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Betulinic acid (BA), a naturally occurring plant‐derived pentacyclic triterpenoid, has gained attention in recent years owing to its broad‐spectrum biological and medicinal properties. Despite the pharmacological activity of BA, it has been associated with some drawbacks, such as poor aqueous solubility and short half‐life in vivo, which limit therapeutic application. To solve these problems, much work in recent years has focused on enhancing BA's aqueous solubility, half‐life, and efficacy by using nanoscale drug delivery systems. Several different kinds of nanoscale delivery systems—including polymeric nanoparticles, magnetic nanoparticles, liposomes, polymeric conjugates, nanoemulsions, cyclodextrin complexes, and carbon nanotubes—have been developed for the delivery of BA. Here, we focus on the recent developments of novel nanoformulations used to deliver BA in order to improve its efficacy.