Nanoemulsion with tuneable lipid shell dedicated to targeted delivery of small and biomacro- molecules

A.C. Couffin, J. Bruniaux, T. Courant, A. Hoang, C. Martin, A. Fournier, F. Mittler, I. Texier, E. Sulpice, R. Auzély-Velty, X. Gidrol, F. Navarro
Commissariat à l'Energie Atomique et aux Energies Alternatives, FR

Keywords: nanoemulsion, surface decoration, biomacromolecules transport


Lipid nanocarriers are considered as suitable carriers to formulate lipophilic drugs, transport them and also deliver more specifically at appropriate biological sites. Based on oil-in-water template emulsion, we have been developing nanodroplets as drug or contrast agent nanocarriers. The outstanding long-term stability of these nano-sized emulsions was evidenced by monitoring at once the lipid-shell and lipid-core composition. Taking advantage of its colloidal behavior and high tolerability, we modulated the surface droplet to tailor make relevant nanocarriers and also transport various molecules such as large drugs, biomacromolecules. Cationic and anionic nanoparticles were prepared by incorporation of either hydrophobic-tailed polysaccharides or cationic lipids within the shell lipids. Such cationic formulations are suitable for the complexation of nucleic acids such as DNA or RNA as illustrated by gel retardation assays. Moreover, large biomacromolecules, such as proteins, peptides or antibodies are chemically grafted on nanoparticle surface via bioconjugation techniques using “home-made” PEGylated surfactants. For example, we have grafted cetuximab antibodies onto nanoparticle surface and demonstrated a receptor-mediated uptake on EGRF overexpressed cell lines confirming the selectivity of delivery thank to the presence of antibody. Further investigations are ongoing to complete in vivo validation for the selected applications (e.g. vaccination or large biomolecules transport)