title: PEGylation of bovine serum albumin using click chemistry for the application as drug carriers.
abstract: Monomethyl poly(ethylene glycol) (mPEG)-modified bovine serum albumin (BSA) conjugates (BSA-mPEG) were obtained by the mild Cu(I)-mediated cycloaddition reaction of azided BSA (BSA-N(3) ) and alkyne-terminated mPEG. The structure and characteristics of BSA-mPEG conjugates were thoroughly investigated. There were about two PEG chains conjugated onto each BSA molecule as determined by matrix-assisted laser desorption/ionization time of flight (MALDI-TOF) analysis. The intrinsic nonspecific binding ability of BSA was used for adsorption and sustained release of both rifampicn and 5-fluorouracil (5-FU). The helical structures of BSA were preserved to a large extent after modification and drug adsorption on BSA was confirmed via circular dichroism spectroscopy. Drugs adsorbed onto the conjugated formulation to a lesser extent than on BSA due to mPEG modification. The in vitro release of both rifampicin and 5-FU, however, indicated that BSA-mPEG can function as a drug carrier. Overall, the click reaction provided a convenient tool for the pegylation of BSA. The biological activity of the BSA-mPEG conjugates, including the drug transportation capacity and biocompatibility, were largely retained.
authors.affiliation: State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, PR China.
authors.forename: Xiao-Yuan
authors.initials: XY
authors.lastname: Li
authors.forename: Tai-Hang
authors.initials: TH
authors.lastname: Li
authors.forename: Jin-Shan
authors.initials: JS
authors.lastname: Guo
authors.forename: Ying
authors.initials: Y
authors.lastname: Wei
authors.forename: Xia-Bin
authors.initials: XB
authors.lastname: Jing
authors.forename: Xue-Si
authors.initials: XS
authors.lastname: Chen
authors.forename: Yu-Bin
authors.initials: YB
authors.lastname: Huang
mesh_terms: D002942:Circular Dichroism; D004337:Drug Carriers; D004591:Electrophoresis, Polyacrylamide Gel; D005472:Fluorouracil / Q000008:administration & dosage; D009682:Magnetic Resonance Spectroscopy; D011092:Polyethylene Glycols / Q000737:chemistry*; D012293:Rifampin / Q000008:administration & dosage; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
chemical_list: D004337:Drug Carriers; D012710:Serum Albumin, Bovine; D011092:Polyethylene Glycols; D005472:Fluorouracil; D012293:Rifampin