Protein charge regulator and protein-encapsulating polymer micelle complex

摘要

The present invention provides a protein delivery means (e.g., a polyion complex) which allows efficient introduction into cells (particularly into the cytoplasm), is highly stable in serum, and is also widely applicable. The polyion complex of the present invention comprises a cationic polymer having a polycation moiety and a charge-conversional protein whose overall charge is converted from basic or neutral to acidic by a specific charge regulator.

主权项

1. A polyion complex comprising a cationic polymer at least partially having a polycation moiety; and a protein whose overall charge is converted by a protein charge regulator;
wherein the protein charge regulator comprises a compound represented by the following formula (I): wherein Ra and Rb each independently represent a hydrogen atom, or an optionally substituted alkyl group, an alkenyl group, a cycloalkyl group, an aryl group, an aralkyl group, an acyl group, a heterocyclic group, a heterocyclic alkyl group, a hydroxy group, an alkoxy group or an aryloxy group; alternatively, Ra and Rb may be linked to each other to form an aromatic ring or a cycloalkyl ring together with their adjacent carbon atoms; and a bond between the carbon atoms adjacent to Ra and Rb, respectively, may be either a single bond or a double bond, and wherein the protein is not associated with an endosome membrane.