Copolymer Including Uncharged Hydrophilic Block and Cationic Polyamino Acid Block Having Hydrophobic Group in Part of Side Chains, and Use Thereof

The present invention relates to a block copolymer containing an uncharged hydrophilic polymer chain block and a cationic polyamino acid chain block, wherein the hydrophilic polymer chain block is covalently bound to one end of the main chain of the polyamino acid chain block, and the hydrophobic group is covalently bound to the side chains of not less than 10% and not greater than 70% of amino acid repeating units in the polyamino acid chain block. This block copolymer forms a stable aggregate with siRNA, a small-molecule nucleic acid, under a physiological condition.

The present invention relates to a block copolymer containing a hydrophilic polymer chain block and a cationic polyamino acid chain block having a hydrophobic group incorporated into part of the side chains, as well as a complex of the copolymer and a nucleic acid molecule, specifically in the form of micellar particles.

Research and development are being carried out on nonviral vectors for nucleic acids from various perspectives. However, there still remains a need for vectors or carriers that can efficiently deliver nucleic acids to the target. For example, although Non-Patent Document 11 discloses that micellar particles prepared from PEGylated poly(N-methyldiethanamine sebacate)-co-((cholesteryloxocarbonylamidoethyl)methylbis(ethylene)amm onium bromide sebacate)) have a certain stability, further improvement is desired from the viewpoint of providing a system capable of easily establishing the homogeneity of a pharmaceutical drug per se.

Patents:
US 20,110,052,917

Inventor(s): KATAOKA KAZUNORI [JP]; NISHIYAMA NOBUHIRO [JP]; ISHII ATSUSHI [JP]; KATO YASUKI [JP]; MIYATA KANJIRO [JP]; KIM HYUNJIN [JP]; TAK

Type of Offer: Sale



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