Novel synthesis and in vitro drug release of polymeric prodrug: Chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate.
A novel approach to synthesize chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate was developed. Chitosan-d4T monophosphate prodrug with a phosphoramidate linkage was efficiently synthesized through Atherton-Todd reaction. In vitro drug release studies in pH 1.1 and 7.4 indicated that chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate prefers to release the d4T 5'-(O-isopropyl)monophosphate than free d4T for a prolonged period. The results suggested that chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate may be used as a sustained polymeric prodrug for improving therapy efficacy and reducing side effects in antiretroviral treatment.
Yang
Lin
L
State Key Laboratory of Chemical Resource Engineering, Department of Pharmaceutical Engineering, Beijing University of Chemical Technology, Beijing 100029, PR China.
Zeng
Rong
R
Li
Chao
C
Li
Gang
G
Qiao
Renzhong
R
Hu
Liming
L
Li
Zelin
Z