A61K51/1234

IODINATED PHENOLIC LIPIDS AND METHODS AND COSOLVENT SYSTEMS FOR IODINATION OF PHENOLIC LIPIDS

Compositions that include a phenol group conjugated to a lipid group to form a phenolic lipid. The lipid group may include a fluorophore and at least one lipid anchor. The lipid anchor may have a carbon number that ranges between 7 carbon atoms and 22 carbon atoms. Also, included are methods of making and using such phenolic lipids. Further included are methods of iodinating hydrophobic compounds such as phenolic lipids in aqueous based iodination protocols. Cosolvent formulations for use in such methods are also described.

NOVEL MOLECULAR ASSEMBLY, MOLECULAR PROBE FOR MOLECULAR IMAGING AND MOLECULAR PROBE FOR DRUG DELIVERY SYSTEM USING THE SAME, AND MOLECULAR IMAGING SYSTEM AND DRUG DELIVERY SYSTEM

The present invention provides a molecular assembly which is less likely to accumulate in tissue other than cancer tissue, is highly safe for a living body, and can be prepared by a simple and safe method and whose particle size can be easily controlled. The present invention provides a molecular imaging system and a molecular probe useful for the system, and a drug delivery system and a molecular probe useful for the system. The present invention provides a method for preparing molecular assembly, by which the particle size of molecular assembly having a signal group or a drug can be arbitrarily controlled in order to allow the molecular assembly to effectively accumulate in cancer tissue by utilizing EPR effect. A molecular assembly comprising: an amphiphilic block polymer A comprising a hydrophilic block chain and a hydrophobic block chain having 10 or more lactic acid units; a hydrophobic polymer A2 having at least 10 or more lactic acid units; and/or a labeled polymer B comprising at least 10 or more lactic acid units and a labeling group.

DELIVERABLE EXTRACELLULAR VESICLES INCORPORATING CELL MEMBRANE TRANSPORT PROTEINS

Disclosed are extracellular vesicles (EVs), such as exosomes, comprising a heterologous cell membrane transporter protein, such as the sodium iodide symporter (NIS). Also disclosed are methods of using the disclosed EVs for delivering agents to recipient cells and methods for measuring efficacy of delivery by the EVs to the recipient cells. Also disclosed are method of making the disclosed EVs and cell lines for producing the EVs.

Novel Liposomal Formulation for the Oral Hepatic Delivery of Drugs

The present invention relates to liposomal compositions, comprising liposomes containing tetraether lipids (TELs), and further comprising the lipopeptide Myr-HBVpreS/2-48 (Myrcludex B) as part of said liposomes, as well as uses thereof for the prevention or treatment of hepatic disorders or diseases, and/or for the oral hepatic delivery of therapeutic and/or diagnostic agents.

PORPHYRIN NANOVESICLE WITH FATTY ACID CONJUGATE

There is described herein a bilayer nanovesicle comprising porphyrin-phospholipid conjugate and a chelator-fatty acid conjugate; wherein the chelator-fatty acid conjugate comprises an aminopolycarboxylic acid conjugated to a single chain fatty acid; and the porphyrin-phospholipid conjugate comprises one porphyrin, porphyrin derivative or porphyrin analog covalently attached to a lipid side chain, preferably at the sn-1 or the sn-2 position, of one phospholipid.

NOVEL COMPOUND COMPRISING ESTER GROUP AND USES THEREOF
20240336632 · 2024-10-10 ·

The present invention relates to a novel compound comprising an ester group and uses thereof and, more particularly, to a novel compound that exhibits excellent visualization ability in a tumor by using the difference in activity of esterase for each organ in the body, and to uses therefor for diagnosing or treating cancer. A novel compound of chemical Formulas 1 to 8 according to the present invention exhibits selectivity according to the difference in activity of esterase for each organ due to ester residue in a structure, and thus is extremely effective in visualizing pancreatic cancer, etc.

COMPOSITION FOR PREVENTING OR TREATING ISCHEMIC DISEASES, CONTAINING LIPOSOMES IN WHICH VEGF-DERIVED PEPTIDES ARE SUPPORTED

The present invention relates to: a pharmaceutical composition for preventing or treating ischemic diseases, containing liposomes into which vascular endothelial growth factor (VEGF)-derived peptides are loaded; a method for treating ischemic diseases, comprising the step of administering the pharmaceutical composition to an individual suspected of having an ischemic disease; a use of the liposomes; and a kit for evaluating, using the liposomes, the amount of liposomes, into which VEGF-derived peptides are loaded, delivered to ischemic lesions and of loaded materials released and absorbed. The composition, of the present invention, for preventing or treating ischemic diseases, containing liposomes into which VEGF-derived peptides are loaded, the liposomes having an average particle size of 90 to 110 nm and a particle distribution of 50 to 200 nm and being surface-modified with polyethylene glycol, is capable of significantly increasing the absorption of VEGF compared with treatment using solely VEGF, thereby effectively treating ischemic diseases such as myocardial infarction, middle cerebral artery stenosis, lower limb ischemia, and cerebral infarction. In addition, the kit provided in the present invention can be useful in evaluating the amount of liposomes, into which VEGF-derived peptides are loaded, delivered to ischemic lesions and of loaded materials released and absorbed, in a treatment step for a patient with ischemic diseases.

Microsphere comprising a lanthanide metal complex

The invention is directed to a method for preparing a microsphere comprising a lanthanide metal phosphate complex, a microsphere, a powder comprising a number of the microspheres, a suspension comprising the microsphere or the powder, the use of the microsphere, a method for detecting a tumor, and a therapeutic composition comprising the microsphere, the powder, or the suspension. The invention provides a method for preparing a microsphere that comprises a lanthanide metal phosphate complex, the method comprising: (a) providing an organic lanthanide metal complex microsphere, wherein the lanthanide metal is present in an amount of more than 20 wt. %, based on total weight of the microspheres, and wherein the organic lanthanide metal complex comprises a lanthanide ion and organic ligands with which the lanthanide ion forms the complex; and thereafter (b) replacing at least part of the organic ligands in the organic lanthanide metal complex microsphere with phosphate in a chimie douce reaction,
wherein the lanthanide metal is present in the resulting microsphere in an amount of more than 20 wt. %, based on total weight of the microsphere, and wherein the lanthanide metal complex in the resulting microsphere comprises a lanthanide ion and phosphate.

HYDROPHILIC FLUORINATED MOLECULES FOR LIPOSOMAL 19F MRI PROBES WITH UNIQUE MR SIGNATURES

Readily available hydrophilic and small organofluorine moieties were condensed via click chemistry to generate nonionic hydrophilic fluorinated molecules with unique .sup.19F MR signatures. These were used to fabricate stable liposome formulations for imaging various tissue types. This approach was tailored to exploit the broad spectrum of organic .sup.19F molecular species and to generate probes with distinct .sup.19F MRI signatures for simultaneous assessment of multiple molecular targets within the same target volume.

IMAGING OF TUMOR-ASSOCIATED MACROPHAGES

Presented herein are methods and compositions for non-invasive imaging of TAMs with discoidal high-density lipoproteins to assess prognosis and therapy outcome. TAMs are increasingly investigated in cancer immunology, and are considered a promising target for better and tailored treatment of malignant growths. Although TAMs also have high diagnostic and prognostic value, TAM imaging still remains largely unexplored. Imaging agents/methods provided herein are of value for non-invasive in vivo evaluation of TAM burden, not only in preclinical but also in clinical settings.