title: Self-Assembly Behavior of Emissive Urea Benzene Derivatives Enables Heat-Induced Accumulation in Tumor Tissue.
abstract: In this study we describe the construction of a system composed of thermally responsive molecules that can be induced to accumulate in tumor tissues by heating. EgX molecules consisting of an urea-benzene framework and oligoethylene glycol (OEG) functional groups with an emissive aminoquinoline formed nanoparticles (NPs) ∼10 nm in size at 23 °C with a fluorescence quantum yield of 7-10%. At higher temperatures, additional self-assembly occurred as a result of OEG dehydration, and the NPs grew to over 1000 nm in size; this was accompanied by low critical solution temperature behavior. EgXs accumulated in tumor tissues of mice at a body temperature of around 33-35 °C, an effect that was accelerated by external heating around the tumor to approximately 40 °C as a result of increased particle size and enhanced retention in tissue. These EgX NPs can serve as a tool for in vivo monitoring of tumor progression and response to treatment.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
authors.forename: Takeru
authors.initials: T
authors.lastname: Araki
authors.affiliation: Department of Molecular Imaging and Theranostics, National Institute of Radiological Sciences (NIRS) , QST, Anagawa 4-9-1, Inage, Chiba 263-8555, Japan.
authors.forename: Shuhei
authors.initials: S
authors.lastname: Murayama
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
authors.forename: Kazuteru
authors.initials: K
authors.lastname: Usui
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Shimada
authors.affiliation: Department of Molecular Imaging and Theranostics, National Institute of Radiological Sciences (NIRS) , QST, Anagawa 4-9-1, Inage, Chiba 263-8555, Japan.
authors.forename: Ichio
authors.initials: I
authors.lastname: Aoki
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyushu University , 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.|PRESTO, Japan Science and Technology Agency , Kawaguchi, 332-0012, Japan.
authors.forename: Satoru
authors.identifier: 0000-0002-3107-442X
authors.initials: S
authors.lastname: Karasawa
mesh_terms: D000634:Aminoquinolines / Q000737:chemistry; D000818:Animals; D001555:Benzene Derivatives / Q000737:chemistry*; D019855:Ethylene Glycol / Q000737:chemistry; D005456:Fluorescent Dyes / Q000737:chemistry*; D006358:Hot Temperature; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000000981:diagnostic imaging*; D061848:Optical Imaging; D010316:Particle Size; D013499:Surface Properties; D013816:Thermodynamics; D014018:Tissue Distribution; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry*
chemical_list: D000634:Aminoquinolines; D001555:Benzene Derivatives; D005456:Fluorescent Dyes; D014508:Urea; D019855:Ethylene Glycol
keywords: LCST; Self-assembly; fluorescence; nanoparticles; tumor imaging