Core-shell biodegradable nanoassemblies for the passive targeting of docetaxel: features, antiproliferative activity and in vivo toxicity

Amphiphilic block copolymers of poly(ɛ-caprolactone) and poly(ethylene oxide) were assembled in core-shell nanoparticles (NPs) by a melting-sonication technique (MeSo). The entrapment of the poorly water-soluble anticancer drug docetaxel (DTX), nanocarrier cytotoxicity toward different cells and toxicity in mice were investigated. The encapsulation mechanism was rationalized and related to copolymer properties such as crystallinity and drug solubility in the copolymer phase. DTX release from NPs occurred in 2 drug pulses over 30 days. DTX entrapment in NPs strongly decreased haemolysis of erythrocytes in comparison with a commercial DTX formulation. In comparison with free DTX, NPs were both more efficient in inhibiting cell growth of breast and prostate cancer cells and less toxic in experimental animal models. The results of this study indicate that MeSo is an interesting technique for the achievement of peculiar core-shell nanocarriers for the passive targeting and sustained release of poorly water-soluble anticancer drugs.From the Clinical EditorIn this study, stealth nanoparticles of PEO/PCL block copolymers for passive targeting of docetaxel to solid tumors were developed using a novel technique. The studied properties of NPs suggest strong potential as anticancer drug-delivery system.

Graphical AbstractStealth nanoparticles (NPs) of PEO/PCL block copolymers for the passive targeting of docetaxel (DTX) in solid tumors were developed. NPs were produced by a novel technique developed in our labs from two amphiphilic copolymers with triblock and simple diblock architectures. Relevant properties of NPs were explored and related to in vitro/in vivo biological profile in view of their application as anticancer drug-delivery system.Figure optionsDownload high-quality image (180 K)Download as PowerPoint slide