18F-Labeled perfluorocarbon droplets for positron emission tomography imaging.

Abstract:

INTRODUCTION:Nanoscale perfluorocarbon (PFC) droplets have been used to create imaging agents and drug delivery vehicles. However, development and characterization of new formulations of PFC droplets are hindered because of the lack of simple methods for quantitative and sensitive assessment of whole body tissue distribution and pharmacokinetics of the droplets. To address this issue, a general-purpose method for radiolabeling the inner core of nanoscale perfluorocarbon droplets with a hydrophobic and lipophobic fluorine-18 compound was developed, so that positron emission tomography (PET) and quantitative biodistribution studies can be employed to evaluate PFC nanodroplets in vivo. METHODS:A robust method to produce [18F]CF3(CF2)7(CH2)3F from a tosylate precursor using [18F]F- was developed. The product's effectiveness as a general label for different PFCs and its ability to distinguish the in vivo behavior of different PFC droplet formulations was evaluated using two types of PFC nanodroplets: fluorosurfactant-stabilized perfluorohexane (PFH) nanodroplets and lipid-stabilized perfluorooctylbromide (PFOB) nanodroplets. In vivo assessment of the 18F-labeled PFH and PFOB nanodroplets were conducted in normal mice following intravenous injection using small animal PET imaging and gamma counting of tissues and fluids. RESULTS:[18F]CF3(CF2)7(CH2)3F was produced in modest yield and was stable with respect to loss of fluoride in vitro. The labeled fluorocarbon was successfully integrated into PFH nanodroplets (~175 nm) and PFOB nanodroplets (~260 nm) without altering their mean sizes, size distributions, or surface charges compared to their non-radioactive analogues. No leakage of the radiolabel from the nanodroplets was detected after droplet formation in vitro. PET imaging and biodistribution data for the two droplet types tested showed significantly different tissue uptake and clearance patterns. CONCLUSION:A convenient method for producing 18F-labeled PFC droplets was developed. The results highlight the potential utility of the strategy for pre-clinical evaluation of different PFC droplet formulations through direct PFC core labeling using a fluorinated radiolabel.

journal_name

Nucl Med Biol

authors

Amir N,Green D,Kent J,Xiang Y,Gorelikov I,Seo M,Blacker M,Janzen N,Czorny S,Valliant JF,Matsuura N

doi

10.1016/j.nucmedbio.2017.07.001

subject

Has Abstract

pub_date

2017-11-01 00:00:00

pages

27-33

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(17)30125-7

journal_volume

54

pub_type

杂志文章
  • Evaluation of a chloride-based 89Zr isolation strategy using a tributyl phosphate (TBP)-functionalized extraction resin.

    abstract:INTRODUCTION:The remarkable stability of the 89Zr-DOTA complex has been shown in recent literature. The formation of this complex appears to require 89Zr-chloride as the complexation precursor rather than the more conventional 89Zr-oxalate. In this work we present a method for the direct isolation of 89Zr-chloride from...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2018.06.003

    authors: Graves SA,Kutyreff C,Barrett KE,Hernandez R,Ellison PA,Happel S,Aluicio-Sarduy E,Barnhart TE,Nickles RJ,Engle JW

    更新日期:2018-01-01 00:00:00

  • An original radio-biomimetic approach to synthesize radiometabolites for PET imaging.

    abstract::To fully exploit the potential of positron emission tomography (PET) imaging to assess drug distribution and pharmacokinetics in the central nervous system, the contribution of radiometabolites to the PET signal has to be determined for correct interpretation of data. However, radiosynthesis and extensive study of rad...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2020.08.001

    authors: Auvity S,Breuil L,Goislard M,Bottlaender M,Kuhnast B,Tournier N,Caillé F

    更新日期:2020-01-01 00:00:00

  • Metabolism of receptor targeted 111In-DTPA-glycoproteins: identification of 111In-DTPA-epsilon-lysine as the primary metabolic and excretory product.

