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 radicalpolymerization (ATRP) of MPC followed by the tertiary amine methacrylate using a 9-fluorenylmethylchloroformate (Fmoc)-protected ATRP initiator. Deprotection of the Fmoc groups produced terminal primaryamine groups, which were conjugated with FA to produce two series of novel FA-functionalized biocompatibleblock copolymers. Nonfunctionalized MPC-DMA diblock copolymers have been previously shown to beeffective synthetic vectors for DNA condensation; thus, these FA-functionalized MPC-DMA diblockcopolymers 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 thedelivery of highly hydrophobic anticancer drugs.
|Numero di pagine||12|
|Stato di pubblicazione||Published - 2005|
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