title: PEGylated Nanoemulsions for Oral Delivery: Role of the Inner Core on the Final Fate of the Formulation.
abstract: Since the past decade, there has been growing interest to grant nanoparticles with diffusion properties across mucosae. In this sense, the nonionic block copolymer Pluronic F127 (PF127) has emerged as a promising coating agent to formulate mucus-penetrating particles. In the journey to find efficient coating agents, researchers have focused more on the effect of the coating agent architecture rather than on the role of the physicochemical properties of the nanoparticle used as the substrate. The current knowledge about mucodiffusive particles is in general based on model-like nanoparticles, such as polystyrene or poly(lactic-co-glycolic) acid nanoparticles, but there is a lack of information about the potential of PF127 on other colloidal systems. This work aims to shed some light on this issue by selecting three oils, palm (solid), coconut (semisolid), and wheat germ (liquid), with different physicochemical properties to formulate PF127-coated nanoemulsions. The obtained nanoemulsions were characterized, and their colloidal stability was tested. Their diffusion capacity was determined by particle tracking after challenging the nanoemulsions across an intestinal porcine mucus layer. In accordance with the evidence of model-like nanoparticles, our results state that PF127 allows mucodiffusion, but its effectiveness as a coating agent clearly depends on the physicochemical properties of the nanostructure core over which PF127 is placed. Among other physicochemical properties, the results certainly showed that the hydrophobic character of the nanostructure core emerges as a critical factor in the formulation of successful PF127 coatings.
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: M J
authors.initials: MJ
authors.lastname: Santander-Ortega
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: M
authors.initials: M
authors.lastname: Plaza-Oliver
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: V
authors.initials: V
authors.lastname: Rodríguez-Robledo
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: L
authors.initials: L
authors.lastname: Castro-Vázquez
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: N
authors.initials: N
authors.lastname: Villaseca-González
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: J
authors.initials: J
authors.lastname: González-Fuentes
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: E L
authors.initials: EL
authors.lastname: Cano
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: P
authors.initials: P
authors.lastname: Marcos
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: M V
authors.identifier: 0000-0001-7774-732X
authors.initials: MV
authors.lastname: Lozano
authors.affiliation: Cellular Neurobiology and Molecular Chemistry of the Central Nervous System Group, Faculty of Pharmacy, ‡Regional Centre of Biomedical Research (CRIB), and §Quantitative Methods and Socio-Economic Development Group, Institute for Regional Development (IDR), University of Castilla-La Mancha (UCLM) , Albacete 02071, Spain.
authors.forename: M M
authors.initials: MM
authors.lastname: Arroyo-Jiménez
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000074263:Coconut Oil / Q000737:chemistry; D004058:Diffusion; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D009093:Mucus / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D000073878:Palm Oil / Q000737:chemistry; D010194:Pancreatin / Q000737:chemistry; D010316:Particle Size; D010434:Pepsin A / Q000737:chemistry; D010938:Plant Oils / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*; D013552:Swine; D024502:alpha-Tocopherol / Q000737:chemistry
chemical_list: D004655:Emulsions; D005079:Excipients; D010938:Plant Oils; D013501:Surface-Active Agents; D020442:Poloxamer; C050055:wheat germ oil; D000073878:Palm Oil; D010194:Pancreatin; D010434:Pepsin A; D024502:alpha-Tocopherol; D000074263:Coconut Oil