Influence of diblock copolymer PCL-mPEG and of various iodinated oils on the formulation by the emulsion-solvent diffusion process of radiopaque polymeric nanoparticles.

This pioneer study in the domain of blood pool contrast media formulation presents the influence of poly-ɛ-caprolactone-monomethoxy poly(ethylene glycol) (PCL-mPEG) and oils on the formulation of polymeric nanoparticles by emulsion-solvent diffusion. The nature of the oil used had no influence on the encapsulation rate, even if particles were formulated with a mix of PCL/PCL-mPEG. It did, however, influence the particle size and polydispersity, with macroglycerides appearing to be the lipid structure best suited to obtain the smallest monodisperse particles. When we used PCL-mPEG to form a PEG-hydrated layer to surround the nanoparticles, its tension active property had a favorable effect on particle size and polydispersity. We also showed the strong deleterious effect on particle size and polydispersity when the polymer proportion was increased to over 1% (w/v) in the pre-emulsion organic phase. Conversely, increasing the oil proportion in this organic phase simply resulted in a slight to insignificant deleterious effect on size and polydispersity, enabling the oil proportion to be enhanced up to 3% (w/v). Finally, we showed the favorable combined effect of oil iodination and the presence of PCL-mPEG on particles formulated by emulsion-solvent diffusion leading to the preparation of smaller polymeric iodine-containing particles.
(© 2013 Wiley Periodicals, Inc. and the American Pharmacists Association.)