    abstract::The hepatic and renal retention of indium-111 (111In) from 111In-labeled polypeptides has been the subject of many investigations. Because the lysosome is a common intracellular destination for the degradation of polypeptides, we studied the lysosomal metabolism of 111In-DTPA-labeled glycoproteins targeted to cell sur...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/0969-8051(94)90174-0

    authors: Franano FN,Edwards WB,Welch MJ,Duncan JR

    更新日期:1994-11-01 00:00:00

  • Comparison of N-[(11)C]methyl-norchloroepibatidine and N-[(11)C]methyl-2-(2-pyridyl)-7-azabicyclo[2.2.1]heptane with N-[(11)C]methyl-epibatidine in small animal PET studies.

    abstract::Structural variations of the nicotinic acetylcholine receptor radioligand N-[(11)C]methyl-epibatidine were made to form (11)C-labeled N-methyl-norchloroepibatidine (N-methyl-NorchloroEPB) and N-methyl-2-(2-pyridyl)-7-azabicyclo[2.2.1]heptane (N-methyl-2PABH). Radiosyntheses were performed by methylation with high radi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00080-9

    authors: Spang JE,Patt JT,Westera G,Schubiger PA

    更新日期:2000-04-01 00:00:00

  • 2-[18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors.

    abstract::The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAC...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(98)00031-6

    authors: Horti AG,Scheffel U,Koren AO,Ravert HT,Mathews WB,Musachio JL,Finley PA,London ED,Dannals RF

    更新日期:1998-10-01 00:00:00

  • Fluorine-18-labeled fluorine gas for synthesis of tracer molecules.

    abstract::The aim of this work was to develop a method to produce 18F-labeled fluorine gas ([18F]F2) with high specific radioactivity (SA, radioactivity/mass-ratio). 18F-Labeled methyl fluoride ([18F]CH3F) was synthesized from [18F]F-aq and mixed with carrier F2 in an inert neon matrix. The constituents were atomized in an elec...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00078-4

    authors: Bergman J,Solin O

    更新日期:1997-10-01 00:00:00

  • Functional neuroanatomy of the basal ganglia as studied by dual-probe microdialysis.

    abstract::Dual probe microdialysis was employed in intact rat brain to investigate the effect of intrastriatal perfusion with selective dopamine D1 and D2 receptor agonists and with c-fos antisense oligonucleotide on (a) local GABA release in the striatum; (b) the internal segment of the globus pallidus and the substantia nigra...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(98)00066-3

    authors: O'Connor WT

    更新日期:1998-11-01 00:00:00

  • High-resolution imaging of brain 5-HT 1B receptors in the rhesus monkey using [11C]P943.

    abstract::The serotonin 5-HT(1B) receptors regulate the release of serotonin and are involved in various disease states, including depression and schizophrenia. The goal of the study was to evaluate a high affinity and high selectivity antagonist, [(11)C]P943, as a positron emission tomography (PET) tracer for imaging the 5-HT(...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.10.007

    authors: Nabulsi N,Huang Y,Weinzimmer D,Ropchan J,Frost JJ,McCarthy T,Carson RE,Ding YS

    更新日期:2010-02-01 00:00:00

  • An alumina ceramic target vessel for the remote production of metallic radionuclides by in situ target dissolution.

    abstract:INTRODUCTION:As the use of metallic radionuclides increases, so does the demand for a simple production method. In this study, we demonstrated an in situ target processing concept for automated metallic radionuclide production without the use of any robotic device. METHODS:An alumina ceramic vessel for a vertical irra...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2012.05.010

    authors: Nagatsu K,Suzuki H,Fukada M,Minegishi K,Tsuji A,Fukumura T

    更新日期:2012-11-01 00:00:00

  • Improved detection and measurement of low levels of [18F]fluoride metabolized from [18F]-labeled pyrimidine nucleoside analogues in biological samples.

    abstract:INTRODUCTION:It is important to identify all circulating metabolites, including free fluoride, for accurate pharmacokinetic modeling of [(18)F]-labeled radiotracers. We sought to determine the most efficient method to detect and quantify low levels of free [(18)F]fluoride in biological samples. METHODS:Low levels of [...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2011.05.008

    authors: Paolillo V,Yeh HH,Mukhopadhyay U,Gelovani JG,Alauddin MM

    更新日期:2011-11-01 00:00:00

  • A novel 177Lu-labeled porphyrin for possible use in targeted tumor therapy.

