A61K49/1818

Crystalline contrast agent for magnetic resonance imaging, kit and composition comprising it and their use

A method of preparing a crystalline contrast agent for magnetic resonance imaging from a zwitterionic carboxylic pyridyl ligand includes mixing metal ion and the pyridyl ligand and obtaining crystals therefrom. The crystalline contrast agent includes a manganese-organic or gadolinium-organic 3D framework. The crystalline contrast agent is employed in a kit and a pharmaceutically acceptable composition. The method allows for preparing crystalline contrast agents with superior properties with easily available starting materials and with an economic and efficient process. The method allows for preparing crystalline contrast agents with exceptional water-stability and water-solubility, which exhibit high longitudinal relaxivities and with excellent stabilities under physiological conditions and low cytotoxicity. Further provided is a method for in vivo imaging of a subject, in particular a human, comprising administering the crystalline contrast agent to the subject.

COMPOSITE PARTICLES FOR IMAGING, METHOD FOR PRODUCING COMPOSITE PARTICLES, CELLS, CELL STRUCTURE, AND MIXED DISPERSION

The purpose of the present invention is to provide composite particles for imaging that have high biodegradability after imaging. To achieve the above purpose, the composite particles for imaging according to the present invention are configured such that the ratio (long-term residual amount/short-term residual amount) of a long-term residual amount, which is the average value of the contrast rate after six days in a cell and the contrast rate after 11 days in a cell of the same type, and a short-term residual amount, which is the contrast rate after two days in a cell of the same type, is less than 99%.

Targeting corroles for tumor toxicity and MRI
10709801 · 2020-07-14 · ·

Disclosed herein are compositions comprising a targeted corrole nanoparticle; and an acceptable excipient. Also disclosed are compositions comprising a targeted corrole nanoparticle; and an acceptable carrier. Further, disclosed herein are methods of imaging a condition in a subject, comprising providing a composition comprising a targeted corrole nanoparticle; administering an effective amount of the targeted corrole nanoparticle to the subject; and imaging the condition in the subject. In addition, disclosed herein are methods of treating cancer in a subject, comprising providing a composition comprising a targeted corrole nanoparticle; and administering a therapeutically effective dosage of the targeted corrole nanoparticle to the subject.

Targeted Nanoparticles for Glioblastoma Theranostics
20200206144 · 2020-07-02 ·

Targeted nanoparticles are provided which facilitate detection of and therapy for glioblastoma multiforme (GBM). The nanoparticles may be used to target other forms of cancer as well, such as pancreatic, colorectal, and breast. The nanoparticles may provide optical contrast for pre-operative diagnostic imaging and intraoperative navigation using surface-enhanced Raman scattering techniques. Moreover, the nanoparticles may inhibit tumoral growth, block tumoral blood flow, and decrease metastatic spread of GBM. The nanoparticles may further reduce the inflammatory response, which is essential to the growth of the glioma and can be harmful to the patient. The nanoparticle may comprise a biologically inert substance, a biocompatible polymer, an optical-acoustic reporter, and a glioblastoma specific receptor ligand conjugated to the biocompatible polymer. For instance, in some embodiments, the biologically inert substance may be a gold or silica nanoshell, the biocompatible polymer may be polyethylene glycol, the optical-acoustic reporter may be prussian blue, and the glioblastoma specific receptor ligand may be aprepitant.

Heat-induced radiochemical labeling of an iron oxide nanoparticle

A method of synthesizing a radiolabeled nanoparticle. The method includes heating a solution including an iron oxide nanoparticle and at least one radioactive metal ion to bind the iron oxide nanoparticle and the at least one radioactive metal ion, thereby forming the radiolabeled nanoparticle. The method further includes adding a quenching agent to the solution to complex with non-bound radioactive metal ions remaining in the solution. The method further includes separating the complexed quenching agent from the radiolabeled nanoparticle.

COMPOSITE EMBOLIZATION BEADS
20200138988 · 2020-05-07 ·

The present invention relates to compositions and methods for imaging and treating various diseases and disorders, including cancers. The composition of the invention can include a plurality of biodegradable micro-beads, each embedding a plurality of nano-beads, further including a polymer, a radionuclide, a radionuclide chelator, a radioligand, a chemotherapeutic agent, and a cell-penetrating peptide. Upon injection into a blood vessel supplying a cancer tumor, the micro-beads lodge into the tumor and degrade, releasing the nano-beads with a therapeutic or diagnostic agent. The compositions and methods of the invention provide a more homogeneous and deeper distribution of radiation or chemotherapeutic agents throughout the target tumor. The micro-beads provide a local, sustained, and controlled delivery nano-beads including therapeutic or diagnostic agents.

Small Highly Uniform Nanomedicine Compositions for Therapeutic, Imaging and Theranostic Applications
20200101176 · 2020-04-02 ·

A targetable nanoconstruct capable of simultaneously serving as a therapeutic platform for photodynamic therapy as well as an MR molecular imaging agent, free of heavy metal atoms. F3-cys targeting agent nanoconstructs, including 8PEGA-Ce6 NCs. A label-free 8PEGA nanoconstruct that can be directly and selectively imaged by MRI, using standard spin-echo imaging sequences with large diffusion magnetic field gradients to suppress the water signal.

PREPARATION OF A SOLID FORM OF GADOBENATE DIMEGLUMINE

The present invention relates to a process for the preparation of a solid form of the gadobenate dimeglumine compound that comprises obtaining a solution of the said compound in a suitable solvent A wherein the amount by weight of the water optionally present in the solution is at most equal to or lower than the amount by weight of the gadobenate dimeglumine comprised in the solution and adding the obtained solution to an organic solvent B, acting as an appropriate antisolvent and favoring the formation of a solid form of the gadobenate dimeglumine that can be collected by filtration.

Multi-encapsulated formulations made with oxidized cellulose
10561744 · 2020-02-18 · ·

A microsphere and method for forming the same are disclosed. The microsphere includes modified cellulose and at least one of a visualization agent, a magnetic material, or a radioactive material.

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.