Small molecular weight PEGylation of diosgenin in an in vivo animal study for diabetic auditory impairment treatment.
Diosgenin was modified to control its in vivo bioavailability by conjugating a hydrophilic unit, tetraethylene glycol. The diosgenin-tetraethylene glycol conjugate (TE) was orally administered in streptozotocin induced diabetic mice for this auditory protection study. The bioactivity improvement of TE for in vivo diabetic auditory impairment treatment was clearly observed in three different auditory tests and compared with that of diosgenin. The improvement in in vivo efficacy suggests that the small molecular weight PEGylation of diosgenin is a synthetically robust and systematically applicable strategy to reform the poor pharmacokinetics of a hydrophobic aglycone.
Graduate School of East-West Medical Science, Kyung Hee University, Gyeonggi-do 449-701, Republic of Korea.
Dong-Hwan
DH
Kim
Bin Na
BN
Hong
Hoa Thi
HT
Le
Ha Na
HN
Hong
Choon Woo
CW
Lim
Keun Ha
KH
Park
Tae Woo
TW
Kim
Tong Ho
TH
Kang
D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004144:Diosgenin / Q000737:chemistry / Q000627:therapeutic use*; D015394:Molecular Structure; D008970:Molecular Weight; D011092:Polyethylene Glycols / Q000737:chemistry
D011092:Polyethylene Glycols; D004144:Diosgenin