Biosurfactants generated from lactic acid bacteria (LAB) offer an advantage over standard microbial surfactants due to their antifungal, antibacterial and antiviral capabilities. Many LAB strains have been related to the manufacture of biosurfactant, an essential chemical with uses in the treatment of a number of illnesses. Furthermore, their effectiveness as anti-adhesive agents against a diverse variety of pathogens proves their utility as anti-adhesive coating agents for medical insertional materials, reducing hospital infections without the need of synthetic drugs and chemicals. LAB produces both low and high molecular weight biosurfactants. Biosurfactants from , and have been reported to produce glycolipopeptides that comprise carbohydrates, proteins and lipids in the ratio of 1:3:6 with palmitic, stearic acid, and linoelaidic acid as the major fatty acid component, whereas has been reported to make surlactin due to the presence of non-ribosomal peptide synthetase genes (NRPS) genes. Antimicrobial activity of sophorolipids and rhamnolipids generated from LAB against , , , and has been demonstrated. The safety of biosurfactants is being evaluated in compliance with a number of regulatory standards that emphasize the importance of safety in the pharmaceutical industry. This review attempts, for the first time, to provide a comprehensive evaluation of several approaches for the synthesis of biosurfactant-mediated molecular modulation in terms of their biological value. Future biosurfactant directions, as well as regulatory considerations that are crucial for the synthesis of biosurfactants from novel LAB, have also been explored.