title: Influence of Structural Features on the Cellular Uptake Behavior of Non-Targeted Polyester-Based Nanocarriers.
abstract: The development of delivery systems efficiently uptaken by cells is of due importance since sites of drug action are generally localized in subcellular compartments. Herein, naked and core-shell polymeric nanoparticles (NPs) have been produced from poly(lactic-co-glycolic acid)-PLGA, poly(ethylene oxide)-b-poly(ε-caprolactone)-PEO-b-PCL, and poly(ethylene oxide)-b-poly(lactic acid)-PEO-b-PLA. The nanostructures are characterized and the cellular uptake behavior is evaluated. The data evidence that cellular uptake is enhanced as the length of the hydrophilic PEO-stabilizing shell reduces and that high negative surface charge restricts cellular uptake. Furthermore, NPs of higher degree of hydrophobicity (PEO-b-PCL) are more efficiently internalized as compared to PEO-b-PLA NPs. Accordingly, taking into account our recent published results and the findings of the current investigation, there should be a compromise regarding protein fouling and cellular uptake as resistance to nonspecific protein adsorption and enhanced cellular uptake are respectively directly and inversely related to the length of the PEO-stabilizing shell.
authors.affiliation: Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170, Santo André, Brazil.
authors.forename: Carlos E
authors.initials: CE
authors.lastname: de Castro
authors.affiliation: Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170, Santo André, Brazil.
authors.forename: Jean-Jacques
authors.initials: JJ
authors.lastname: Bonvent
authors.affiliation: Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170, Santo André, Brazil.
authors.forename: Maria C C
authors.initials: MC
authors.lastname: da Silva
authors.affiliation: Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170, Santo André, Brazil.
authors.forename: Fabiane L F
authors.initials: FL
authors.lastname: Castro
authors.affiliation: Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, 09210-170, Santo André, Brazil.
authors.forename: Fernando C
authors.initials: FC
authors.lastname: Giacomelli
mesh_terms: D045744:Cell Line, Tumor; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D019344:Lactic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D053758:Nanoparticles / Q000737:chemistry*; D011091:Polyesters / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011100:Polyglycolic Acid / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013329:Structure-Activity Relationship
chemical_list: D011091:Polyesters; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C016240:polycaprolactone; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols
keywords: cellular uptake; confocal microscopy; flow cytometry; light scattering; polymeric nanoparticles