Here, a novel pH-responsive block copolymer, poly (ethylene glycol)-poly(ε-caprolactone)-poly(L-histidine) (PEG-PCL-PHis), was synthesized and designed for anti-cancer drug delivery with excellent biocompatible, biodegradable, and strong drug loading efficiency. 1H-NMR, IF-IR, and GPC were used to characterize the structure of the PEG-PCL-PHis copolymer. In addition, the morphology, particle size, Zeta potential, and critical micelle concentration (CMC) of different degree of polymerization were determined by transmission electron microscopy (TEM), dynamic light scattering granulometer (DLS), and fluorescence spectrometer, respectively. The strong affinity between the core of micelles and hydrophobic drug was manifested with 15.09% drug loading content and 84.65% entrapment efficiency. In vitro release of DOX from the block copolymer micelle demonstrated, the PEG-PCL-PHis copolymer micelle has stable and durable drug releasing ability accompanied with pH-sensitivity. From the mechanism of cellular uptake the micelles, the pathway of drug release was captured by confocal laser scanning microscope. These experiments demonstrated the safe delivery for anticancer medicine through this novel copolymer. In conclusion, the PEG-PCL-PHis copolymer micelle has great potential to become a safe drug carrier for cancer chemotherapy.
Keywords: Nanomicelles; cancer therapy; pH-responsive; target drug delivery.