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Wilde runderen grazen in enkele gebieden tussen de rivier en dijk (uiterwaarden) als een vorm van natuurbeheer. Sommige dieren worden geslacht om de grootte en samenstelling van de kuddes goed te houden. Het vlees wordt verkocht als 'wildernisvlees'. In 2020 zijn in het vlees van enkele wilde runderen te hoge hoeveelheden dioxinen gemeten. Dit komt door de dioxinen en dioxine-achtige PCB (polychlorobiphenyls)’s in het gras en in de grond in uiterwaarden. Het RIVM en Wageningen Food Safety Research hebben daarom modellen ontwikkeld om te berekenen hoeveel van deze stoffen via gras en grond in het vlees van deze runderen terechtkomen. Hiermee is ook geschat hoe lang het duurt voordat de hoeveelheden op het toegestane niveau komen als de runderen naar een gebied buiten de uiterwaarden worden verplaatst. Daar zijn de concentraties lager. De modellen zijn ontwikkeld voor drie typen wilde runderen in een kudde: runderen die geen melk geven, runderen die melk geven, en kalveren. Voor de berekeningen zijn metingen in gras en bodem in de uiterwaarden in de buurt van Beuningen gebruikt. Er is gerekend met hoge concentraties in gras die vlak na een overstroming zijn gemeten. Daarnaast is met lagere concentraties gerekend, die vaker voorkomen. De concentraties in gras zijn na een overstroming vaak hoger doordat slib dat achterblijft op het gras, dioxinen en dioxine-achtige PCB’s bevat. De gemeten concentraties in de bodem waren in beide situaties ongeveer hetzelfde. Zowel bij de hogere als de lagere concentraties kwamen de berekende hoeveelheden in het vlees van alle drie typen wilde runderen boven de hoeveelheid uit die wettelijk is toegestaan. Wanneer koeien hun kalveren melk gaven, zaten de hoeveelheden in het vlees van deze koeien onder de wettelijke grens. Dat komt omdat dioxinen en dioxine-achtige PCB’s via de melk worden uitgescheiden. Na de verplaatsing naar een schoner gebied daalden de berekende hoeveelheden. Bij volwassen runderen kwamen ze binnen anderhalve tot vier maanden tot onder de toegestane hoeveelheid. Bij kalveren duurde het langer dan zes maanden. Dioxinen en dioxine-achtige PCB’s zijn chemische stoffen die bij (vuil)verbranding zijn ontstaan. Ondanks de sterk gedaalde uitstoot in de laatste 25 jaar, komen ze nog steeds voor in Nederland. Bijvoorbeeld in gras, de bodem en rivierslib. Dioxinen kunnen schadelijk zijn voor het immuunsysteem, de ontwikkeling van de hersenen, en de voortplanting.

International audience; HypothesisPoly(2-alkyl/aryl-oxazoline)s (PAOx) have seen a resurgence of interest in the new millennium due to their biocompatibility, low toxicity, and higher tunability compared to poly(ethylene glycol)s (PEG)s. Due to the straightforward access to hydrophilic and hydrophobic PAOx, it was hypothesized that amphiphilic PAOx should be capable of stabilizing oil/water (O/W) interfaces. Furthermore, the control of their composition, chain length, and monomer distribution could suggest the formulation of tunable emulsions. Special emphasis was given to evaluate whether spontaneously formed amphiphilic gradient copolymer could stabilize O/W emulsions.ExperimentsWe prepared a series of amphiphilic block and gradient copolymers based on 2-methyl-2-oxazoline and 2-phenyl-2-oxazoline with variable hydrophilic/lipophilic balance, degree of polymerization, and monomer distribution as basis to explore their ability to stabilize emulsions. Systematic granulometry, stability, and rheology studies were performed to characterize the final emulsions.FindingsRemarkably, stable O/W emulsions are obtained with only 0.5 wt% of copolymers. The finer emulsions stabilized by the most hydrophilic copoly(2-oxazoline)s allow an adjustment of their texture, as well as the concentration increase and oil content. Importantly, emulsion properties prepared with gradient copolymers show similar behavior compared with their block counterparts offering easy access to new biocompatible emulsifiers as these gradient copolymers are spontaneously formed by statistical copolymerization.

Efficient polymer-protein conjugation is a crucial step in the design of many therapeutic protein formulations including nanoscopic vaccine formulations, antibody-drug conjugates and to enhance the in vivo behaviour of proteins. Here we aimed at preparing well-defined polymers for conjugation to proteins by reversible addition-fragmentation chain transfer (RAFT) polymerization of both acrylates and methacrylamides with protein-reactive chain transfer agents (CTAs). These RAFT agents contain either a N-hydroxysuccinimide (NHS) or pentafluorophenyl (PFP) ester moiety that can be conjugated to lysine residues, and alternatively a maleimide (MAL) or pyridyl disulfide (PDS) moiety that can be conjugated to cysteine residues. Efficiency of the bioconjugation of these polymers to bovine and avian serum albumin was investigated as a function of stoichiometry, polymer molecular weight and the presence of reducing agents. A large molar excess of polymer was required to obtain an acceptable degree of protein conjugation. However, protein modification with N-succinimidyl-S-acetylthiopropionate (SATP) to introduce sulfhydryl groups onto primary amines, significantly increased conjugation efficiency with MAL- and PDS-containing polymers.

A strained dibenzoazacyclooctyne (DIBAC) derivative was introduced for the preparation of a rotaxane by strain-promoted azide-alkyne cycloaddition (SPAAC), also referred to as a copper-free click reaction. The DIBAC can efficiently act as a bulky reactive chain stopper to transform a pseudorotaxane architecture consisting of a diazo-functionalized dialkoxy-naphthalene guest and a tetracationic cyclobis(paraquat-p-phenylene) (CBPQT(4+)) host into the corresponding [2]rotaxane. Furthermore, the use of the DIBAC is demonstrated to be limited to short rigid macrocycles, as it is unable to act as stopper for a rotaxane featuring a larger crown ether macrocyclic host.

