Trastuzumab-functionalized nanoparticles of biodegradable copolymers for targeted delivery of docetaxel

Abstract

Aims: We synthesized a novel system of docetaxel-loaded, tratuzumab-functionalized nanoparticles (NPs) of biodegradable copolymers for targeted and synergistic chemotheraphy. Material & Methods: NPs of two component biodegradable copolymers were prepared by a modified solvent extraction/evaporation method with D-α-tocopheryl polyethylene glycol succinate (TPGS) as emulsifier. One component copolymer is poly(lactide)-TPGS, which is of desire hydrophobic-lipophilic balance for cellular adhesion, and another is carboxyl group-terminated TPGS, which facities the conjugation of trastuzumab on the NP surface for targeting. Results: In vitro investigation with SK-BR-3 breast cancer cell of HER2 overexpression showed that the tratuzumab-functionalized NPs have great advantages over nude NPs in cellular uptake and cytotocity. Conclusion: Trastuzumab conjugated onto the NP surface has two functions: one is to target HER2-overexpressing cancer cells and the other is to enhance the cytotoxicity of docetaxel through synergistic effects. The trastusumab-functionalized, docetaxel-loaded NPs have great potential for targeted chemotheraphy to treat HER2-overexpressing cancer. © 2009 Future Medicine Ltd.