Patent classifications
A61K49/18
Chelating amphiphilic polymers
Described are amphiphilic polymers that are provided with chelating moieties. The amphiphilic polymers are block copolymers comprising a hydrophilic block and a hydrophobic block, with the chelating moieties linked to the end-group of the hydrophilic block. The disclosed polymers are capable of self-assembly into structures such as micelles and polymersomes. With suitable metals present in the form of coordination complexes with the chelating moieties, the chelating amphiphilic polymers of the invention are suitable for use in various imaging techniques requiring metal labeling, such as MRI (T.sub.1/T.sub.2 weighted contrast agents or CEST contrast agents) SPECT, PET or Spectral CT.
Chelate nanoemulsion for MRI
The present invention relates to an oil-in-water nanoemulsion composition for MRI, comprising: an aqueous phase, representing 70% to 90% by weight of the composition, advantageously 75% to 85% and more advantageously from 78% to 82% a lipid phase comprising an oil, representing 9.5% to 29.5% by weight of the composition, advantageously 14% to 25% and more advantageously 17% to 21%, a surfactant at the interface between the aqueous and lipid phases, the surfactant comprising at least one amphiphilic paramagnetic metal chelate and optionally an amphiphilic lipid; the total content of surfactant by weight relative to the oil being between 4% and 10% and advantageously between 5% and 8%; the total content of surfactant by weight relative to the composition being between 0.35% and 2.95% and advantageously between 0.5% and 2%; the oil comprising at least 70%, advantageously at least 80%, advantageously at least 95% by weight and especially at least 97% of saturated C6-C18, advantageously C6-C14 and more advantageously C6-C10 fatty acids.
METAL COMPLEX FORMULATIONS
The present invention relates to a method of preparation of formulations of lanthanide metal complexes of macrocyclic chelators which further comprise a small excess of free chelator. The method uses a solid phase-bound scavenger chelator to remove excess lanthanide metal ions, prior to the addition of a defined excess chelator. Also provided is a method of preparation of MRI contrast agents, together with solid-phase bound chelator meglumine salts useful in the methods.
METAL COMPLEX FORMULATIONS
The present invention relates to a method of preparation of formulations of lanthanide metal complexes of macrocyclic chelators which further comprise a small excess of free chelator. The method uses a solid phase-bound scavenger chelator to remove excess lanthanide metal ions, prior to the addition of a defined excess chelator. Also provided is a method of preparation of MRI contrast agents, together with solid-phase bound chelator meglumine salts useful in the methods.
A PROCESS FOR PREPARING WATER-DISPERSIBLE SINGLE-CHAIN POLYMERIC NANOPARTICLES
The present invention comprises a process for preparing water-dispersible single-chain polymeric nanoparticles, which comprises cross-linking a polymer having a solubility equal to or higher than 100 mg per litre of water, and an amount of complementary reactive groups comprised from 5 to 60 molar % of the total amount of monomer units present in the polymer chain; with a crosslinking agent having crosslinkable groups; at a temperature comprised from 20 to 25° C. in the absence of a catalyst; to obtain water-dispersible conjugates and compositions containing the nanoparticle; and the use thereof.
Method for the spatially resolved determination of physcial, chemical and/or biological properties or state variables
Method for the spatially resolved determination of physical, chemical and/or biological properties or state variables and/or the change therein in an examination area of an examination object by determining the change in the spatial distribution and/or the mobility, particularly the mobility in rotation, of magnetic particles in this examination area or in parts thereof as a function of the effect of physical, chemical and/or biological influencing variables on at least a part-area and/or in the physical, chemical and/or biological conditions in at least a part-area of the examination area, by means of the following steps: a) introducing covered and/or coated magnetic particles with at least one solid, viscous and/or liquid shell or coating into at least part of the examination area and/or introducing magnetic particles into at least part of the examination area and/or covering and/or coating at least some of these particles in the examination area, b) generating a magnetic field with a spatial profile of the magnetic field strength such that there is produced in the examination area a first part-area having a low magnetic field strength and a second part-area having a higher magnetic field strength, 15 c) changing the, in particular relative, spatial position of the two part-areas in the examination area or changing the magnetic field strength in the first part-area so that the magnetization of the particles is locally changed, d) detecting signals that depend on the magnetization in the examination area that is influenced by this change, and e) evaluating the signals so as to obtain information about the change in the spatial distribution and/or mobility of the magnetic particles in the examination area. The invention also relates to functionalized magnetic particle compositions and magnetic particle compositions suitable for use in the above method. The invention further also relates to an apparatus for the measurement of state variables in the examination area.
Contrast agent for nuclear magnetic resonance imaging comprising melanin nanoparticles stably dispersed in water
The present invention relates to a contrast agent for nuclear magnetic resonance imaging, and more particularly, to a contrast agent for nuclear magnetic resonance imaging containing melanin nanoparticles having a uniform shape and size, thereby providing good dispersibility in water, no cell toxicity, and a long retention time in vivo.
Hypoosmotic solutions for lymph node detection
Provided are compositions for rapid detection of lymph nodes. The compositions include magnetic particles, such as iron oxide, and a solute present in an amount that results in a hypoosomotic solution. Methods for detecting lymph nodes also are provided.
MRI contrasting agent for contrasting cancer cell
The present invention relates to MRI contrasting agent for contrasting cancer cell which contains ultrafine nanoparticles. More particularly, the present invention is directed to a self-assembled ligand composition comprising a ligand A, which is separated at a specific pH range, and a ligand B of which surface charge changes at a specific pH range, MRI contrast agent for contrasting cancer cell comprising said ligand composition and MRI contrasting nanoparticles, and the methods for preparing them.
COMPOSITIONS FOR DETECTING ANALYTES BY MAGNETIC RESONANCE IMAGING
Injectable compositions for the MRI detection of an analyte selected from the group consisting of reactive oxygen species, proteases and enzymes, comprising a) a matrix material based on a responsive hydrophobic polymer capable of undergoing a chemical reaction with the analyte to be detected, such reaction leading to a disruption of the polymer chain of the responsive polymer, b) a contrast agent suitable for use in magnetic resonance imaging, embedded in or encapsulated in the polymer a), c) optionally, a functionality capable of binding a marker or probe or a probe for creating a second detection signal, and d) optionally, a non-responsive polymer not undergoing a chemical reaction with the analyte under the conditions where polymer a) undergoes a reaction leading to chain breakage