Bilosomes are novel vesicular colloidal carrier that contains bile salts as one of the main components. Recently, bilosomes have gained significant attention as a drug delivery system due to the reported flexibility and stability, relative to other traditional vesicular carriers. As bile salts are natural endogenous surfactants, their presence in bilosomes imparts important characteristics to the vesicles such as biodegradability, compatibility, and minimal toxicity. Bilosomes were investigated for drug delivery through different routes of administration (such as transdermal, ocular, nose to brain) with improved therapeutic efficacy of the entrapped drug. This minireview attempted to present a brief overview on the application of bilosomes in oral delivery of drug. When administered orally, the presence of bile salts in the main structure of bilosomes offers benefits over other vesicular systems. Bile salts provide protection to the vesicles against the effect of endogenous bile salts with improved therapeutic performance of the entrapped active pharmaceutical ingredient(s).