Biosurfactants are natural amphiphilic molecules obtained from natural sources that have gained significant attention as sustainable and biocompatible compared to synthetic surfactants in novel drug delivery systems. Their ability to reduce surface and interfacial tension, self-assemble into micelles or vesicles, and stabilize emulsions makes them valuable tools for enhancing the solubility, stability, and bioavailability of therapeutic agents. Structurally diverse classes such as glycolipids, lipopeptides, phospholipids, and polymeric biosurfactants exhibit various physicochemical and biological properties. When incorporated into novel systems, biosurfactants improve encapsulation efficiency and controlled release. Their antimicrobial, anticancer, and wound-healing properties further extend their biomedical relevance. As natural, eco-friendly excipients, biosurfactants represent a bridge between biotechnology and pharmaceutical innovation, providing a pathway toward safer and sustainable drug delivery platforms.