OP03 Selective extraction of medically-related radionuclides from proton-irradiated thorium targets, V. Radchenko, J.W. Engle, C. Roy, J. Griswold, M.F. Nortier, E.R. Birnbaum, M. Brugh, S. Mirzadeh, K. D. John, M.E. Fassbender, OP04 Comparison of [68Ga]FSC(succ-RGD)3 and [68Ga]NODAGA-RGD for PET imaging of αvβ3 integrin expression, Chuangyan Zhai, Gerben M. Franssen, Milos Petrik, Peter Laverman, Clemens Decristoforo, OP05 A new NPY-Y1R targeting peptide for breast cancer PET imaging, Ait-Mohand Samia, Dumulon-Perreault Véronique, Guérin Brigitte, OP06 The influence of multivalency on CCK 2 receptor targeting, D. Summer, A. Kroess, C. Rangger, H. Haas, P. Laverman, F. Gerben, E. von Guggenberg, C.Decristoforo, OP07 SPECT Imaging of αvβ3 Expression by [99mTc(N)PNP43]- Bifunctional Chimeric RGD Peptide not Cross-Reacting with αvβ5, Cristina Bolzati, Nicola Salvarese, Fiorenzo Refosco, Laura Meléndez-Alafort, Debora Carpanese, Antonio Rosato, Michele Saviano, Annarita Del Gatto, Daniela Comegna, Laura Zaccaro, OP09 New dienophiles for the inverse-electron-demand Diels-Alder reaction and for pretargeted PET imaging, Emilie Billaud, Muneer Ahamed, Frederik Cleeren, Elnaz Shahbazali, Tim Noël, Volker Hessel, Alfons Verbruggen and Guy Bormans, OP10 New complexing agent for Al18F-labelling of heat-sensitive biomolecules: Synthesis and preclinical evaluation of Al18F-RESCA1-HAS, Cleeren F, Lecina J, Koole M, Verbruggen A and Bormans G, OP11 A novel versatile precursor efficient for F-18 radiolabelling via click-chemistry, B. Lugatoa, S. Stucchia, E.A. Turollaa, L. Giulianoa, S.Toddea, P. Ferraboschib, OP12 A general applicable method to quantify unidentified UV impurities in radiopharmaceuticals, R.P. Klok, M.P.J. Mooijer, N.H. Hendrikse, A.D. Windhorst, OP13 Development of [18F]Fluoro-C-glycosides to radiolabel peptides, Collet C., Petry N., Chrétien F., Karcher G., Pellegrini-Moïse N., Lamandé-Langle S., OP14 A Microfluidic Approach for the 68Ga-labeling of PSMAHBED-CC and NODAGA-RGD, Sarah Pfaff, Cecile Philippe, Markus Mitterhauser, Marcus Hacker, Wolfgang Wadsak, OP16 Surprising reactivity of astatine in the nucleophilic substitution of aryliodonium salts: application to the radiolabeling of antibodies, François Guérard, Yong-Sok Lee, Sébastien Gouard, Kwamena Baidoo, Cyrille Alliot, Michel Chérel, Martin W. Brechbiel, Jean-François Gestin, OP17 64Cu-NOTA-pertuzumab F(ab')2 fragments, a second-generation probe for PET imaging of the response of HER2-positive breast cancer to trastuzumab (Herceptin), Lam K, Chan C, Reilly RM, OP18 Development of radiohalogenated analogues of a avb6-specific peptide for high LET particle emitter targeted radionuclide therapy of cancer, Salomé Paillas, John Marshall, Jean-Pierre Pouget, Jane Sosabowski, OP19 Ligand Specific Efficiency (LSE) as a guide in tracer optimization, Emmanuelle Briard, Yves P. Auberson, John Reilly, Mark Healy, David Sykes, OP23 The radiosynthesis of an 18F-labeled triglyceride, developed to visualize and quantify brown adipose tissue activity, Andreas Paulus, Wouter van Marken Lichtenbelt,Felix Mottaghy, Matthias Bauwens, OP24 Influence of the fluorescent dye on the tumor targeting properties of dual-labeled HBED-CC based PSMA inhibitors, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, OP25 [18F]MEL050 as a melanin PET tracer : fully automated radiosynthesis and evaluation for the detection of pigmented melanoma in mice pulmonary metastases, Chaussard M, Hosten B, Vignal N, Tsoupko-Sitnikov V, Hernio N, Hontonnou F, Merlet P, Poyet JL, Sarda-Mantel L, Rizzo-Padoin N, OP26 Design and Preclinical Evaluation of Novel Radiofluorinated PSMA Targeting Ligands Based on PSMA-617, J. Cardinale, M. Schäfer, M. Benešová, U. Bauder-Wüst, O. Seibert, F. Giesel, U. Haberkorn, M. Eder, K. Kopka, OP27 A novel radiolabeled peptide for PET imaging of prostate cancer: 64Cu-DOTHA2-PEG-RM26, Mansour Nematallah, Paquette Michel, Ait-Mohand Samia, Dumulon-Perreault Véronique, Lecomte Roger, Guérin Brigitte, OP29 Biodistribution of [18F]Amylovis®, a new radiotracer PET imaging of β-amyloid plaques, Fernandez-Maza L, Rivera-Marrero S, Prats Capote A, Parrado-Gallego A, Fernandez-Gomez I, Balcerzyk M, Sablon-Carrazana M, Perera-Pintado A, Merceron-Martinez D, Acosta-Medina E, Rodriguez-Tanty C, OP30 Synthesis and preclinical evaluation of [11C]-BA1 PET tracer for the imaging of CSF-1R, Bala Attili, Muneer Ahamed, Guy Bormans, OP31 In vivo imaging of the MCHR1 in the ventricular system via [18F]FE@SNAP, C. Philippe, M. Zeilinger, T. Scherer, C. Fürnsinn, M. Dumanic, W. Wadsak, M. Hacker, M. Mitterhauser, OP32 Synthesis of the first carbon-11 labelled P2Y12 receptor antagonist for imaging the anti-inflammatory phenotype of activated microglia, B. Janssen, D.J. Vugts, G.T. Molenaar, U. Funke, P.S. Kruijer, F. Dollé, G. Bormans, A.A. Lammertsma, A.D. Windhorst, OP33 Radiosynthesis of a selective HDAC6 inhibitor [11C]KB631 and in vitro and ex vivo evaluation, Koen Vermeulen, Muneer Ahamed, Michael Schnekenburger, Mathy Froeyen, Dag Erlend Olberg, Marc Diederich, Guy Bormansa, OP34 Improving metabolic stability of fluorine-18 labelled verapamil analogues, Raaphorst RM, Luurtsema G, Lammertsma AA, Elsinga PH, Windhorst AD, OP36 Development of a novel PET tracer for the activin receptor-like kinase 5, Lonneke Rotteveel, Uta Funke, Peter ten Dijke, Harm Jan Bogaard, Adriaan A. Lammertsma, Albert D. Windhorst, OP37 SPECT imaging and biodistribution studies of 111In-EGF-Au-PEG nanoparticles in vivo, Lei Song, Sarah Able, Nadia Falzone, Veerle Kersemans, Katherine Vallis, OP38 Melanoma targeting with [99mTc(N)(PNP3)]-labeled NAPamide derivatives: preliminary pharmacological studies, Davide Carta, Nicola Salvarese, Wiebke Sihver, Feng Gao, Hans Jürgen Pietzsch, Barbara Biondi, Paolo Ruzza, Fiorenzo Refosco, Cristina Bolzati, OP39 [68Ga]NODAGA-RGD: cGMP synthesis and data from a phase I clinical study, Roland Haubner, Armin Finkensted, Armin Stegmair, Christine Rangger, Clemens Decristoforo, Heinz Zoller, Irene J. Virgolin, OP44 Implementation of a GMP-grade radiopharmacy facility in Maastricht, Ivo