Amine-modified Poly(vinyl alcohol) as a novel surfactant to modulate size and surface charge of Poly-Lactic-co-Glycolic Acid nanoparticles

Poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) represent a promising tool for effective delivery of biomacromolecules, thanks to their biodegradability and biocompatibility properties. PLGA NPs are often synthesized by emulsion-solvent evaporation method and Poly(vinyl) alcohol (PVA) represents one of the most commonly used surfactant. Although PVA-mediated synthesis of PLGA NPs is effective in tailoring NPs size and stability, the resulting negative surface charge can prevent both endosomal escape and biomacromolecules release in the cells cytosol. To overcome this limit, a novel surfactant (amino-PVA) with a cationic charge was synthesized and its potential for PLGA NPs formulation investigated. In either single (oil-in-water) or double (water-in-oil-in-water) emulsion synthesis, different mixtures of PVA and amino-PVA were studied, by monitoring their effects on NPs size and surface charge. The optimized properties were obtained by the combination of 0.975% w/v of PVA with 0.025% w/v of amino-PVA. This formulation has been further investigated for degradation properties and cytocompatibility. High stability and low cytotoxicity made the system promising for the encapsulation and release of hydrophilic drugs and biomacromolecules.