title: Polyamine/salt-assembled microspheres coated with hyaluronic acid for targeting and pH sensing.
abstract: The poly(allylamine hydrochloride)/trisodium citrate aggregates were fabricated and further covalently crosslinked via the coupling reaction of carboxylic sites on trisodium citrate with the amine groups on polyamine, onto which poly-L-lysine and hyaluronic acid were sequentially assembled, forming stable microspheres. The pH sensitive dye and pH insensitive dye were further labeled to enable the microspheres with pH sensing property. Moreover, these microspheres could be specifically targeted to HeLa tumor cells, since hyaluronic acid can specifically recognize and bind to CD44, a receptor overexpressed on many tumor cells. Quantitative pH measurement by confocal laser scanning microscopy demonstrated that the microspheres were internalized into HeLa cells, and accumulated in acidic compartments. By contrast, only a few microspheres were adhered on the NIH 3T3 cells surface. The microspheres with combined pH sensing property and targeting ability can enhance the insight understanding of the targeted drug vehicles trafficking after cellular internalization.
authors.affiliation: MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Pan
authors.initials: P
authors.lastname: Zhang
authors.affiliation: MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Yang
authors.affiliation: MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Guojun
authors.initials: G
authors.lastname: Wang
authors.affiliation: MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China. Electronic address: tongwj@zju.edu.cn.
authors.forename: Weijun
authors.initials: W
authors.lastname: Tong
authors.affiliation: MOE Key Laboratory of Macromolecular Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou 310027, China.
authors.forename: Changyou
authors.initials: C
authors.lastname: Gao
mesh_terms: D000327:Adsorption; D000818:Animals; D001692:Biological Transport; D002234:Carbodiimides; D002951:Citrates / Q000737:chemistry*; D003432:Cross-Linking Reagents; D004337:Drug Carriers; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry; D015870:Gene Expression; D006367:HeLa Cells; D006801:Humans; D018960:Hyaluronan Receptors / Q000235:genetics / Q000378:metabolism; D006820:Hyaluronic Acid / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D051379:Mice; D008863:Microspheres; D041681:NIH 3T3 Cells; D009928:Organ Specificity; D011073:Polyamines / Q000737:chemistry*; D011107:Polylysine / Q000737:chemistry; D011485:Protein Binding; D012235:Rhodamines / Q000737:chemistry
chemical_list: C518491:1-ethyl-3-(3-(diethylamino)propyl)carbodiimide; C497483:CD44 protein, human; D002234:Carbodiimides; D002951:Citrates; D003432:Cross-Linking Reagents; D004337:Drug Carriers; D005456:Fluorescent Dyes; D018960:Hyaluronan Receptors; D011073:Polyamines; D012235:Rhodamines; C514290:trisodium citrate; D011107:Polylysine; C063994:polyallylamine; D006820:Hyaluronic Acid; C027755:rhodamine isothiocyanate; D016650:Fluorescein-5-isothiocyanate
keywords: Cellular uptake; Hyaluronic acid; Microspheres; Polyamine-salt assembly; Targeting; pH sensing