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Near-infrared fluorophores for imaging, targeting and therapy
현훈 한국공업화학회 2015 한국공업화학회 연구논문 초록집 Vol.2015 No.0
To be clinically viable, the ideal NIR fluorophore requires certain optical properties, including excitation and emission □800 nm, and a high extinction coefficient and quantum yield in serum. To date, every NIR fluorophore described in the literature suffers from two fundamental flaws: 1) hepatic clearance, which results in NIR fluorescence signal throughout the GI tract that persists for hours, and/or 2) non-specific background uptake in normal tissues, which typically persists for hours and results in a low signal-to-background ratio (SBR). The goal of this work is to develop a new class of ideal NIR fluorophores that can be injected into the bloodstream. These fluorophores would “stick” to tumors and other diseased tissue, but not to normal tissue. Currently, we are developing on the synthesis of optimized NIR fluorophores for in vivo and surgical imaging, on validating their use as targeted diagnostic agents for various diseases including cancer. Completion of these aims will lay the foundation for future clinical testing during imageguided surgery.
Native Tissues-Specific Near-Infrared Fluorophores for Image-Guided Surgery
현훈,조단비 한국공업화학회 2016 한국공업화학회 연구논문 초록집 Vol.2016 No.1
Our initial efforts to prepare tissue-specific near-infrared (NIR) fluorescent compounds generated successful correlation between physicochemical properties and global uptake in major organs after systemic circulation and biodistribution. Herein, we focus on the effects on biodistribution based on modulating electronic influencing moieties from donating to withdrawing moieties at both the heterocyclic site and through meso-substitution of pentamethine cyanine fluorophores. These selected modifications harnessed innate biodistribution pathways through the structure-inherent targeting, resulting in effective imaging of the adrenal glands, pituitary gland, lymph nodes, pancreas, and thyroid and salivary glands. These native-tissue contrast agents will arm surgeons with a powerful and versatile arsenal for intraoperative NIR imaging in real time.
Design of Near-Infrared Fluorophores for Target-Specific Imaging
현훈,이지민 한국공업화학회 2016 한국공업화학회 연구논문 초록집 Vol.2016 No.1
Near-infrared (NIR) fluorophores are emerging in optical imaging as sensitive, cost-effective, and nonharmful alternatives to current agents that emit harmful ionizing radiation. Developing spectrally distinct NIR fluorophores to visualize sensitive vital tissues to selectively avoid them during surgical resection of diseased tissue is of great significance. Herein, we report the synthetic variation of pentamethine cyanine fluorophores with modifications of physicochemical properties toward prompting tissue-specific uptake into sensitive tissues (i.e., endocrine glands). Tissue-specific targeting and biodistribution studies revealed localization of contrast agents in the adrenal and pituitary glands, pancreas, and lymph nodes with dependence on molecular characteristics. These NIR contrast agents have potential for clinical translation for intraoperative imaging in the delineation of delicate glands.
현훈,이성수,임원봉,조단비,정진석,조가영,김소연,이덕원,엄세욱,양대혁,전흥재 한국공업화학회 2019 Journal of Industrial and Engineering Chemistry Vol.70 No.-
In this study, we prepared a beta-cyclodextrin (β-CD)-based carrier consisting of β-CD, polyethyleneglycol (PEG) and folic acid (FA) (CDPF) for improved doxorubicin (DOX) delivery to targeted breast cancerin vitro and in vivo. The morphology and size distribution were characterized by transmission electronmicroscopy (TEM) and dynamic light scattering (DLS) measurements, which revealed in particles rangingfrom 38 nm to 52 nm in size. DOX from CDPF was released in a sustained manner for 48 h. Cell viabilityanalysis showed the low toxicity of free DOX, whereas CDPF-DOX remarkably exhibited reduced viabilityafter incubation for 7 days. In vivo animal test showed that intravenous injection of CDPF-DOXcontributes to decreased tumor volume, along with no systemic toxicity and cardiotoxicity. The resultssuggested that CDPF can maximize the efficacy of DOX delivery; therefore can be used as a goodcandidate for developing optimal drug delivery systems.