Functionalized amphiphilic hyperbranched polymers for targeted drug delivery.
Amphiphilic hyperbranched core-shell polymers with folate moieties as the targeting groups were synthesized and characterized. The core of the amphiphilic polymers was hyperbranched aliphatic polyester Boltorn H40. The inner part and the outer shell of the amphiphilic polymers were composed of hydrophobic poly(epsilon-caprolactone) segments and hydrophilic poly(ethylene glycol) (PEG) segments, respectively. To achieve tumor cell targeting property, folic acid was further incorporated to the surface of the amphiphilic polymers via a coupling reaction between the hydroxyl group of the PEG segment and the carboxyl group of folic acid. The polymers were characterized by (1)H NMR, (13)C NMR, and combined size-exclusion chromatography and multiangle laser light scattering analysis. The nanoparticles of the amphiphilic polymers prepared by dialysis method were characterized by transmission electron microscopy and particle size analysis. Two antineoplastic drugs, 5-fluorouracil and paclitaxel, were encapsulated into the nanoparticles. The drug release property and the targeting of the drug-loaded nanoparticles to different cells were evaluated in vitro. The results showed the drug-loaded nanoparticles exhibited enhanced cell inhibition because folate targeting increased the cytotoxicity of drug-loaded nanoparticles against folate receptor expressing tumor cells.
Chen
Si
S
Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan 430072, People's Republic of China.
Zhang
Xian-Zheng
XZ
Cheng
Si-Xue
SX
Zhuo
Ren-Xi
RX
Gu
Zhong-Wei
ZW
D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002845:Chromatography / Q000379:methods; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005492:Folic Acid / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D008968:Molecular Conformation; D053758:Nanoparticles / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012542:Scattering, Radiation
D000970:Antineoplastic Agents; D004337:Drug Carriers; D011108:Polymers; D011092:Polyethylene Glycols; D005492:Folic Acid