Biodegradable polymeric nanoparticles have received growing interest as one of the most promising agents for drug delivery. In the present work, functional and core-crosslinked poly(ethylene glycol) with poly(ϵ-caprolactone) (PEG -PCL ) block copolymer and lecithin as biodegradable polymer doped with polyaniline was used to assemble nanoparticles which were prepared for targeted delivery and controlled release of cisplatin. The morphology of the polyaniline nanoparticles was determined by dynamic light scattering and the prepared nanoparticles showed a size of 83(±1) nm and a uniform spherical shape. For targeting to HER2 receptors, Herceptin was applied to guide the nanoparticles to breast cancer cells. Studies on cellular uptake and drug release of the nanocarriers showed that the prepared nanoparticles were efficiently taken up by breast cancer cells and the drug was released efficiently under acidic conditions when exposed to a near-infrared laser (808 nm, 1.54 W) for 5 min. Our research highlights the great potential of near-infrared light and pH dual-responsive release by core-crosslinked nanoparticles in nanobiomedicine.

The near-infrared (NIR)-mediated novel strategy to control the drug release from nanocarriers has developed rapidly in recent decades. Polyaniline as a non-cytotoxic and electroactive material for studying cellular proliferation has attracted great attention in recent years. In the present work, polyaniline-mediated polymeric nanoparticles were developed to target the delivery of cisplatin and release it in a controllable way. The prepared polyaniline nanoparticles displayed a size of 90 ± 1.0 nm, a favorable morphology in water, and could be targeted to tumors through the high affinity between trastuzumab and the overexpressed Her2 in tumor cells. In addition, the developed nanoparticles demonstrated exciting photothermal conversion efficiency induced by NIR light and achieved significant cell inhibition efficiency (93.97%) in vitro when exposed to an 808 nm NIR laser with the power of 1.54 W for 5 min. Therefore, the developed external control release delivery system with excellent specificity and high cytotoxicity exhibited great potential in cell research and our research demonstrated that the polyaniline also has potential in the application of photothermal conversion in biomedicine.

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The discovery and development of an efficient synthesis route to axinitib is reported. The first-generation route researched by Pfizer, implemented two Pd-catalyzed coupling reactions as key steps. In this work, the development of Heck-type and C-S coupling reactions catalyzed by CuI is briefly described, using an economic and practical protocol. Aspects of route, such as selecting ligands, solvent and other conditions are discussed in detail to obtain the optimal conditions. The scale up experiment was carried out to provide more than 300 g active pharmaceutical ingredients (API) of axitinib in Form XLI which was produced with 99.9 % purity in 39 % yield. In short, we provide a new choice of axitinib synthesis route, through two copper-catalyzed coupling reactions with good yield.