The University of Tokyo

Nanocarrier Co., Ltd.

Japan Science and Technology Agency

Tokyo Medical and Dental University

Public University Corporation Nagoya City University

Kawasaki Institute of Industrial Promotion

Kanjiro Miyata

Kazunori Kataoka

Nobuhiro Nishiyama

Yasuki Kato

Yasutaka Anraku

Shigeto Fukushima

HyunJin Kim

Takehiko Ishii

Hiroyasu Takemoto

Makoto Oba

Atsushi Ishii

Yu Matsumoto

Hiroyuki Chaya

Sumiyo Watanabe

Tomoya Suma

Takanori Yokota

Masataka Nakanishi

Kazutaka Nishina

Hidehiro Mizusawa

Akihiro Kishimura

Kensuke Osada

Hiroya Kuwahara

Shigehito Osawa

Sayan Chuanoi

Akihiro Mizoguchi

Yu Fukusato

Satoru Matsumoto

Takahiro Nomoto

Keiji Itaka

Hideki Shimizu

Mitsuru Naito

Naoki Kanayama

Kotaro Hayashi

Keisuke Katsushima

Yutaka Kondo

Yan Lee

Tatsuyuki Hayashi

Shourong Wu

Kazuko Toh

Shunsaku Asano

Woo-Dong Jang

Beob Soo Kim

Shinya Kaname

Toshiro Fujita

Yuichi Hori

Ronald James Christie

Mai Sanjo

Shigehiro Hiki

Meng Zheng

Hyun Jin Kim

An amphiphilic poly(amino acid) for nucleic acid delivery, which is represented by the following formula (1):

Amphiphilic poly (amino acid), block copolyer using the amphiphilic poly (amino acid), and complex including the amphiphilic poly (amino acid) or the block copolymer and nucleic acid

A drug-polymer conjugate having thermoresponsiveness includes at least one drug conjugated to at least one end portion of at least one thermoresponsive polymer segment having a lower critical solution temperature. The drug-polymer conjugate is capable of forming a micellular aggregate in an aqueous medium at temperatures equal to or above the lower critical solution temperature. The drug-polymer conjugate or the micellular aggregate thereof may be administered to and absorbed in the lungs.

Temperature-responsive drug/polymer compound and application of compound to drug delivery

A unit-type polyion complex for use in delivering nucleic acid to a target site in a patient includes one or more molecules of a block copolymer having a poly(ethylene glycol) segment and a cationic poly(amino acid) segment and one or more molecules of a nucleic acid. A total quantity of positive charges derived from side chains of the cationic poly(amino acid) segment of the block copolymer in the unit-type polyion complex is not offset by a total quantity of negative charges derived from the nucleic acid. Furthermore, the nucleic acid has a strand length of 10-50 bases, the molecular weight of the poly(ethylene glycol) segment is 40&#xd7;10or more, and the block copolymer has a binding constant (Ka) for the nucleic acid of 3.0&#xd7;10or more.

Nucleic acid-loaded unit polyion complex

This invention provides an antitumor drug delivery formulation for treating a subject having a tumor more highly expressing a TUG1 gene than normal tissues or preventing the subject from tumor metastasis, comprising a polymeric micelle comprising a nucleic acid that suppresses high expression of the TUG1 gene as an active ingredient, wherein the polymeric micelle comprises a block copolymer having a cationic poly(amino acid) segment and a hydrophilic polymer chain segment and the nucleic acid, and wherein the nucleic acid is bound to a cationic group of the cationic poly(amino acid) segment to form a complex and/or the nucleic acid is incorporated in the micelle or attached into the micelle; and the polymeric micelle accumulates in the tumor.

Antitumor drug delivery formulation

A unit structure-type pharmaceutical composition includes a single nucleic acid, such as an antisense nucleic acid, electrostatically bound to a single block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charges of the nucleic acid are counterbalanced, at least substantially, by the positive charges of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment. The block copolymer thereby improves the blood retention capability of the nucleic acids.

