title: Novel synthesis and in vitro drug release of polymeric prodrug: Chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate.
abstract: 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.
authors.affiliation: State Key Laboratory of Chemical Resource Engineering, Department of Pharmaceutical Engineering, Beijing University of Chemical Technology, Beijing 100029, PR China.
authors.forename: Lin
authors.initials: L
authors.lastname: Yang
authors.forename: Rong
authors.initials: R
authors.lastname: Zeng
authors.forename: Chao
authors.initials: C
authors.lastname: Li
authors.forename: Gang
authors.initials: G
authors.lastname: Li
authors.forename: Renzhong
authors.initials: R
authors.lastname: Qiao
authors.forename: Liming
authors.initials: L
authors.lastname: Hu
authors.forename: Zelin
authors.initials: Z
authors.lastname: Li