for its diverse pharmacological properties. Traditional uses include blood sugar regulation and wound healing, while modern applications focus on its antioxidant and anti‐inflammatory effects. Its synthesis involves complex biochemical pathways, contributing to its unique characteristics. Pharmacokinetic studies have shed light on its absorption, distribution, metabolism, and excretion, crucial for understanding its efficacy. Toxicity concerns underscore the need for further research into its safety. Additionally, novel dosage forms of arbutin are explored, presenting innovative strategies to enhance its delivery and efficacy in therapeutic applications. Arbutin's pharmacological activities span antioxidant, anti‐inflammatory, and glucose metabolism regulation thus modulating various molecular pathways and targets, such as glucose transporter‐4, insulin‐like growth factor‐1 receptor, and adenosine monophosphate‐activated protein kinase, offering promising therapeutic avenues in medicine. This review covers arbutin comprehensively, encompassing its sources, chemical properties, synthesis methods, pharmacokinetics, pharmacological activities, food supplements, toxicity profiles, and novel dosage forms. By addressing these aspects, the review lays the groundwork for future research and development in natural therapeutics.