Copolymers for hepatocyte-specific targeting carrying galactose and hydrophobic alkyl groups.
Core-forming hydrophobic alkyl groups were incorporated into amphiphilic PVLA to enhance the stability and inclusion ability of the homopolymeric micelles in water. The CAC and hepatocyte targeting in the synthesized P(VLA-co-VBH) were investigated in vitro. The CAC of the copolymers decreased and the stability of the copolymeric micelles increased with the incorporation of hydrophobic groups into the homopolymer. The galactose moieties in the copolymer could be recognized by the ASGP-R of the hepatocytes through a receptor-mediated mechanism. The copolymers efficiently delivered a water-insoluble drug to the hepatocytes. Hence, they be used to deliver hydrophobic drugs to cure various liver diseases.
Hiratsuka
Takahiro
T
Department of Biomolecular Engineering, Tokyo Institute of Technology, Yokohama 226-8501, Japan. takaike@bio.titech.ac.jp
Goto
Mitsuaki
M
Kondo
Yoshiyuki
Y
Cho
Chong-Su
CS
Akaike
Toshihiro
T
D000478:Alkylation; D000818:Animals; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D005434:Flow Cytometry; D005690:Galactose / Q000378:metabolism*; D022781:Hepatocytes / Q000378:metabolism*; D007785:Lactose / Q000031:analogs & derivatives / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008823:Micelles; D015394:Molecular Structure; D011108:Polymers / Q000378:metabolism*; D011137:Polystyrenes / Q000378:metabolism; D013056:Spectrophotometry, Ultraviolet
D008823:Micelles; D011108:Polymers; D011137:Polystyrenes; C074112:poly-N-4-vinylbenzyllactonamide; D007785:Lactose; D005690:Galactose