KMID : 0369820100400060379
|
|
Jorunal of Korean Pharmaceutical Sciences 2010 Volume.40 No. 6 p.379 ~ p.386
|
|
Long-acting Recombinant Human Granulocyte Colony Stimulating Factor (rhG-CSF) with a Trimer-Structured Polyethylene Glycol
|
|
Jo Yeong-Woo
Lee Mee-Yong Choi Yun-Kyu Lee Sung-Hee Kang Soo-Hyoung Na Kun Youn Yu-Seok Choi Eung-Chil
|
|
Abstract
|
|
|
Mono PEGylated rhG-CSF (PEG-G-CSF) prepared by utilizing unique PEG was purified and characterized by cation-exchange chromatography. A unique, trimer-structured PEG was chosen for PEGylation of rhG-CSF among various PEG moieties. The in-vitro bioactivity, stability, and pharmacokinetics of mono-PEG-G-CSF were examined and compared to those of native rhG-CSF. Mono PEG-G-CSF exhibited reduced in-vitro bioactivity to native rhG-CSF but showed an excellent in-vivo bioactivity and stability. Furthermore, it showed markedly reduced clearance in rats, thereby increasing the biological half-life by about 4.5-fold compared to that of native rhG-CSF. The results suggest that this unique, trimer-structured 23 kDa PEG can provide advantages to improve the bioactivity of therapeutic proteins in clinical use.
|
|
KEYWORD
|
|
G-CSF, PEG, Structure, Characteristics
|
|
FullTexts / Linksout information
|
|
|
|
Listed journal information
|
|
|