Antiangiogenic folate-targeted nanoparticles for docetaxel delivery in ovarian cancer

A multifunctional nanosystem based on biodegradable poly(ethylene glycol) and poly(?-caprolactone) (PEG-PCL) copolymers for the delivery of docetaxel, targeted to specific cancer cells via folate (FOL) receptor ? ?1? and exposing an anti-FLT1 hexapeptide (aFLT1) with anti-angiogenic properties ?2? has been developed. PEG-PCL were modified at PEG end with FOL or aFLT1 via click chemistry. A combination of unmodified PEG-PCL and the two derivatives (Fol-PEG-PCL, aFLT1-PEG-PCL, respectively) were assembled into core-shell nanoparticles (NPs) through nanoprecipitation (Fig. 1). The efficacy of NPs was tested in in vivo zebrafish embryos xenografted with KB cells. The treatments with DTX-DBLFol/aFLT1 abolished completely the formation of multiple tumor masses. This multifunctional approach, based on the combination of antiangiogenic molecules with conventional anticancer drugs delivered through biodegradable targeted nanoplatforms, is expected to potentiate therapeutic outcome by decreasing in the same time the blood supply to the tumor and cancer progression.