title: Influence of diblock copolymer PCL-mPEG and of various iodinated oils on the formulation by the emulsion-solvent diffusion process of radiopaque polymeric nanoparticles.
abstract: 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.
authors.affiliation: Université Lyon 1, LAGEP, équipe de génie pharmacotechnique, UMR 5007, CNRS, CPE, 43 bd du 11 novembre, Villeurbanne, 69100, France; Université de Lyon, Lyon, 69622, France; Hospices Civils de Lyon, Lyon, 69229, France.
authors.forename: François
authors.initials: F
authors.lastname: Hallouard
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Briançon
authors.forename: Nicolas
authors.initials: N
authors.lastname: Anton
authors.forename: Xiang
authors.initials: X
authors.lastname: Li
authors.forename: Thierry
authors.initials: T
authors.lastname: Vandamme
authors.forename: Hatem
authors.initials: H
authors.lastname: Fessi
mesh_terms: D004058:Diffusion; D004655:Emulsions / Q000737:chemistry; D054879:Halogenation; D053758:Nanoparticles / Q000737:chemistry*; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*
chemical_list: D004655:Emulsions; D009821:Oils; D011091:Polyesters; C439611:methoxy poly(ethylene glycol-co-epsilon-caprolactone); D011092:Polyethylene Glycols
keywords: Emulsion- solvent diffusion process; Excipients; Formulation; Imaging methods; Iodinated oils; Nanoparticles; Poly(caprolactone)-m poly(ethylene glycol); Surfactants