The development of dual-targeting drug delivery system is helpful to overcome the poor physiochemical properties
of chemotherapeutic agents. The RGD sequence has a potential dual-targeting property, with which the chemotherapeutic
agents can be delivered to bone tissue and tumor. And the Janus dendrimer which consists of two dendrons
with different tasks is useful for improving the effect of polymer on pharmacokinetic properties. In this paper, a Janustype
peptide dendrimer which consisted of RGD dimer and 5-FU dimer was synthesized and well characterized by 1H
NMR and MS techniques, as well as the other three compounds for contrast. The hydroxyapatite binding assay and drug
release study were evaluated. The Janus-type dendrimer with both enhanced targeting property and optimized release property,
may reduce the side effects in normal tissues and have potential sustained-release effect. Thus, it may represent a
novel opportunity to apply the versatile Janus-type dual-targeting delivery system to applications in bone tumor treatment.
Keywords: Bone cancer, dual-targeting, hydroxyapatite, in vitro, Janus dendrimer, peptide, RGD.
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