    abstract:INTRODUCTION:Porphyrin and its derivatives exhibit inherent affinity for localization in tumors. Hence, porphyrin derivatives radiolabeled with suitable therapeutic radionuclides could be envisaged as potential agents for targeted tumor therapy. In this direction, a water-soluble porphyrin derivative, viz., 5,10,15,20-...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2010.02.007

    authors: Das T,Chakraborty S,Sarma HD,Banerjee S,Venakatesh M

    更新日期:2010-07-01 00:00:00

  • Synthesis and in vivo evaluation of [(11)C]CGP62349, a new GABA(B) receptor antagonist.

    abstract::This paper describes the radiosynthesis of [(11)C]CGP62349, a potential ligand to assess GABA(B) receptors in vivo. (11)C was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(00)00124-4

    authors: Todde S,Moresco RM,Fröstl W,Stampf P,Matarrese M,Carpinelli A,Magni F,Galli Kienle M,Fazio F

    更新日期:2000-08-01 00:00:00

  • 64Cu-Labeled tetraiodothyroacetic acid-conjugated liposomes for PET imaging of tumor angiogenesis.

    abstract:INTRODUCTION:We synthesized and evaluated (64)Cu-labeled tetraiodothyroacetic acid (tetrac)-conjugated liposomes for PET imaging of tumor angiogenesis, because tetrac inhibits angiogenesis via integrin αVβ3. METHODS:Tetrac-PEG-DSPE and DOTA-PEG-DSPE were synthesized and formulated with other lipids into liposomes. The...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2013.08.003

    authors: Kang CM,Koo HJ,Lee S,Lee KC,Oh YK,Choe YS

    更新日期:2013-11-01 00:00:00

  • [1-11C]octanoate as a potential PET tracer for studying glial functions: PET evaluation in rats and cats.

    abstract::To evaluate the ability of [1-11C]octanoate as a PET tracer for imaging the brain, we examined its distribution in the brain and surrounding tissues in rats and cats with PET. In rats, owing to the accumulated radioactivity in the harderian glands, clear brain images were not obtained at rostral levels. In cats, the b...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(96)00148-5

    authors: Kuge Y,Kawashima H,Yamazaki S,Hashimoto N,Miyake Y

    更新日期:1996-11-01 00:00:00

  • Comparative uptakes and biodistributions of internalizing vs. noninternalizing copper-64 radioimmunoconjugates in cell and animal models of colon cancer.

    abstract::Copper-64-labeled monoclonal antibodies (mAbs) have previously demonstrated unexpectedly effective tumor control in rodent models of cancer at relatively low tumor-absorbed radiation doses. This property has been associated with delivery platforms resulting in cellular internalization. The purpose of the present studi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2005.05.006

    authors: Bryan JN,Jia F,Mohsin H,Sivaguru G,Miller WH,Anderson CJ,Henry CJ,Lewis MR

    更新日期:2005-11-01 00:00:00

  • Production of Zr-89 using sputtered yttrium coin targets 89Zr using sputtered yttrium coin targets.

    abstract::An increasing interest in zirconium-89 (89Zr) can be attributed to the isotope's half-life which is compatible with antibody imaging using positron emission tomography (PET). The goal of this work was to develop an efficient means of production for 89Zr that provides this isotope with high radionuclidic purity and spe...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.03.004

    authors: Queern SL,Aweda TA,Massicano AVF,Clanton NA,El Sayed R,Sader JA,Zyuzin A,Lapi SE

    更新日期:2017-07-01 00:00:00

  • Evaluation of [11C]laniquidar as a tracer of P-glycoprotein: radiosynthesis and biodistribution in rats.

    abstract::At present, P-glycoprotein (P-gp) function can be studied using positron emission tomography (PET) together with a labelled P-gp substrate such as R-[11C]verapamil. Such a tracer is, however, less suitable for investigating P-gp (over)expression. Laniquidar is a third-generation P-gp inhibitor, which has been used in ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.03.004

    authors: Luurtsema G,Schuit RC,Klok RP,Verbeek J,Leysen JE,Lammertsma AA,Windhorst AD

    更新日期:2009-08-01 00:00:00

  • Cytotoxic and genotoxic effect of the [166Dy]Dy/166Ho-EDTMP in vivo generator system in mice.

