Surfactants are amphipathic substances with lyophobic and lyophilic groups and are critical components in pharmaceutical products. Surfactants have several uses in pharmaceuticals, i) for solubilisation of hydrophobic drugs in aqueous media, ii) as components of emulsions ,iii) surfactant self-assembly vehicles for oral and transdermal drug delivery, iv) as plasticizers in semisolid delivery systems, and v) as agents to improve drug absorption and penetration. Non-ionic surfactants such as ethers of fatty alcohols are most commonly used in pharmaceuticals. Cationic surfactants are capable of exerting antibacterial properties by disrupting bacterial cell membranes. In pharmaceutical processing, phospholipid lecithin, bile salts, certain fatty acids and their derivatives have become indispensable since they afford a uniquely effective and eficient mechanism of drug carriage by solubilising the drugs of fatty origin. The antibacterial, antifungal and antiviral activities make biosurfactants relevant molecules for applications in combating many diseases and as therapeutic agents. Biosurfactants have the potential for use as major immunomodulatory molecules, as anti-adhesive biological coating for biomaterials, in vaccines and gene therapy, and they may be incorporated into probiotic preparations to combat urogenetical tract infections and pulmonary immunotherapy. Gemini surfactants are effective potential transfection agents for non-viral gene therapy. Ionic liquids act as secondary surfactants and the use of surfactant/ionic liquid systems should be explored to build speciic properties in the organized medium, and to explore pharmaceutical applications of traditional, biosurfactant and Gemini surfactants.