The invention relates to a biodegradable amphiphilic
albumin derivative and a pharmaceutical composition thereof. In the biodegradable amphiphilic
albumin derivative, hydrophilic long-chain polyethyleneglycol and
alkyl (acyl) group or (deoxidized)
cholic acid are led to an
albumin skeleton so that the amphiphilic albumin derivative is amphipathic and is self-assembled in water to form nano-
micelle. The biodegradable amphiphilic albumin derivative is characterized in that medicament can be encapsulated through the double actions of a hydrophobic group and an albumin molecule chain with the medicament, and the capacity of the albumin encapsulating the medicament is markedly improved; in addition, a hydrophilic long-chain can reduce the
immunogenicity of the albumin and improve the nano-
micelle surface hydrophilicity so that the stability of the nano-
micelle in
aqueous medium can be improved and the nano-micelle has long-circulation characteristics in a body. The pharmaceutical composition of the biodegradable amphiphilic albumin derivative can be used as the carrier of organic medicament, water-insoluble or insoluble medicament and amphiphilic medicament, can be used for intravascular administration,
intramuscular injection administration,
oral administration, cavitary administration or external administration. The invention can be prepared with simple method and mature process and is suitable of large-scale
continuous production.