Pooters, Maartje Lotz, Roel Wierts, Felix Mottaghy, Matthias Bauwens, OP45 Setting up a GMP production of a new radiopharmaceutical, Forsback, Sarita, Bergman Jörgen, Kivelä Riikka, OP48 In vitro and in vivo evaluation of 68-gallium labeled Fe3O4-DPD nanoparticles as potential PET/MRI imaging agents, M. Karageorgou, M. Radović, C. Tsoukalas, B. Antic, M. Gazouli, M. Paravatou-Petsotas, S. Xanthopouls, M. Calamiotou, D. Stamopoulos, S. Vranješ-Durić, P. Bouziotis, OP49 Fast PET imaging of inflammation using 68Ga-citrate with Fe-containing salts of hydroxy acids, A. S. Lunev, A. A. Larenkov, K.A. Petrosova, O. E. Klementyeva, G. E. Kodina, PP01 Installation and validation of 11C-methionine synthesis, Kvernenes, O.H., Adamsen, T.C.H., PP02 Fully automated synthesis of 68Ga-labelled peptides using the IBA Synthera® and Synthera® Extension modules, René Martin, Sebastian Weidlich, Anna-Maria Zerges, Cristiana Gameiro, Neva Lazarova, Marco Müllera, PP03 GMP compliant production of 15O-labeled water using IBA 18 MeV proton cyclotron, Gert Luurtsema, Michèl de Vries, Michel Ghyoot, Gina van der Woude, Rolf Zijlma, Rudi Dierckx, Hendrikus H. Boersma, Philip H. Elsinga, PP04 In vitro Nuclear Imaging Potential of New Subphthalocyanine and Zinc Phthalocyanine, Fatma Yurt Lambrecht, Ozge Er, Mine Ince, Cıgır Biray Avci, Cumhur Gunduz, Fatma Aslihan Sarı, PP05 Synthesis, Photodynamic Therapy Efficacy and Nuclear Imaging Potential of Zinc Phthalocyanines, Kasim Ocakoglu, Ozge Er, Onur Alp Ersoz, Fatma Yurt Lambrecht, Mine Ince, Cagla Kayabasi, Cumhur Gunduz, PP06 Radio-U(H)PLC – the Search on the Optimal Flow Cell for the γ-Detector, Torsten Kniess, Sebastian Meister, Steffen Fischer, Jörg Steinbach, PP07 Radiolabeling, characterization & biodistribution study of cysteine and its derivatives with Tc99m, Rabia Ashfaq, Saeed Iqbal, Atiq-ur-Rehman, Irfan ullah Khan, PP08 Radiolabelling of poly (lactic-co.glycolic acid) (PLGA) nanoparticles with 99mTC, R Iglesias-Jerez, Cayero-Otero, L. Martín-Banderas, A. Perera-Pintado, I. Borrego-Dorado, PP09 Development of [18F]PD-410 as a non-peptidic PET radiotracer for gastrin releasing peptide receptors, Ines Farinha-Antunes, Chantal Kwizera, Enza Lacivita, Ermelinda Lucente, Mauro Niso, Paola De Giorgio, Roberto Perrone, Nicola A. Colabufo, Philip H. Elsinga, Marcello Leopoldo, PP10 An improved nucleophilic synthesis of 2-(3,4-dimethoxyphenyl)-6-(2-[18F]fluoroethoxy) benzothiazole ([18F]FEDMBT), potential diagnostic agent for breast cancer imaging by PET, V.V. Vaulina, O.S. Fedorova, V.V. Orlovskaja, ?�.L. Chen, G.Y. Li, F.C. Meng, R.S. Liu, H.E. Wang, R.N. Krasikova, PP11 Internal radiation dose assessment of radiopharmaceuticals prepared with accelerator-produced 99mTc, Laura Meléndez-Alafort, Mohamed Abozeid, Guillermina Ferro-Flores, Anna Negri, Michele Bello, Nikolay Uzunov, Martha Paiusco, Juan Esposito, Antonio Rosato, PP12 A specialized five-compartmental model software for pharmacokinetic parameters calculation, Laura Meléndez-Alafort, Cristina Bolzati, Guillermina Ferro-Flores, Nicola Salvarese, Debora Carpanese, Mohamed Abozeid, Antonio Rosato, Nikolay Uzunov, PP13 Molecular imaging of the pharmacokinetic behavior of low molecular weight 18F-labeled PEtOx in comparison to 89Zr-labeled PEtOx, Palmieri L, Verbrugghen T, Glassner M, Hoogenboom R, Staelens S, Wyffels L, PP14 Towards nucleophilic synthesis of the α-[18F]fluoropropyl-L-dihydroxyphenylalanine, V. V. Orlovskaja, O. F. Kuznetsova, O. S. Fedorova, V. I. Maleev, Yu. N. Belokon, A. Geolchanyan, A. S. Saghyan, L. Mu, R. Schibli, S. M. Ametamey, R. N. Krasikova, PP15 A convenient one-pot synthesis of [18F]clofarabine, Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, PP16 BODIPY-estradiol conjugates as multi-modality tumor imaging agents, Samira Osati,Michel Paquette,Simon Beaudoin,Hasrat Ali,Brigitte Guerin, Jeffrey V. Leyton, Johan E. van Lier, PP17 Easy and high yielding synthesis of 68Ga-labelled HBED-PSMA and DOTA-PSMA by using a Modular-Lab Eazy automatic synthesizer, Di Iorio V, Iori M, Donati C, Lanzetta V, Capponi PC, Rubagotti S, Dreger T, Kunkel F, Asti M, PP18 Synthesis and evaluation of fusarinine C-based octadentate bifunctional chelators for zirconium-89 labelling, Chuangyan Zhai, Christine Rangger, Dominik Summer, Hubertus Haas, Clemens Decristoforo, PP19 Fully automated production of [18F]NaF using a re-configuring FDG synthesis module., Suphansa Kijprayoon, Ananya Ruangma, Suthatip Ngokpol, Samart Tuamputsha, PP20 Extension of the Carbon-11 Small Labeling Agents Toolbox and Conjugate Addition, Ulrike Filp, Anna Pees, Carlotta Taddei, Aleksandra Pekošak, Antony D. Gee, Alex J. Poot, Albert D. Windhorst, PP21 In vitro studies on BBB penetration of pramipexole encapsulated theranostic liposomes for the therapy of Parkinson’s disease, Mine Silindir Gunay, A. Yekta Ozer, Suna Erdogan, Ipek Baysal, Denis Guilloteau, Sylvie Chalon, PP22 Factors affecting tumor uptake of 99mTc-HYNIC-VEGF165, Filippo Galli, Marco Artico, Samanta Taurone, Enrica Bianchi, Bruce D. Weintraub, Mariusz Skudlinski, Alberto Signore, PP23 Rhenium-188: a suitable radioisotope for targeted radiotherapy, Nicolas Lepareur, Nicolas Noiret, François Hindré, Franck Lacœuille, Eric Benoist, Etienne Garin, PP24 Preparation of a broad palette of 68Ga radiopharmaceuticals for clinical applications, Trejo-Ballado F, Zamora-Romo E, Manrique-Arias JC, Gama-Romero HM, Contreras-Castañon G, Tecuapetla-Chantes RG, Avila-Rodriguez MA, PP25 68Ga-peptide preparation with the use of two 68Ge/68Ga-generators, H. Kvaternik, D. Hausberger, C. Zink, B. Rumpf, R. M. Aigner, PP26 Assay of HEPES in 68Ga-peptides by HPLC, H. Kvaternik, D. Hausberger, B. Rumpf, R. M. Aigner, PP27 Preparation, in vitro and in vivo evaluation of a 99mTc(I)-Diethyl Ester (S,S)-Ethylenediamine- N,N´-DI-2-(3-Cyclohexyl) Propionic acid as a target-specific radiopharmaceutical, Drina Janković, Mladen Lakić, Aleksandar Savić, Slavica Ristić, Nadežda Nikolić, Aleksandar Vukadinović, Tibor J. Sabo, Sanja Vranješ-Đurić, PP28 90Y-labeled magnetite nanoparticles for possible application in cancer