Unit structure-type pharmaceutical composition for nucleic acid delivery

The present invention provides a vesicle, a conjugate, a composition comprising the vesicle or the conjugate, for use in delivering a drug to the brain, and a method for administering the same. The composition of the present invention is a composition for administration to a subject according to a dosing regimen, comprising a carrier for drug delivery, wherein the dosing regimen comprises administering the composition to a subject who has been fasted or caused to have hypoglycemia and inducing an increase in blood glucose level in the subject, and the carrier is modified at the outer surface thereof with a GLUT1 ligand.

Carrier for use in delivering drug, conjugate, composition comprising same, and method for administrating same

Provided are a micelle composition for nucleic acid delivery using a temperature-sensitive polymer, and a method for producing the micelle. For example, provided is a polyion complex comprising a temperature-sensitive copolymer and a nucleic acid, wherein the temperature-sensitive copolymer comprises a cationic block and a temperature-sensitive block, the cationic block optionally carrying a hydrophilic block linked thereto, and the polyion complex is obtained by mixing the temperature-sensitive copolymer with the nucleic acid under temperature conditions equal to or lower than the lower critical solution temperature (LCST) of the temperature-sensitive copolymer.

Micelle composition for nucleic acid delivery using temperature-sensitive polymer and method for producing same

Provided is a method for easily and efficiently producing encapsulated substance vesicles wherein a substance is encapsulated in the cavity of vesicles obtained by polymer self-assembly. Empty vesicles that have membranes comprising a first polymer that is a block copolymer with uncharged hydrophilic segments and a first kind of charged segments and a second polymer with a second kind of charged segments that carry a charge that is the opposite of said first kind of charged segments as well as spaces that are enclosed by said membranes are mixed in an aqueous medium with the substance that is to be encapsulated in the spaces.

Substance-encapsulating vesicle and process for producing the same

A unit structure-type pharmaceutical composition includes at least one nucleic acid, such as siRNA, electrostatically bound to at least one block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charge(s) of the nucleic acid are counterbalanced, at least substantially, by the positive charge(s) of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment(s). The at least one block copolymer thereby improves the blood retention capability of the nucleic acid(s).

Disclosed is a polymer composite (polyplex) that contains nucleic acid, a cationic polymer, and an anionic polymer. The anionic polymer covers the surface of the composite comprising the cationic polymer and nucleic acid, has a negative charge at neutral pH, and can change so as to have a positive charge at mildly acidic pH.

Charge conversional ternary polyplex

A composition of matter for use in encapsulating a drug is expressed by formula (1) or formula (2): wherein Rand Rare each independently a hydrogen atom or a substituted or unsubstituted, linear or branched alkyl group having 1 to 12 carbon atoms; A is a hydrophilic polymer chain; Land Lare each a linking group; B is a cation-containing group; Ris a side chain of an amino acid; z is an integer of 5 to 500; x is an integer of 40% or more of z; y is 0 or a positive integer; z-x-y is 0 or a positive integer; p is an integer of 1 to 10; and q is an integer of 1 to 10.

Particle composition and pharmaceutical composition using particle composition

Fine particles of crystalline polyol are provided having a cationic polymer fixed on the crystal surfaces. These fine particles can stably carry an anionically charged compound on their surfaces.

Fine particles of crystalline polyol, and method of preparing same

The present invention provides a cationic polyamino acid suitable for a carrier that can form a stable complex with a nucleic acid under a physiological condition and release the nucleic acid in cells suitably. The cationic polyamino acid can associate with a nucleic acid and includes a cationic amino acid residue having a cationic group in a side chain and a hydrophobic amino acid residue having a hydrophobic group in a side chain. The cationic polyamino acid includes 1 to 20 units of the cationic amino acid residue and is represented by the following formula (1). The meaning of each symbol in the formula is as shown in the description.

Short-chain cationic polyamino acid and use thereof

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Tokyo, Japan

Kanjiro Miyata