Background: Surfactants are an important category of additives that are used widely in most of the
formulations as solubilizers, stabilizers, and emulsifiers. Current drug delivery systems comprise of numerous
synthetic surfactants (such as Cremophor EL, polysorbate 80, Transcutol-P), which are associated with several
side effects though used in many formulations. Therefore, to attenuate the problems associated with conventional
surfactants, a new generation of surface-active agents is obtained from the metabolites of fungi, yeast, and
bacteria, which are termed as biosurfactants.
Objectives: In this article, we critically analyze the different types of biosurfactants, their origin along with
their chemical and physical properties, advantages, drawbacks, regulatory status, and detailed pharmaceutical
Methods: 243 papers were reviewed and included in this review.
Results: Briefly, Biosurfactants are classified as glycolipids, rhamnolipids, sophorolipids, trehalolipids, surfactin,
lipopeptides & lipoproteins, lichenysin, fatty acids, phospholipids, and polymeric biosurfactants. These
are amphiphilic biomolecules with lipophilic and hydrophilic ends and are used as drug delivery vehicles (foaming,
solubilizer, detergent, and emulsifier) in the pharmaceutical industry. Despite additives, they have some biological
activity as well (anti-cancer, anti-viral, anti-microbial, P-gp inhibition, etc.). These biomolecules possess
better safety profiles and are biocompatible, biodegradable, and specific at different temperatures.
Conclusion: Biosurfactants exhibit good biomedicine and additive properties that can be used in developing
novel drug delivery systems. However, more research should be driven due to the lack of comprehensive toxicity
testing and high production cost which limits their use.