therapy, S. Vranješ-Đurić, M. Radović, D. Janković, N. Nikolić, G. F. Goya, P. Calatayud, V. Spasojević, B. Antić, PP29 Simplified automation of the GMP production of 68Ga-labelled peptides, David Goblet, Cristiana Gameiro, Neva Lazarova, PP30 Combining commercial production of multi-products in a GMP environment with Clinical & R&D activities, Cristiana Gameiro, Ian Oxley, Antero Abrunhosa, Vasko Kramer, Maria Vosjan, Arnold Spaans, PP31 99mTc(CO)3-labeling and Comparative In-Vivo Evaluation of Two Clicked cRGDfK Peptide Derivatives, Kusum Vats, Drishty Satpati, Haladhar D Sarma, Sharmila Banerjee, PP32 Application of AnaLig resin for 99mTc separation from molybdenum excess, Wojdowska W., Pawlak D.W., Parus L. J., Garnuszek P., Mikołajczak R., PP33 Constraints for selection of suitable precursor for one-step automated synthesis of [18F]FECNT, the dopamine transporter ligand, Pijarowska-Kruszyna J, Jaron A, Kachniarz A, Malkowski B, Garnuszek P, Mikolajczak R, PP34 Gamma scintigraphy studies with 99mTc- amoxicillin sodium in bacterially infected and sterile inflamed rats, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP35 Preparation of 99mTc- Amoxicillin Sodium Lyophilized Kit, Derya Ilem-Ozdemir, Oya Caglayan-Orumlu, Makbule Asikoglu, PP36 Outfits of Tracerlan FXC-PRO for 11C-Labeling, Arponen Eveliina, Helin Semi, Saarinen Timo, Vauhkala Simo, Kokkomäki Esa, Lehikoinen Pertti, PP37 Microfluidic synthesis of ω-[18F]fluoro-1-alkynes, Mariarosaria De Simone, Giancarlo Pascali, Ludovica Carzoli, Mauro Quaglierini, Mauro Telleschi, Piero A. Salvadori, PP38 Automated 18F-flumazenil production using chemically resistant disposable cassettes, Phoebe Lam, Martina Aistleitner, Reinhard Eichinger, Christoph Artner, PP39 The effect of the eluent solutions (TBAHCO3, Kryptand K2.2.2) on the radiochemical yields of 18F-Fluoromethylcholine, Surendra Nakka, Hemantha Kumara MC, Al-Qahtani Mohammed, PP40 [68Ga]Radiolabeling of short peptide that has a PET imaging potentials, Al-Qahtani, Mohammed, Al-Malki, Yousif, PP41 Is validation of radiochemical purity analysis in a public hospital in a developing country possible?, N Mambilima, SM Rubow, PP42 Improved automated radiosynthesis of [18F]FEPPA, N. Berroterán-Infante, M. Hacker, M. Mitterhauser, W. Wadsak, PP43 Synthesis and initial evaluation of Al18F-RESCA1-TATE for somatostatin receptor imaging with PET, Uta Funke, Frederik Cleeren, Joan Lecina, Rodrigo Gallardo, Alfons M. Verbruggen, Guy Bormans, PP44 Radiolabeling and SPECT/CT imaging of different polymer-decorated zein nanoparticles for oral administration, Rocío Ramos-Membrive, Ana Brotons, Gemma Quincoces, Laura Inchaurraga, Inés Luis de Redín, Verónica Morán, Berta García-García, Juan Manuel Irache, Iván Peñuelas, PP45 An analysis of the quality of 68Ga-DOTANOC radiolabelling over a 3 year period, Trabelsi, M., Cooper M.S., PP46 In vivo biodistribution of adult human mesenchymal stem cells I (MSCS-ah) labeled with 99MTC-HMPAO administered via intravenous and intra-articular in animal model. Preliminary results, Alejandra Abella, Teodomiro Fuente, Antonio Jesús Montellano, Teresa Martínez, Ruben Rabadan, Luis Meseguer-Olmo, PP47 Synthesis of [18F]F-exendin-4 with high specific activity, Lehtiniemi P, Yim C, Mikkola K, Nuutila P, Solin O, PP48 Experimental radionuclide therapy with 177Lu-labelled cyclic minigastrin and human dosimetry estimations, von Guggenberg E, Rangger C, Mair C, Balogh L, Pöstényi Z, Pawlak D, Mikołajczak R, PP49 Synthesis of radiopharmaceuticals for cell radiolabelling using anion exchange column, Socan A, Kolenc Peitl P, Krošelj M, Rangger C, Decristoforo C, PP50 [68Ga]peptide production on commercial synthesiser mAIO, Collet C., Remy S., Didier R,Vergote T.,Karcher G., Véran N., PP51 Dry kit formulation for efficient radiolabeling of 68Ga-PSMA, D. Pawlak, M. Maurin, P. Garnuszek, U. Karczmarczyk, R. Mikołajczak, PP52 Development of an experimental method using Cs-131 to evaluate radiobiological effects of internalized Auger-electron emitters, Pil Fredericia, Gregory Severin, Torsten Groesser, Ulli Köster, Mikael Jensen, PP53 Preclinical comparative evaluation of NOTA/NODAGA/DOTA CYCLO-RGD peptides labelled with Ga-68, R. Leonte, F. D. Puicea, A. Raicu, E. A. Min, R. Serban, G. Manda, D. Niculae, PP54 Synthesizer- and Kit-based preparation of prostate cancer imaging agent 68Ga-RM2, Marion Zerna, Hanno Schieferstein, Andre Müller, Mathias Berndt, PP55 Synthesis of pancreatic beta cell-specific [18F]fluoro-exendin-4 via strain-promoted aza-dibenzocyclooctyne/azide cycloaddition, Cheng-Bin Yim, Kirsi Mikkola, Pirjo Nuutila, Olof Solin, PP56 Automated systems for radiopharmacy, D. Seifert, J. Ráliš, O. Lebeda, PP57 Simple, suitable for everyday routine use quality control method to assess radionuclidic purity of cyclotron-produced 99mTc, Svetlana V. Selivanova, Helena Senta, Éric Lavallée, Lyne Caouette, Éric Turcotte, Roger Lecomte, PP58 Effective dose estimation using Monte Carlo simulation for patients undergoing radioiodine therapy, Marina Zdraveska Kochovska, Emilija Janjevik Ivanovska, Vesna Spasic Jokic, PP59 Chemical analysis of the rituximab radioimmunoconjugates in lyophilized formulations intended for oncological applications, Darinka Gjorgieva Ackova, Katarina Smilkov, Petre Makreski, Trajče Stafilov, Emilija Janevik-Ivanovska, PP61 The need and benefits of established radiopharmacy in developing African countries, Aschalew Alemu, Joel Munene Muchira, David Mwanza Wanjeh, Emilija Janevik-Ivanovska, PP62 University Master Program of Radiopharmacy – step forward for Good Radiopharmacy Education, Emilija Janevik-Ivanovska, Zoran Zdravev, Uday Bhonsle, Osso Júnior João Alberto, Adriano Duatti, Bistra Angelovska, Zdenka Stojanovska, Zorica Arsova Sarafinovska, Darko Bosnakovski, Darinka Gorgieva-Ackova, Katarina Smilkov, Elena Drakalska, Meera Venkatesh, Rubin Gulaboski, PP63 Synthesis and preclinical validations of a novel 18F-labelled RGD peptide prepared by ligation of a 2-cyanobenzothiazole with 1,2-aminothiol to image angiogenesis., Didier J. Colin, James A. H. Inkster, Stéphane Germain, Yann Seimbille

