Nippon Kayaku Kabushiki Kaisha

Yuki Kawano

Keiichirou Yamamoto

Tsuyoshi Fukuda

Dai Kurihara

Provided is a polymeric micelle type DDS preparation that may efficiently exhibit pharmacological activity effects by enhancing migration characteristics, penetrability, and retention characteristics toward a diseased target tissue such as a tumor tissue or an inflammation-affected tissue, and thereby enhancing the action of a pharmacologically active substance. Disclosed is a block copolymer (A) having a hydrophilic polymer segment linked to a hydrophobic polymer segment, the hydrophilic polymer segment containing a polyethylene glycol chain, and the hydrophobic polymer segment containing a polyamino acid chain having a hydrophobic substituent in a side chain, wherein the hydrophilic polymer segment has a target binding site bonded thereto, and the main chain polymer combining the polyethylene glycol chain and the polyamino acid chain has a molecular weight of not less than 2 kilodaltons and not more than 10 kilodaltons.

Active-targeting-type polymer derivative, composition containing said polymer derivative, and uses of said polymer derivative and said composition

Provided are a block copolymer having an enhanced effect of imaging the interior of a tumor compared to known block copolymers and imaging probes using the known block copolymers; and an imaging probe using the block copolymer. Specifically, for the purpose of enhancing penetrability into a diseased target tissue and efficiently enhancing an imaging effect compared to known block copolymers and imaging probes using the known block copolymers, disclosed is a block copolymer in which a hydrophilic polymer segment containing a polyethylene glycol chain is linked to a hydrophobic polymer segment containing a polyamino acid chain having a signal group and optionally a hydrophobic substituent in a side chain, wherein the main chain polymer combining the polyethylene glycol chain and the polyamino acid chain has an average molecular weight of not less than 2 kDa and not more than 10 kDa, and the mass content percentage of the signal group and the optional hydrophobic substituent is not less than 5% by mass and not more than 50% by mass; and also disclosed is a composition including the block copolymer.

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Tokyo, Japan

Yuki Kawano