Novel synthesis and in vitro drug release of polymeric prodrug: Chitosan-O-isopropyl-5 '-O-d4T monophosphate conjugate - Details

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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.　(C)　2009　Elsevier　Ltd.　All　rights　reserved.

Keyword：

Phosphoramidate linkage Drug delivery Chitosan-nucleoside monophosphate conjugate Polymeric prodrugs

Author Community：

[ 1 ] [Zeng, Rong]Jinan Univ, Coll Sci & Engn, Dept Mat Sci & Engn, Guangzhou 510632, Guangdong, Peoples R China
[ 2 ] [Yang, Lin]Beijing Univ Chem Technol, State Key Lab Chem Resource Engn, Dept Pharmaceut Engn, Beijing 100029, Peoples R China
[ 3 ] [Li, Chao]Beijing Univ Chem Technol, State Key Lab Chem Resource Engn, Dept Pharmaceut Engn, Beijing 100029, Peoples R China
[ 4 ] [Li, Gang]Beijing Univ Chem Technol, State Key Lab Chem Resource Engn, Dept Pharmaceut Engn, Beijing 100029, Peoples R China
[ 5 ] [Qiao, Renzhong]Beijing Univ Chem Technol, State Key Lab Chem Resource Engn, Dept Pharmaceut Engn, Beijing 100029, Peoples R China
[ 6 ] [Hu, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
[ 7 ] [Li, Zelin]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China