Abstract
A novel method was developed for the one-pot synthesis of ultrafine poly(lactic-co-glycolicacid) nanoparticles (PLGA NPs), using an emulsion solvent evaporation formulationmethod. Using either cetyltrimethylammonium bromide (CTAB) or poly(ethyleneglycol)-distearyl phosphoethanolamine (PEGPE) as an oily emulsifier during the emulsionprocess, produced PLGA particle sizes of less than 50 nm, constituting a breakthrough inemulsion formulation methods. The yield of ultrafine PLGA NPs increased withPEGPE/PLGA ratio, reaching a plateau at around 85%, when thePEGPE/PLGA ratio reached 3:1. The PEGPE–PLGA NPs exhibited high drug loading content, reducedburst release, good serum stability, and enhanced cell uptake rate compared withtraditional PLGA NPs. Sub-50 nm diameter PEG-coated ultrafine PLGA NPs show greatpotential for in vivo drug delivery systems.
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