    abstract::Multiple myeloma and other hematological malignancies have been treated by myeloablative radiotherapy/chemotherapy and subsequent stem cell transplantation. [(166)Dy]Dy/(166)Ho-ethylenediaminetetramethylene phosphonate (EDTMP) forms a stable in vivo generator system with selective skeletal uptake in mice; therefore, i...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2004.08.010

    authors: Pedraza-López M,Ferro-Flores G,Arteaga de Murphy C,Morales-Ramírez P,Piedras-Ross J,Murphy-Stack E,Hernández-Oviedo O

    更新日期:2004-11-01 00:00:00

  • Synthesis of L-2,4-diamino[4-11C]butyric acid and its use in some in vitro and in vivo tumour models.

    abstract::L-2,4-Diamino[4-11C]butyric acid (DAB) was synthesized by an enzyme catalysed carrier added (0.1 micromol KCN) reaction of hydrogen [11C]cyanide with O-acetyl-L-serine followed by reduction. L-[11C]DAB was obtained with a radiochemical purity higher than 96% and with a decay corrected radiochemical yield of 30-40% wit...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00032-2

    authors: Antoni G,Omura H,Bergström M,Furuya Y,Moulder R,Roberto A,Sundin A,Watanabe Y,Långström B

    更新日期:1997-08-01 00:00:00

  • New bis(dithiocarboxylato) nitridotechnetium-99m radiopharmaceuticals for leucocyte labelling: in vitro and in vivo studies.

    abstract::Dithiocarboxylate ligands were synthesized and characterised. New nitrido 99m-technetium complexes were obtained with these ligands and identified by thin layer chromatography. The nitrido complexes were tested in vitro in whole blood for leucocyte labelling and the design of the ligand was optimized. Best results wer...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00025-5

    authors: Demaimay F,Noiret N,Roucoux A,Patin H,Bellande E,Pasqualini R,Moisan A

    更新日期:1997-07-01 00:00:00

  • An electrochemical approach for removal of radionuclidic contaminants of Eu from 153Sm for effective use in metastatic bone pain palliation.

    abstract:INTRODUCTION:Thermal neutron activation of 152Sm [152Sm(n,γ)153Sm] using natural or isotopically enriched (by 152Sm) samarium target is the established route for production of 153Sm used for preparation of 153Sm-EDTMP for pain palliation in cancer patients with disseminated bone metastases. However, some long-lived rad...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.11.010

    authors: Chakravarty R,Chakraborty S,Khan MS,Ram R,Sarma HD,Dash A

    更新日期:2018-03-01 00:00:00

  • Evaluation of nigrostriatal damage and its change over weeks in a rat model of Parkinson's disease: small animal positron emission tomography studies with [(11)C]beta-CFT.

    abstract:INTRODUCTION:The cardinal pathological feature of Parkinson's disease (PD) is progressive loss of dopaminergic neurons. Since dopamine transporter (DAT) is a protein located presynaptically on dopaminergic nerve terminals, radioligands that bind to these sites are promising radiopharmaceuticals for evaluation of the in...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2009.06.005

    authors: Liu L,Wang Y,Li B,Jia J,Sun Z,Zhang J,Tian J,Wang X

    更新日期:2009-11-01 00:00:00

  • Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy.

    abstract::We report herein the preparation and biological evaluation of two radioastatinated biotin conjugates, (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide. Both conjugates were stable in the presence of human serum and cerebrospinal fluid as well as murine serum, indicating ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00166-2

    authors: Foulon CF,Alston KL,Zalutsky MR

    更新日期:1998-02-01 00:00:00

  • Synthesis and biological evaluation of 68Ga-bis-DOTA-PA as a potential agent for positron emission tomography imaging of necrosis.

    abstract:INTRODUCTION:Necrosis is a form of cell death that occurs in a variety of pathological conditions but can also be the result of therapy in cancer treatment. A radiotracer that could image necrotic cell death using PET could therefore be a useful tool to provide relevant information on the disease activity or therapeuti...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2013.04.011

    authors: Prinsen K,Cona MM,Cleynhens BJ,Li J,Vanbilloen H,Dyubankova N,Lescrinier E,Ni Y,Bormans GM,Verbruggen AM

