Two synthetic routes to folic acid (FA)-functionalized diblock copolymers based on 2-(methacryloyloxy)- ethyl phosphorylcholine [MPC] and either 2-(dimethylamino)ethyl methacrylate [DMA] or 2-(diisopropylamino) ethyl methacrylate [DPA] were explored. The most successful route involved atom transfer radical polymerization (ATRP) of MPC followed by the tertiary amine methacrylate using a 9-fluorenylmethyl chloroformate (Fmoc)-protected ATRP initiator. Deprotection of the Fmoc groups produced terminal primary amine groups, which were conjugated with FA to produce two series of novel FA-functionalized biocompatible block copolymers. Nonfunctionalized MPC-DMA diblock copolymers have been previously shown to be effective synthetic vectors for DNA condensation; thus, these FA-functionalized MPC-DMA diblock copolymers appear to be well suited to gene therapy applications based on cell targeting strategies. In contrast, the FA-MPC-DPA copolymers are currently being evaluated as pH-responsive micellar vehicles for the delivery of highly hydrophobic anticancer drugs.
|Data di pubblicazione:||2005|
|Titolo:||Synthesis of novel folic acid-functionalized biocompatible block copolymers by atom transfer radical polymerization for gene delivery and encapsulation of hydrophobic drugs|
|Autori:||LICCIARDI M; TANG Y; BILLINGHAM NC; ARMES SP; LEWIS AL|
|Tipologia:||Articolo su rivista|
|Citazione:||LICCIARDI M, TANG Y, BILLINGHAM NC, ARMES SP, & LEWIS AL (2005). Synthesis of novel folic acid-functionalized biocompatible block copolymers by atom transfer radical polymerization for gene delivery and encapsulation of hydrophobic drugs. BIOMACROMOLECULES, 6, 1085-1096.|
|Digital Object Identifier (DOI):||10.1021/bm049271i|
|Appare nelle tipologie:||01 - Articolo su rivista|