Thermoresponsive, hydrolytically degradable polymer micelles intended for radionuclide delivery. 2009

Martin Hruby, and Cestmir Konak, and Jan Kucka, and Miroslav Vetrik, and Sergey K Filippov, and David Vetvicka, and Hana Mackova, and Goran Karlsson, and Katarina Edwards, and Blanka Rihova, and Karel Ulbrich
Institute of Macromolecular Chemistry, Academy of Sciences of the Czech Republic, 162 06 Prague 6, Czech Republic. mhruby@centrum.cz

Novel polymer micelles, prepared by self-assembling thermoresponsive poly(N-isopropylacrylamide)-graft-poly[N-(2-hydroxypropyl)methacrylamide] copolymers with hydrolytically degradable N-glycosylamine groups between the polymer blocks are proposed for delivery of diagnostic and therapeutic radionuclides into solid tumors. The micelles are formed by fast heating of an aqueous solution of the copolymer to 37 degrees C. They have a hydrodynamic diameter of 128 nm (measured using dynamic light scattering) and slowly degrade during incubation in aqueous buffer at pH = 7.4. Labeling with both (131)I and (90)Y proceeds with high yields (>85%). The unlabeled polymers are not cytotoxic for any of the tested murine and human cell lines.

UI MeSH Term Description Entries
D008422 Materials Testing The testing of materials and devices, especially those used for PROSTHESES AND IMPLANTS; SUTURES; TISSUE ADHESIVES; etc., for hardness, strength, durability, safety, efficacy, and biocompatibility. Biocompatibility Testing,Biocompatible Materials Testing,Hemocompatibility Testing,Testing, Biocompatible Materials,Testing, Hemocompatible Materials,Hemocompatibility Testings,Hemocompatible Materials Testing,Materials Testing, Biocompatible,Materials Testing, Hemocompatible,Testing, Biocompatibility,Testing, Hemocompatibility,Testing, Materials,Testings, Biocompatibility
D008823 Micelles Particles consisting of aggregates of molecules held loosely together by secondary bonds. The surface of micelles are usually comprised of amphiphatic compounds that are oriented in a way that minimizes the energy of interaction between the micelle and its environment. Liquids that contain large numbers of suspended micelles are referred to as EMULSIONS. Micelle
D011108 Polymers Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS). Polymer
D011868 Radioisotopes Isotopes that exhibit radioactivity and undergo radioactive decay. (From Grant & Hackh's Chemical Dictionary, 5th ed & McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Daughter Isotope,Daughter Nuclide,Radioactive Isotope,Radioactive Isotopes,Radiogenic Isotope,Radioisotope,Radionuclide,Radionuclides,Daughter Nuclides,Daugter Isotopes,Radiogenic Isotopes,Isotope, Daughter,Isotope, Radioactive,Isotope, Radiogenic,Isotopes, Daugter,Isotopes, Radioactive,Isotopes, Radiogenic,Nuclide, Daughter,Nuclides, Daughter
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D006868 Hydrolysis The process of cleaving a chemical compound by the addition of a molecule of water.
D000178 Acrylamides Colorless, odorless crystals that are used extensively in research laboratories for the preparation of polyacrylamide gels for electrophoresis and in organic synthesis, and polymerization. Some of its polymers are used in sewage and wastewater treatment, permanent press fabrics, and as soil conditioning agents.
D000180 Acrylic Resins Polymers of high molecular weight which are derived from acrylic acid, methacrylic acid or other related compounds and are capable of being molded and then hardened to form useful components. Acrylic Resin,Resin, Acrylic,Resins, Acrylic
D001672 Biocompatible Materials Synthetic or natural materials, other than DRUGS, that are used to replace or repair any body TISSUES or bodily function. Biomaterials,Bioartificial Materials,Hemocompatible Materials,Bioartificial Material,Biocompatible Material,Biomaterial,Hemocompatible Material,Material, Bioartificial,Material, Biocompatible,Material, Hemocompatible

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