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There is an increasing need for smart materials capable of removing multivalent ions from aqueous streams without the inconvenience of brine regeneration as in ion-exchange processes. Herein, we present a thermoresponsive micellar system consisting of polystyrene-poly(methoxy diethyleneglycol acrylate) block copolymer surfactants modified with carboxylic acid end groups (PS-PMDEGA-COOH) that can be used to switch between the adsorption and desorption of divalent calcium(II) cations by a mild temperature trigger, thus providing a new type of thermoregenerable ion-adsorbing materials. The switch of calcium(II)-binding capacity is demonstrated to result from a shift in the pKa value of the carboxylic acid groups by the collapse and redissolution of the PMDEGA block and the associated change in local polarity.

Efficient polymer-protein conjugation is a crucial step in the design of many therapeutic protein formulations including nanoscopic vaccine formulations, antibody-drug conjugates and to enhance the in vivo behaviour of proteins. Here we aimed at preparing well-defined polymers for conjugation to proteins by reversible addition-fragmentation chain transfer (RAFT) polymerization of both acrylates and methacrylamides with protein-reactive chain transfer agents (CTAs). These RAFT agents contain either a N-hydroxysuccinimide (NHS) or pentafluorophenyl (PFP) ester moiety that can be conjugated to lysine residues, and alternatively a maleimide (MAL) or pyridyl disulfide (PDS) moiety that can be conjugated to cysteine residues. Efficiency of the bioconjugation of these polymers to bovine and avian serum albumin was investigated as a function of stoichiometry, polymer molecular weight and the presence of reducing agents. A large molar excess of polymer was required to obtain an acceptable degree of protein conjugation. However, protein modification with N-succinimidyl-S-acetylthiopropionate (SATP) to introduce sulfhydryl groups onto primary amines, significantly increased conjugation efficiency with MAL- and PDS-containing polymers.