    更新日期:2013-08-01 00:00:00

  • 18F-fluoro-2-deoxyglucose PET informs neutrophil accumulation and activation in lipopolysaccharide-induced acute lung injury.

    abstract:INTRODUCTION:Molecular imaging of the earliest events related to the development of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) could facilitate therapeutic development and patient management. We previously reported that 18F-fluoro-2-deoxyglucose (18F-FDG) PET identifies ALI/ARDS prior to radiogr...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.01.005

    authors: Rodrigues RS,Bozza FA,Hanrahan CJ,Wang LM,Wu Q,Hoffman JM,Zimmerman GA,Morton KA

    更新日期:2017-05-01 00:00:00

  • Dual radiolabeled liposomes: biodistribution studies and localization of focal sites of infection in rats.

    abstract::Liposomes encapsulating both glutathione and deferoxamine were labeled with 99mTc-HMPAO and 111In-oxine at the same time. These dual radiolabeled liposomes were intravenously injected in rats with S. aureus infection in thigh. The target-to-background ratio (T/BG) increased from 2.9 at 2 h to 4.4 at 8 h in 99mTc image...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(97)00162-5

    authors: Awasthi VD,Goins B,Klipper R,Phillips WT

    更新日期:1998-02-01 00:00:00

  • Evaluation of a bromine-76-labeled progestin 16alpha,17alpha-dioxolane for breast tumor imaging and radiotherapy: in vivo biodistribution and metabolic stability studies.

    abstract:INTRODUCTION:Progesterone receptors (PRs) are present in many breast tumors, and their levels are increased by certain endocrine therapies. They can be used as targets for diagnostic imaging and radiotherapy. METHOD:16alpha,17alpha-[(R)-1'-alpha-(5-[(76)Br]Bromofurylmethylidene)dioxyl]-21-hydroxy-19-norpregn-4-ene-3,2...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2008.05.001

    authors: Zhou D,Sharp TL,Fettig NM,Lee H,Lewis JS,Katzenellenbogen JA,Welch MJ

    更新日期:2008-08-01 00:00:00

  • Sigma1 and dopamine D2 receptor occupancy in the mouse brain after a single administration of haloperidol and two dopamine D2-like receptor ligands.

    abstract::We investigated sigma(1) and dopamine D(2) receptor occupancy in mouse brain after a single injection of haloperidol, nemonapride, or spiperone using [(11)C]SA4503 and [(11)C]raclopride, respectively. Co-injection of the three compounds significantly blocked the uptake of each radioligand. Six hours later, only halope...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/s0969-8051(03)00003-9

    authors: Ishiwata K,Kawamura K,Kobayashi T,Matsuno K

    更新日期:2003-05-01 00:00:00

  • Radiosynthesis and biological evaluation of N-(2-[18F]fluoropropionyl)-3,4-dihydroxy-l-phenylalanine as a PET tracer for oncologic imaging.

    abstract:INTRODUCTION:Several 11C and 18F labeled 3,4-dihydroxy-l-phenylalanine (l-DOPA) analogues have been used for neurologic and oncologic diseases, especially for brain tumors and neuroendocrine tumors PET imaging. However, 18F-labeled N-substituted l-DOPA analogues have not been reported so far. In the current study, radi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2017.04.002

    authors: Tang C,Nie D,Tang G,Gao S,Liu S,Wen F,Tang X

    更新日期:2017-07-01 00:00:00

  • Chemical design of a radiolabeled gelatinase inhibitor peptide for the imaging of gelatinase activity in tumors.

    abstract::Since elevated levels of gelatinases [matrix metalloproteinase (MMP)-2 and MMP-9] are associated with a poor prognosis in cancer patients, these enzymes are potential targets for tumor imaging. In the present study, a cyclic decapeptide, cCTTHWGFTLC (CTT), was selected as a mother compound because of its selective inh...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章

    doi:10.1016/j.nucmedbio.2007.04.002

    authors: Hanaoka H,Mukai T,Habashita S,Asano D,Ogawa K,Kuroda Y,Akizawa H,Iida Y,Endo K,Saga T,Saji H

    更新日期:2007-07-01 00:00:00