Poly-(amido amine) (PAMAM) dendrimers have been studied as macromolecular carriers to deliver drugs, resulting in selective accumulation in tumor tissues due to EPR effect. The use of PAMAM derivatives with a cleavable cystamine core enables the assembly of different generations of half dendrons modified with different functionalities into single molecule. Thus, a novel PAMAM-based asymmetric bow-tie dendrimer platform bearing a PEGylated bis-maleimido spacer was designed. Furthermore, this platform with a triazine module as the branching unit was designed to incorporate an imaging component to the drug delivery system (DDS). This platform has been applied to the construction of several tumor-targeting DDSs bearing a vitamin as the tumor-targeting module and a new-generation taxoid as the warhead, connected by a self-immolative disulfide linker, wherein a fluorescein derivative was incorporated as the imaging module. The synthesis and biological evaluation of novel dendrimer-based drug conjugates will be presented.

Design, synthesis, and development of a novel PAMAM-based bow-tie dendrimer platform for tumor-targeting drug delivery

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.