title: [Mechanism of cellular uptake and transport mediated by integrin receptor targeting trimethyl chitosan nanoparticles].
abstract: This study investigated a nano drug delivery system built by one sort of modified trimethyl chitosan (TMC). The TMC was modified by cRGDyk, ligand of integrin receptor avβ3. Single factor screening was used to optimize the prescription in which the particle sizes of TMC nanoparticle (TMC NPs) and cRGDyk modified TMC nanoparticle (C-TMC NPs) were (240.3 ± 4.2) nm and (259.5 ± 3.3) nm. Electric potential of those two nanoparticles were (33.5 ± 0.8) mV and (25.7 ± 1.6) mV. Encapsulation efficiencies were (76.0 ± 2.2) % and (74.4 ± 2.0) %. Drug loading efficacies were (50.1 ± 2.1) % and (26.1 ± 1.0) %. Then the cellular uptake, uptake mechanism and transport efficacy of TMC NPs and C-TMC NPs were investigated using Caco-2 cell line. The uptake rate and accumulating drug transit dose of C-TMC NPs were 1.98 and 2.84 times higher than TMC NPs, separately. Mechanism investigations revealed that caveolae-mediated endocytosis, clathrin-mediated endocytosis and macropinocytosis were involved in the intercellular uptake of both TMC NPs and C-TMC NPs. What is more, free cRGDyk could remarkably inhibit the uptake of C-TMC NPs.
authors.forename: Juan
authors.initials: J
authors.lastname: Xu
authors.forename: Chong
authors.initials: C
authors.lastname: Liu
authors.forename: Yi-ning
authors.initials: YN
authors.lastname: Xu
authors.forename: Wei
authors.initials: W
authors.lastname: Shan
authors.forename: Min
authors.initials: M
authors.lastname: Liu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Huang
mesh_terms: D001692:Biological Transport; D018938:Caco-2 Cells; D021941:Caveolae; D048271:Chitosan / Q000737:chemistry*; D002966:Clathrin; D004705:Endocytosis; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000737:chemistry*; D053758:Nanoparticles; D010316:Particle Size; D010873:Pinocytosis
chemical_list: D002966:Clathrin; D039302:Integrin alphaVbeta3; C118071:N-trimethyl chitosan chloride; D048271:Chitosan