Cancer remains the second leading cause of death in the United States. In spite of tremendous efforts, there is still no common cure for cancer.<br/>Over the past decades, significant achievements have been made in the development of tumor-targeted drug delivery systems (TTDDS) to distinguish cancer cells from normal cells. Vitamin receptors are overexpressed on the surface of some cancer cell lines to maintain rapid cancer cell growth. Dendrimers are well-defined three-dimensional macromolecules, which can be used to increase the payload of the drugs, targeting efficacy of the conjugate, and other biological and physiological properties. Based on these advantageous features, PAMAM dendrimer-based multifunctional conjugates were designed and synthesized by connecting a biotin-PEGlated G3/G1 PAMAM half-dendron with a new-generation taxoid or a fluorescent probe. Biological evaluations (MTT, CFM and flow-cytometry analyses) of these conjugates against various cancer cell lines, overexpressing biotin receptors (BRs), indicate that these dendrimer-based tumor-targeting drug conjugates exhibited excellent BR-specific cytotoxicity, and substantially enhanced receptor-mediated endocytosis (RME).

Dendrimer-based multifunctional conjugates of new-generation taxoids for tumor-targeted drug delivery

254th National Meeting (2017)

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