Contains fulltext : 147203.pdf (Publisher’s version ) (Open Access) One aspect of the invention relates to a biocompatible medical product comprising at least 1% by weight of dry matter of a covalently cross-linked polymer that is obtained by reacting a nucleophilically activated polyoxazoline (NU-POX) with an electrophilic cross-linking agent other than an electrophilically activated polyoxazoline, said NU- POX comprising m nucleophilic groups; and said electrophiliccross-linking agent comprising n electrophilic groups, wherein the m nucleophilic groups are capable of reaction with the n electrophilic groups to form covalent bonds; wherein m>=2, n>=2 and m+n >=5; and wherein the NU-POX comprises at least 30 oxazoline units in case the electrophilic cross-linking agent is an isocyanate. Also provided is a kit for producing the aforementionedbiocompatible cross-linked polymer. The biocompatible cross-linked polymers according to the invention have excellent implant and/or sealing characteristics. 19 september 2013

The homogeneous atom transfer radical polymerization of methyl methacrylate mediated by CuBr/N-(n-hexyl)-2-pyridylmethanimine was successfully carried out using an automated synthesizer. The effects of initiators, solvents and reactant ratios on the polymerization were investigated. Three different kinds of initiators, namely ethyl 2-bromoisobutyrate, (1-bromoethyl)-benzene, and p-toluenesulfonyl chloride, were utilized to initiate the polymerization and ethyl 2-bromoisobutyrate was proven to be the best initiator for the studied system in terms of molecular weight control and narrow polydispersities of the obtained polymers. The solvents used (i.e., toluene, p-xylene, and n-butylbenzene) were found to have strong effects on the polymerization. The reactions in toluene and p-xylene were well-controlled and almost the same polymerization rates were observed. However, the reaction rate dramatically increased in the case of n-butylbenzene, resulting in radical termination during the polymerization. The initiator and Cu(I) concentrations had a positive effect on the polymerization rate. In the meantime, all the reactions were controlled and polymers with predetermined molecular weights and low polydispersity indices (

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Contains fulltext : 147205.pdf (Publisher’s version ) (Open Access) One aspect of the invention relates to a biocompatible, covalently cross-linked, polymer that is obtained by reacting an electrophilically activated polyoxazoline (EL-POX) with a nucleophilic cross-linking agent, said electrophilically activated POX comprising m electrophilic groups; and said nucleophilic cross-linking agent comprising n nucleophilic groups, wherein the m electrophilic groups are capable of reaction with the n nucleophilic groups to form covalent bonds; wherein m=2, n=2 and m+n =5; wherein at least one of the m electrophilic groups is a pendant electrophilic group and/or wherein m=3; and wherein the EL-POX comprises an excess amount of electrophilic groups relative to the amount of nucleophilic groups contained in the nucleophilic cross-linking agent. The invention further relates to biocompatible medical products comprising such a cross-linked POX-polymer. Also provided is a kit for producing a biocompatible, cross-linked POX-polymer. The invention further provides a tissue adhesive medical product comprising at least 1% by weight of dry matter of EL-POX, said EL-POX comprising at least 2 electrophilic groups, including at least one pendant electrophilic group. The polymers according to the invention have excellent implant and/or sealing characteristics. 03 mei 2012

The hydrolysis of PEtOx is studied to evaluate the potential toxicity of partially hydrolyzed polymers that might interfere with its increasing popularity for biomedical applications. The hydrolysis of PEtOx is studied in the presence of digestive enzymes (gastric and intestinal) and at 5.8?M hydrochloric acid as a function of temperature (57, 73, 90, and 100?degrees C). It is found that PEtOx undergoes negligible hydrolysis at 37?degrees C and that thermal and solution properties are not altered when up to 10% of the polymer backbone is hydrolyzed. Mucosal irritation and cytotoxicity is also absent up to 10% hydrolysis levels. In conclusion, PEtOx will not decompose at physiological conditions, and partial hydrolysis will not limit its biomedical applications.

Metallo-supramolecular chemistry offers possibilities for the construction of stimuli-responsive polymeric materials where the environment can have a large impact on the reversibility and strength of interactions between the individual components. The potential of manipulating the strength of the intermolecular non-covalent bonds can result in impressive modifications of the metallo-supramolecular structure and, subsequently, produces changes in the properties of the designed material. The present feature article provides an overview on recent developments in the field of metallo-polymerization of chelating terpyridyl and analogues ligands. Synthetic strategies are described followed by a discussion regarding the characterization and the application of the reviewed metallo-supramolecular structures, mainly based on terpyridines.

