Patent classifications
A61K49/105
Ultrafine nanoparticles as multimodal contrast agent
The invention relates to a novel use of ultrafine nanoparticles, of use as a diagnostic, therapeutic or theranostic agent, characterized by their mode of administration via the airways. The invention is also directed toward the applications which follow from this novel mode of administration, in particular for imaging the lungs, and the diagnosis or prognosis of pathological pulmonary conditions. In the therapeutic field, the applications envisioned are those of radiosensitizing or radioactive agents for radiotherapy (and optionally curietherapy), or for neutron therapy, or of agents for PDT (photodynamic therapy), in particular for the treatment of lung tumors.
CONJUGATED POLYMER-BASED NANOPROBE AND PREPARATION METHOD AND APPLICATION THEREOF
Disclosed is a conjugated polymer-based nanoprobe, including a fluorescent conjugated polymer, a surface ligand, a target molecule, a near-infrared fluorescent dye and optionally a gadolinium-containing magnetic resonance contrast agent. This application also discloses a method for preparing the conjugated polymer-based nanoprobe, including: adding raw materials to an organic solvent followed by ultrasonication to obtain a mixture; and adding the mixture to ultrapure water and continuously ultrasonicating the reaction mixture. The conjugated polymer-based nanoprobe can be applied in a combined molecular imaging technique of near infrared fluorescence imaging, photoacoustic imaging and magnetic resonance imaging to effectively recognize metastatic lymph nodes and normal lymph nodes, and it can be retained in the metastatic lymph nodes for a long time, meeting the requirements for long-term observation. Moreover, the near-infrared fluorescent conjugated polymer-based nanoprobe can generate reactive oxygen under irradiation, which is suitable for the photodynamic treatment of tumors.
SOLVENT-FREE GADOLINIUM CONTRAST AGENTS
Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.
DETECTION OF HIGH-RISK UNSTABLE ATHEROSCLEROTIC PLAQUE
The technology relates to a method for detecting high-risk unstable atherosclerotic plaque in a subject, the method comprising: a) administering to the subject a magnetic resonance imaging (MRI) contrast agent capable of being activated by myeloperoxidase (MPO) in atherosclerotic plaque; b) allowing the contrast agent to be activated by myeloperoxidase in atherosclerotic plaque; c) obtaining an image of the atherosclerotic plaque from the subject using such molecular MRI, wherein enhanced imaging is indicative of unstable plaque. In some embodiments an MPO inhibitor is administered to a subject identified as having a high-risk unstable atherosclerotic plaque.
Imaging Compositions
In one aspect, compositions are described herein. In some embodiments, a composition described herein comprises, consists of, or consists essentially of an MRI-active or MRI-sensitive polymer or oligomer formed from (i) a non-alkoxylated and non-alkenoxylated citric acid, citrate, or ester/amide of citric acid, and optionally an alkoxylated or alkenoxylated citric acid, citrate, or ester/amide of citric acid, (ii) a polyol/polyamine such as a diol/diamine, (iii) a monomer comprising an MRI contrast agent, and (iv) an amino acid monomer. The polymer or oligomer may be photoluminescent and MRI-sensitive. In another aspect, imaging methods utilizing the compositions described herein are described. In another aspect, scaffolds, grafts, and films comprising, consisting of, or consisting essentially of the compositions described herein are described.
METHODS AND KITS FOR DETECTING NON-LUMINESCENT OR WEAKLY LUMINESCENT METALS
The invention provides methods and kits for detecting the presence of, the amount of, or the concentration of a substantially non-emitting metal in a sample by a) providing a sensitizer to a chelator of the substantially non-emitting metal thereby creating a sensitized-metal complex; b) adding an unsensitized chelate, and c) detecting a signal from the unsensitized chelate. The substantially non-emitting metal may be gadoliniumn and may exist in complex with a chelator. The unsensitized chelate may be terbium (Tb) or europium (Eu) and the detecting a signal may be performed by fluorescence.
SOLVENT-FREE GADOLINIUM CONTRAST AGENTS
Disclosed herein are complexes of gadolinium metal, ligand and meglumine that are substantially free of non-aqueous solvents. In particular, solvent-free complexes of 1) gadopentetate dimeglumine and 2) gadoterate meglumine are disclosed and methods of their preparation are disclosed. In addition, methods are disclosed for purifying reactants, monitoring and controlling pH, quantifying the free gadolinium content, quantifying the concentration of gadolinium-ligand complex in aqueous solution, and procedures for producing a drug product in one step. The one step process eliminates the need to dry the gadolinium-ligand complex, which is typically highly hygroscopic. The one step process includes purification steps that do not require the use of non-aqueous solvents.
Imaging compositions
In one aspect, compositions are described herein. In some embodiments, a composition described herein comprises, consists of, or consists essentially of an MRI-active or MRI-sensitive polymer or oligomer formed from (i) a non-alkoxylated and non-alkenoxylated citric acid, citrate, or ester/amide of citric acid, and optionally an alkoxylated or alkenoxylated citric acid, citrate, or ester/amide of citric acid, (ii) a polyol/polyamine such as a diol/diamine, (iii) a monomer comprising an MRI contrast agent, and (iv) an amino acid monomer. The polymer or oligomer may be photoluminescent and MRI-sensitive. In another aspect, imaging methods utilizing the compositions described herein are described. In another aspect, scaffolds, grafts, and films comprising, consisting of, or consisting essentially of the compositions described herein are described.
SYSTEMS AND METHODS OF DETECTING INTERSTITIAL CYSTITIS
The invention provides systems and methods for providing a diagnostic examination to a patient, including, but not limited to a determination of the permeability of a patients' body cavity.
FLUORESCENCE-MAGNETIC RESONANCE DUAL-MODALITY CONTRAST AGENT, PREPARATION METHOD THEREFOR AND USE THEREOF
A fluorescence-magnetic resonance dual-modality contrast agent, a preparation method thereof and the use thereof. The contrast agent has the following structure: X-L-Y, wherein: formula (I); R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, and R.sub.12 are each independently selected from H, halogen, OH, NH.sub.2, COOH, CONH.sub.2, NO.sub.2, CN, and low alkyl groups, the low alkyl groups can be substituted with halogen, OH, NH.sub.2, COOH, CONH.sub.2, SO.sub.3H, NO.sub.2, and CN, wherein R.sub.3 and R.sub.4, taken together with the carbon atoms to which they are attached, may form a phenyl group or a heterocyclic group; R.sub.7 and R.sub.8, taken together with the carbon atoms to which they are attached, may form a phenyl group or heterocyclic group; L is a linking group; and Y is a metal chelate.
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