Abstract: The present invention provides a composition that controls pharmacokinetics. Specifically, the present invention provides: a composition for controlling pharmacokinetics, the composition containing a polyvalent cation as an active ingredient; and a method for controlling pharmacokinetics using the polyvalent cation.

Abstract: A poly-ion complex micelle comprising: a block copolymer having a hydrophilic block portion, a cationic hydrophobic block portion and a crosslinking block portion positioned between the hydrophilic block and the cationic hydrophobic block, and an anionic molecule drug encapsulated by the block copolymer, wherein the crosslinking block has a hydrazone bond, the block copolymer comprises the first block copolymer chain and the second block copolymer chain, the first block copolymer chain and the second block copolymer chain crosslinked to each other in the crosslinking block portion, the hydrophilic block portion comprises the first hydrophilic block of the first block copolymer chain and the second hydrophilic block of the second block copolymer chain, and the cationic hydrophobic block portion comprises the first cationic hydrophobic block of the first block copolymer chain.

Abstract: A method of administering a nanoparticle to a subject including: administering to the subject an effective amount of an antibody that binds to an antigen expressed on a surface of a brain endothelial cell such that a sufficient amount of the antibody can bind to the surface of the brain endothelial cell, where the antibody is conjugated to a 1st molecule. Then administering to the subject a nanoparticle that is coated with a 2nd molecule that binds to the 1st molecule under a physiological condition in a brain blood vessel such that the nanoparticle can bind to the 1st molecule that has attached to the surface of the brain endothelial cell.

Abstract: The present invention provides a functionalized mRNA including mRNA and double-stranded RNA including at least one RNA oligomer hybridized with mRNA. Functionalized mRNA is provided according to this configuration.

Abstract: A complex is provided comprising a conjugate in which a polymer having a boronic acid group and a compound having a diol structure are bonded, and a substance that is complexed with the conjugate.

Abstract: The present invention provides a functionalized mRNA including mRNA and double-stranded RNA including at least one RNA oligomer hybridized with mRNA. Functionalized mRNA is provided according to this configuration.

Abstract: 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 40×103 or more, and the block copolymer has a binding constant (Ka) for the nucleic acid of 3.0×105 or more.

Abstract: The present invention provides a nanoreactor (nano size reaction field) using a polyion complex polymersome and a method for producing the nanoreactor. The present invention provides a polyion complex polymersome encapsulating e.g., an enzyme, in which the enzyme is an enzyme acting on a substance passing through a membrane of the polyion complex polymersome, as a substrate.

Abstract: The present invention provides a polyion complex micelle including an antisense oligonucleotide and a block copolymer of a cationic polymer and a PEG block having a number average molecular weight of 3 kDa to 10 kDa.

Abstract: The present invention provides an amphiphilic poly(amino acid) for nucleic acid delivery, which is represented by the following formula (1): where: R1 represents a hydroxy group, an oxybenzyl group, an —O—R1a group, or an —NH—R1b group, where R1a and R1b each independently represent an unsubstituted or substituted, linear or branched alkyl group having 1 to 12 carbon atoms; R2 represents a hydrogen atom, an unsubstituted or substituted, linear or branched alkyl group having 1 to 12 carbon atoms, or an unsubstituted or substituted, linear or branched alkylcarbonyl group having 1 to 24 carbon atoms; R3a, R3b, R4a, and R4b each independently represent a methylene group or an ethylene group; R5a and R5b each independently represent —O— or —NH—; R6a and R6b each independently represent an unsubstituted or substituted aliphatic hydrocarbon group having 7 to 12 carbon atoms that may contain an alicycle; R7a and R7b are each independently selected from groups identical to or different from each other in the group con

Abstract: The present invention provides a polyion complex which can efficiently deliver mRNA into a living body as well as a therapeutic agent and a therapeutic method of arthropathy in which the polyion complex is used. For example, there is provided a polyion complex comprising a cationic polymer and mRNA, wherein the cationic polymer is a polymer comprising a cationic unnatural amino acid as a monomer unit and the cationic unnatural amino acid is an amino acid having a group represented by —(NH—(CH2)2)p—NH2, wherein p is 2, 3 or 4, as a side chain.

Abstract: The present invention provides a nanoreactor (nano size reaction field) using a polyion complex polymersome and a method for producing the nanoreactor. The present invention provides a polyion complex polymersome encapsulating e.g., an enzyme, in which the enzyme is an enzyme acting on a substance passing through a membrane of the polyion complex polymersome, as a substrate.

Abstract: 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.

Abstract: A pharmaceutical composition includes polymer units ? and ?, each having a hydrophilic polymer chain bound to a cationic polymer chain, and a drug. The polymer units ? and ? are radially arranged such that the cationic polymer chains are directed inward and the hydrophilic polymer chains are directed outward, thereby forming a micelle with the drug encapsulated in the micelle. The cationic polymer chain of the polymer unit ? has a phenylboronic acid group in a side chain, and the cationic polymer chain of the polymer unit ? has a phenylboronic acid binding site in a side chain. The phenylboronic acid group and the phenylboronic acid binding site form a cross-linked structure that can dissociate in an acidic environment and/or in the presence of a substance capable of competitive binding.

Abstract: 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.

Abstract: A pharmaceutical composition includes polymer units ? and ?, each having a hydrophilic polymer chain bound to a cationic polymer chain, and a drug. The polymer units ? and ? are radially arranged such that the cationic polymer chains are directed inward and the hydrophilic polymer chains are directed outward, thereby forming a micelle with the drug encapsulated in the micelle. The cationic polymer chain of the polymer unit ? has a phenylboronic acid group in a side chain, and the cationic polymer chain of the polymer unit ? has a phenylboronic acid binding site in a side chain. The phenylboronic acid group and the phenylboronic acid binding site form a cross-linked structure that can dissociate in an acidic environment and/or in the presence of a substance capable of competitive binding.

Abstract: The present invention provides a composition that controls pharmacokinetics. Specifically, the present invention provides: a composition for controlling pharmacokinetics, the composition containing a polyvalent cation as an active ingredient; and a method for controlling pharmacokinetics using the polyvalent cation.

Abstract: 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.

Abstract: 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 40×103 or more, and the block copolymer has a binding constant (Ka) for the nucleic acid of 3.0×105 or more.

Abstract: 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.