Preparation, characterization, and in vivo evaluation of doxorubicin loaded BSA nanoparticles with folic acid modified dextran surface.
Biocompatible and biodegradable doxorubicin loaded nanoparticles with targeting ability were prepared from BSA-dextran-folic acid conjugate via a pH adjustment and heating process. The BSA-dextran-folic acid conjugate was produced by an esterification reaction between folic acid and dextran and then the Maillard reaction between the modified dextran and BSA. The nanoparticles have a size about 90nm and excellent dispersibility at pH 7.4 aqueous solution. The doxorubicin loading efficiency and loading amount of the nanoparticles are larger than 90% and 14%, respectively. The antitumor activity and toxicity of the nanoparticles were evaluated through murine ascites hepatoma H22 tumor-bearing mice. The nanoparticles allow the administration of the doxorubicin with higher dose. At doxorubicin dose of 10mg/kg, the nanoparticles can achieve 88.9% of the tumor inhibition rate that is the same as the free doxorubicin at the dose of 5mg/kg. Importantly, the nanoparticles can decrease the toxicity of doxorubicin that results in a significant increase of the average life time in comparison with the free doxorubicin as well as the nanoparticles without folic acid.
State Key Laboratory of Molecular Engineering of Polymer and Department of Macromolecular Science, Fudan University, Shanghai 200433, China.
Hequn
H
Hao
Qingming
Q
Ma
Chong
C
Huang
Fen
F
He
Ping
P
Yao
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage* / Q000737:chemistry; D045744:Cell Line, Tumor; D003911:Dextrans / Q000737:chemistry; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry; D005492:Folic Acid / Q000737:chemistry; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D053758:Nanoparticles / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D012710:Serum Albumin, Bovine / Q000737:chemistry; D047368:Tumor Burden / Q000187:drug effects
D000903:Antibiotics, Antineoplastic; D003911:Dextrans; D004337:Drug Carriers; D012710:Serum Albumin, Bovine; D004317:Doxorubicin; D005492:Folic Acid