Shimadzu Corporation

Kyoto University

Shunsaku Kimura

Eiichi Ozeki

Isao Hara

Akira Makino

Hideo Saji

Masahiro Ono

Takashi Temma

Shigenori Nozawa

Masashi Isozaki

Takayuki Sato

Hitoshi Akitsu

Ryoji Fushimi

Ryo Yamahara

Kensuke Kurihara

Eri Takeuchi

Fumihiko Yamamoto

Shinae Kondoh

Provided is a molecular assembly (for example, a polymeric micelle nanoparticle) which is capable of efficiently encapsulating a fat-soluble drug. A molecular assembly comprising: an amphiphilic block polymer A1 comprising a hydrophilic block having a sarcosine unit and a hydrophobic block having a lactic acid unit; a hydrophobic polymer A2 having a lactic acid unit; a fatty acid triglyceride; and a fat-soluble drug. Examples of the fat-soluble drug include miriplatin.

Medicinal agent-containing molecular assembly which uses amphiphilic block polymer

[Problem] To provide a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye in a blood component and emit fluorescence in a tumor or an inflamed site to be imaged). [Solution] A fluorescent nanoparticle probe comprising: a molecular assembly composed of an amphiphilic block polymer having a hydrophilic block chain and a hydrophobic block chain; and a fluorescent dye encapsulated in the assembly, wherein (a) the hydrophilic block chain comprises, as an essential hydrophilic structural unit, a unit selected from a sarcosine unit and an alkylene oxide unit, (b) the hydrophobic block chain comprises, as an essential hydrophobic structural unit, a unit selected from the group consisting of an amino acid unit and a hydroxylic acid unit, and (c) the fluorescent dye is a polylactic acid-bound cyanine compound comprising: a fluorescent group represented by the formula (I): and a polylactic acid group having 5 to 50 lactic acid units, and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.

Switching-type fluorescent nanoparticle probe, and fluorescent molecular imaging method using same

Provided is a polymeric micelle pharmaceutical preparation that can increase the ratio of contrast at tumor site to background contrast in a short period of time after administration of a lactosome and can suppress the ABC phenomenon so that the lactosome can be administered more than once within a short span. A branched-type amphiphilic block polymer comprising: a multi-branched hydrophilic block comprising sarcosine; and a hydrophobic block comprising polylactic acid. The branched-type amphiphilic block polymer, wherein the number of branches of the hydrophilic block is 3. A molecular assembly comprising the branched-type amphiphilic block polymer. The molecular assembly further comprising a linear type amphiphilic block polymer.

Branched amphipathic block polymer and molecular aggregate and drug delivery system using same

The present invention provides a molecular assembly whose retention time in a target site is adjusted depending on the kind or purpose of a labeling agent or drug encapsulated therein, and a molecular assembly that can suppress the ABC phenomenon and that can be administered more than once within a short span. A molecular assembly comprising: a branched-type amphiphilic block polymer A comprising a branched hydrophilic block comprising sarcosine and a hydrophobic block comprising a polylactic acid chain; and a functional substance F comprising a functional site and a polylactic acid chain, wherein the polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises L-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises D-lactic acid units, or the polylactic acid chain constituting the hydrophobic block of the amphiphilic block polymer A comprises D-lactic acid units, and the polylactic acid chain contained in the functional substance F comprises L-lactic acid units.

Molecular assembly using branched amphiphilic block polymer, and drug transportation system

The present invention provides a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye during nanoparticle preparation, and emit fluorescence during imaging). A switching fluorescent nanoparticle probe comprising: a molecular assembly composed of an amphiphilic block polymer having a hydrophilic block chain and a hydrophobic block chain; and a fluorescent dye encapsulated in the molecular assembly, wherein (a) the hydrophilic block chain comprises, as an essential hydrophilic structural unit, a unit selected from a sarcosine unit and an alkylene oxide unit, (b) the hydrophobic block chain comprises, as an essential hydrophobic structural unit, a unit selected from the group consisting of an amino acid unit and a hydroxylic acid unit, and (c) the fluorescent dye is a cyanine compound represented by the formula (I): and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.

Switching fluorescent nanoparticle probe and fluorescent particle imaging method using same

The present invention provides a novel amphiphilic substance, a nanoparticle using the novel amphiphilic substance, which can be used as a nanocarrier having high biocompatibility, a drug delivery system and a probe useful for the system, and, a molecular imaging system and a probe useful for the system. An amphiphilic block polymer comprising a hydrophilic block; and a hydrophobic block, wherein the hydrophilic block is a hydrophilic polypeptide chain having 10 or more sarcosine units, and the hydrophobic block is a hydrophobic molecular chain comprising units selected from the group consisting of amino acid units and hydroxyl acid units as essential structural units, and having 5 or more of the essential structural units.

Amphiphilic substance, and drug delivery system and molecular imaging system using the same

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Kyoto, Japan

Shunsaku Kimura