Glycolipid Biosurfactant as Multilamellar Vesicular Drug Carriers

Microbial amphiphiles, known as biosurfactants, are molecules obtained fermentation of yeasts or bacteria. Biobased and biodegradable, they have been historically developed for detergency formulations, whereas more recent work has shown their interest as antimicrobials or depollutants. However, their self-assembly properties and their interactions with macromolecules suggest a broader potential of applications. Drug encapsulation for anti-cancer purposes is a well-known application of lipids such as phospholipids. In this study, for the first time, a drug delivery system based on microbial amphiphiles is designed and tested against human cervical carcinoma HeLa cells. For this purpose, multilamellar wall vesicles (MLWV) consisting of microbial glucolipid (GC) amphiphiles and polylysine (PLL), attracted by electrostatic interactions, have been synthesized. Curcumin, a highly lipophilic molecule, has been used as natural drug model to evaluate the GCPLL MLWVs as potential nanocarrier to specifically deliver drugs into cancer cells. The curcumin loaded MLWVs uptake measured by flow cytometry is much higher in Hela cells (50%) compared to NHDF (35%) and THP-1 derived macrophages (20%). This uptake is correlated to cytotoxicity as cell viability only decreases for Hela cells (by 50%). A dedicated mechanistic study shows that the cytotoxic effect is based on MLWV fusion with the cell membrane and the curcumin release within the cellular cytoplasm. Taken together, these results demonstrate that microbial amphiphiles can be used to develop engineered drug delivery system to efficiently target cancer cells