Well-defined functional star-shaped polymer structures with up to 29 arms have been successfully synthesized by the combination of atom transfer radical polymerization (ATRP) and click chemistry. First, azide end-functionalized poly(isobornyl acrylate) (PiBA) star-shaped polymers were prepared by successive ATRP and bromine substitution. Subsequently, alkyne end-functionalized molecules and polymers were introduced onto the starshaped PiBA bearing pendant azide moieties by copper-catalyzed azide-alkyne cycloaddition (CuAAC). The possibilities and limits for the CuAAC on such highly branched polyacrylates are described. (Figure Presented). © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

The use of microwave-irradn. instead of conventional heating has been demonstrated to result in faster and cleaner reactions and in some cases to different selectivity. In our previous work, we have demonstrated that the use of pressurized microwave conditions results in a tremendous acceleration for the cationic ring-opening polymn. of 2-oxazolines. However, this obsd. acceleration could be reproduced using conventional heating in an autoclave. Nonetheless, the control over the polymn. was slightly better under microwave irradn. due to the more homogeneous temp. profile. This improved control over the polymn. allowed the synthesis of well-defined triblock and tetrablock copoly(2-oxazoline)s for the first time. In this contribution, the use of ionic liqs., which are well-known as excellent microwave absorbers, as solvent for the microwave-assisted cationic ring-opening polymn. of 2-ethyl-2-oxazoline is discussed. In addn., a continuous flow operating procedure is proposed, in which the poly(2-ethyl-2-oxazoline) is extd. with water and the ionic liq. is reused for the polymn. after removal of the residual water using a microwave-assisted distn. The second part of this contribution deals with the microwave-assisted cationic ring-opening polymn. of fluorinated 2-phenyl-2-oxazolines. These monomers have never been considered for polymn. since the electron withdrawing substituents on the arom. system were thought to result in too slow polymn. Nonetheless, the accelerated microwave-assisted polymn. procedure allowed the polymn. of these monomers, whereby surprisingly fast polymns. were obtained for monomers with ortho-fluoro substituents. [on SciFinder (R)]

Kinetic investigations on the cationic ring opening polymn. (CROP) of 2-ethyl-2-oxazoline (EtOx) were conducted using acetyl chloride, acetyl bromide, and acetyl iodide as initiators. Various polymn. temps. ranging from 80 DegC to 220 DegC were applied under microwave irradn. The resulting polymn. mixts. were characterized with gas chromatog. (GC) and gel permeation chromatog. (GPC) for the detn. of monomer conversion and mol. wt. distribution, resp. [on SciFinder (R)]

The host-guest abilities of core-shell architectures has been successfully applied in various areas such as, drug delivery, stimuli responsive release, catalysis or phase transfer. For all these purposes and esp. for biomedical applications well defined structures are required. Polymeric systems with core-shell architecture can posses well-defined structure, unimol. micellar properties, high loading capacities and do not require a complex multistep synthesis and are therefore accessible in larger scale. Our preliminary results showed that different model guest mols., either hydrophilic or hydrophobic, could be encapsulated and transported by the appropriate star-shaped polymeric host with a hydrophilic or hydrophobic core. The size of the outer shell does not influence the encapsulation abilities, but it is responsible for the soly. of the host-guest systems in the aq./org. phases, preventing the polymer aggregation. [on SciFinder (R)]

The synthesis of 1-butyl-3-methyl-1H-imidazolium chloride in a small-scale microwave reactor was optimized. The optimized conditions were directly transferable to larger batch synthesis. [on SciFinder (R)]

Besides the stimuli responsive release, catalysis or phase transfer, the encapsulation behavior of the star polymers has been also successfully exploited for drug-delivery applications. For all these purposes, esp. for biomedical applications, well defined structures are required. Our group has recently reported the synthesis and the encapsulation properties of well defined 5-arm star-shaped poly(ethylene glycol)-b-poly(a-caprolactone)s that present good encapsulation capabilities and even more they are able to transport guest mols. within biphasic systems. Here we report the encapsulation properties of the reversed systems with a hydrophobic core and a hydrophilic shell using disperse red 1 as model guest mol. The encapsulation abilities of these amphiphilic nancontainers have been evaluated by probing the changes in the microenvironment of the poor water sol. guest mols. using UV/Vis spectroscopy. The bathochromic shift from 420 to 512 nm of the intensity maxima in the absorption spectra of aq. solns. of different nanocontainer/disperse red 1 contents evidences the host-guest interactions. [on SciFinder (R)]

Self-recognition and self-assembly are the two main concepts on which supramol. chem. is based, involving weak and non-covalent interactions such as hydrogen bonding, van der Waals, coordinative and ionic interactions. From all the mentioned weak interactions, metal-ligand coordination gained a particular interest for the synthesis of supramol. structures due to the fact that the coordination bond is highly directional, a wide range of easily functionalized ligands such as terpyridines is available, and the interaction strength can be fine-tuned by choosing appropriate metal ions. Furthermore, the presence of a metal complex in the "supra-structure" introduces addnl. electrochem., photophys., catalytic and magnetic properties. In the present contribution we discuss the synthesizes, characterization and the properties of the amphiphilic ABA block copolymers obtained via Ru(II) terpyridine complexation. [on SciFinder (R)]

In this contribution, a novel on demand drug delivery concept based on polymeric implants is presented. The simple combination of drug substance and polymer matrix was found to result in a robust and reproducible on demand drug delivery device that can be switched by temp. High switching ratios (several hundreds) were found in repetitive (up to 5) on demand drug dosing. In addn., the use of several other noninvasive triggers was explored. Finally, the potential of this novel drug delivery technol. will be demonstrated by in vivo on demand drug delivery.

