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

Abstract

Aims: We synthesized a novel system of docetaxel-loaded, trastuzumab-functionalized nanoparticles (NPs) of biodegradable copolymers for targeted and synergistic chemotherapy. Materials & 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 desired hydrophobic–lipophilic balance for cellular adhesion, and another is carboxyl group-terminated TPGS, which facilitates the conjugation of trastuzumab on the NP surface for targeting. Results: In vitro investigation with SK-BR-3 breast cancer cells of HER2 overexpression showed that the trastuzumab-functionalized NPs have great advantages over nude NPs in cellular uptake and cytotoxicity. 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 trastuzumab-functionalized, docetaxel-loaded NPs have great potential for targeted chemotherapy to treat HER2-overexpressing cancer.