TY - JOUR
T1 - Water-soluble gambogic acid PEGylated prodrugs
T2 - Synthesis, characterization, physicochemical properties and in vitro hydrolysis
AU - Tang, Xiaoyan
AU - Zhang, Peng
AU - Ye, Hai
AU - Zhang, Can
AU - Shen, Wenbin
AU - Ping, Qineng
PY - 2008/10
Y1 - 2008/10
N2 - A series of poly(ethylene glycol) (PEG) prodrugs of gambogic acid (GA) with different molecular weight which used L-leucine as spacer were synthesized and characterized by FT-IR, 1H NMR and TOF MS. Drug loading capability, analyzed by UV spectrum, was 17.48, 9.26, 3.99, and 1.79%, aqueous solubility of the prodrugs was determined to be 1750, 1250, 800, and 645 mg/ml, respectively. The drug release from prodrugs was investigated under simulated in vivo conditions whose half-time (t1/2) in plasma ranged from 1.26 to 6.12 h. The effect of temperature on drug release was studied at four different temperatures and activation energy was determined as well. The stability of the prodrugs was improved in parallel with increasing molecular weight of PEG while prodrug yields and drug loading capability were reduced.
AB - A series of poly(ethylene glycol) (PEG) prodrugs of gambogic acid (GA) with different molecular weight which used L-leucine as spacer were synthesized and characterized by FT-IR, 1H NMR and TOF MS. Drug loading capability, analyzed by UV spectrum, was 17.48, 9.26, 3.99, and 1.79%, aqueous solubility of the prodrugs was determined to be 1750, 1250, 800, and 645 mg/ml, respectively. The drug release from prodrugs was investigated under simulated in vivo conditions whose half-time (t1/2) in plasma ranged from 1.26 to 6.12 h. The effect of temperature on drug release was studied at four different temperatures and activation energy was determined as well. The stability of the prodrugs was improved in parallel with increasing molecular weight of PEG while prodrug yields and drug loading capability were reduced.
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U2 - 10.1691/ph.2008.8571
DO - 10.1691/ph.2008.8571
M3 - Article
C2 - 18972831
AN - SCOPUS:54149096519
SN - 0031-7144
VL - 63
SP - 711
EP - 717
JO - Die Pharmazie
JF - Die Pharmazie
IS - 10
ER -