The ATRP of PEGMAs could be successfully applied to an octafunctional macroinitiator with the formation of the well-defined 8-arm star polymers of narrow polydispersities (PDI = 1.08-1.11). The control over the polymns. could be achieved under surprisingly mild conditions, even at ambient temp. The star coupling reaction could be suppressed by using appropriate reaction conditions. [on SciFinder (R)]

Microwave irradn. is rapidly evolving into a common heat source in different areas of chem. including medicinal and org. chem. as well as polymer chem. The major advantages of the use of microwave irradn. are the often obsd. faster and cleaner reactions and sometimes changes in selectivity. Although the majority of beneficial effects might be explained by the faster heating, higher attainable temps. due to closed reaction vessels and the more homogeneous heat profile, in some cases selective heating results under microwave irradn. results in changes in selectivity or it allows chem. that cannot be performed with conventional heating. Besides these well-documented advantages of the use of microwave irradn., it is often claimed that microwave irradn. is a fast and efficient heat source. To investigate the validity of the claimed efficient heating under microwave irradn., we examd. the efficiency of microwave heating various solvents under microwave irradn. using a monomode microwave reactor. Examples of temp.-time profiles and the corresponding efficiency curves are shown in the Figure. In addn., the effects of adding salt or passive heating elements on the heating efficiency were studied. The heating efficiency for water was further examd. using different reaction vols. as well as monomode and multimode microwave synthesizers. [on SciFinder (R)]

A poly(2-nonyl-2-oxazoline-block-2-ethyl-2-oxazoline-block-2-methyl-2-oxazoline) triblock copolymer was used for the prepn. of self-assembled micelles in the hydrophobic ionic liq. 1-butyl-3-methylimidazolium hexafluorophosphate. It was found that the transfer of the micelles formed by this triblock copolymer from the ionic liq. phase to an aq. phase can be reversibly achieved by heating or cooling the system. The findings reported in this contribution reveal the existence of interesting stimuli-responsive block copolymer micellar structures exhibiting thermo-reversible phase transfer characteristics in a bi-phase system. Stimuli-responsive block copolymer micelles prepd. within this kind of heterogeneous systems may find important applications in the encapsulation, transport, and delivery of guest mols. as well as the development of advanced heterogeneous micellar catalytic and novel sepn. processes.

The development of controlled radical polymn. techniques, namely atom transfer radical polymn. (ATRP), reversible addn. fragmentation transfer (RAFT) and nitroxide mediated radical polymn. (NMP), have opened up unprecedented possibilities for the synthesis of well-defined macromol. architectures with a large no. of different monomers. In addn., well-defined polymers with LCST behavior have wound widespread interest for a use as -smart' responsive materials. Here we report our automated parallel investigations on the NMP of 2 hydroxypropylacrylate (HPA), N,N-dimethylacrylamide (DMA) and N-acryloyl morpholine (Amor) using BlocBuilder- nitroxide and addnl. free SG-1 nitroxide. The high-throughput approach allowed fast optimization of the polymn. procedure for solvent, temp. and concn. of free nitroxide. In addn., the optimal polymn. conditions were applied for the synthesis of systematical libraries of well-defined statistical copolymers based on HPA and DMA or Amor. The effect of monomer compn. on the thermal properties and thermoresponsiveness of the copolymers was studied in detail. [on SciFinder (R)]

Poly(2-oxazoline)s are highly interesting polymers with tunable properties because they can be obtained from a large no. of differently substituted monomers. These 2-oxazoline monomers can undergo living cationic ring-opening polymn. under appropriate conditions resulting in well-defined polymers with narrow mol. wt. distributions. Moreover, the living character allows the synthesis of multiblock copolymers. However, the rather long reaction times (up to several days) for the polymn. of 2-oxazolines has been an important problem, limiting potential applications. Recently, an improved polymn. procedure, which overcomes this drawback, has been reported. This procedure uses closed reaction vials and microwave irradn. yielding an acceleration of the cationic ring-opening polymn. of 2-oxazolines by a factor of 400 when compared to conventional reflux polymns. Block copoly(2-oxazoline)s obtained by this method have been used as starting materials for the formation nanostructured surfaces by evapn.-induced micellization during spin-coating. [on SciFinder (R)]

Ionic liqs. were recently found to dissolve cellulose, the most abundant biorenewable polymer in nature with a broad range of applications. Ionic liqs. are considered to be -green' solvents in comparison to conventional cellulose solvents, like carbon disulfide or N-methylmorpholine-N-oxide, due to their interesting properties like non-volatility, non-flammability and their recycability. In the present work 1 alkyl-3-methyl-imidazolium based ionic liqs. contg. chloride as a counter ion were used to dissolve cellulose. The influence of different alkyl chain lengths on the dissoln. of cellulose was investigated. The alkyl chain length was varied from Et to decyl, including both even and odd numbered chains, to elucidate structure-dissoln. properties revealing a remarkable odd-even effect. The tritylation of cellulose was performed in 1-butyl-3-methyl-imidazolium chloride using pyridine as base (see Figure). The influence of the reaction time and the ratio of trityl chloride per cellulose monomer unit on the degree of substitution were investigated in detail.

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The environmental awareness has triggered research for the development of more efficient and cleaner technologies in chem. industry. Ionic liqs. and microwave irradn. have appeared in recent years as promising approaches for the replacement of org. volatile compds. in different chem. processes and for the utilization of more efficient heating sources, resp. Ionic liqs. are considered to be very effective substances for the absorption of microwave irradn. In this work, a combination of these two technol. approaches is applied to polymn. processes. The efficient use of ionic liqs., avoiding the use of volatile org. compds. in polymer synthesis is demonstrated including ionic liq. selection and recycling. A more efficient heating source for the polymn. reaction mixts. in comparison to conventional heating sources has been detected as direct consequence of the use of the combination of ionic liqs. and microwave irradn. Furthermore, the investigated concept in the reaction process is proposed to be extended to the ionic liq. recycling step by the means of a sort of microwave-assisted distn., which may open possibilities for the development of more efficient sepn. processes.

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The miniaturization of devices and the advances in nanotechnol.-enabled products has led to the requirement of an increased understanding of the various interactions present in nanoscale contacts - including adhesion and surface tension. It is well known that adhesion plays an important role in the tribol. behavior and contact mechanics of many modern nano-devices and will affect future products currently under development. Adhesion of materials is ruled by interactions that extend down to the at. scale of the contributing materials. The forces involved include non-covalent interactions such as Van-der-Waals forces, hydrogen bonds and Coulomb forces as well as covalent chem. bonds. Although Van-der-Waals forces are only short range, they often rule the adhesion between two materials and are therefore responsible for contact interaction between two films. While the adhesion between two materials is one important factor, the elasticity of both is also very important. This elasticity has a major influence on the size of a contact area that is developed underneath a point contact when a certain force is active. Modern instruments for nanoindentation are sensitive enough to detect the small surface forces and to study adhesion effects. [on SciFinder (R)]