Combination lung cancer chemotherapy: Design of a pH-sensitive transferrin-PEG-Hz-lipid conjugate for the co-delivery of docetaxel and baicalin

The aim of the present study is to design a novel dual-ligand lipid based nanoparticle system. It is conducted by a specific ligand and pH sensitive lipid conjugate. Docetaxel (DTX) and baicalein (BA) are co-delivered by this system for combination lung cancer chemotherapy. Firstly, transferrin (Tf)-polyethylene glycol (PEG)-hydrazone (hz)-glyceryl monostearate (GMS), Tf-PEG-hz-GMS, was synthesized. Tf decorated DTX and BA loaded solid lipid nanoparticles (Tf-D/B-SLNs) were prepared by emulsification method. The capability of Tf-D/B-SLNs in suppressing lung cancer cells in vitro and in vivo was investigated. The results revealed the better antitumor efficiency of Tf-D/B-SLNs than the non-decorated SLNs and single drug loaded SLNs. Significant synergistic effects were observed in the dual drugs loaded systems. The best tumor inhibition ability and the lowest systemic toxicity also proved the pH-sensitive co-delivery nano-system could be a promising strategy for treatment of lung cancer.