双重响应二硫化钼纳米载药体系的制备及其性能研究.

Objective: A targeted MoS2 nanodrug loading system that responds to the tumor microenvironment was prepared, and its drug loading and drug release performance were evaluated. Methods: Based on the MoS2 nanosheets synthesized by hydrothermal method, the S vacant sites of the MoS2 nanosheets were used to connect lipoic acid polyethylene glycol carboxylic acid, which was combined to the Arg-Gly-Asp (RGD) targeting molecule by amide coupling reaction. Succinimidyl 3- [2-pyridyldithio] propionate (SPDP), a linker was then chemically binding to the precedingly prepared composite material, forming the nanocarrier, MoS2-PEG-RGD-SPDP (MPRS). Further, thiolated doxorubicin (DOX) was tethered to the as-prepared nanocarrier, ultimately producing the nanodrug, MPRS-DOX. The synthesized materials were characterized by transmission electron microscope (TEM), X-ray Photoelectron Spectrometer (XPS) and nano-particle potentiometer; The drug loading performance of MPRS was tested by ultraviolet visible spectrophotometer, and the drug releasing performance of MPRS-DOX was investigated by fluorescence spectrophotometer. Results: The MPRS-DOX nanodrug-loading system was successfully synthesized. Its particle size was about 200 nm, and its Zeta potential was +28.2 mV; In addition, its drug-loading efficiency was 86.8%, and its drug-loading amount was 53.5%. In vitro drug release experiments showed that DOX release volume was the highest under the conditions of 10 mM Glutathione (GSH) and pH=5.5. Conclusion: With appropriate particle size, MPRS-DOX nanodrug delivery system is successfully prepared. Furthermore, MPRS-DOX has dual responsiveness of GSH and pH, which can realize the expected controlled drug release in simulated tumor microenvironment. This dual-response nanodrug system of GSH and pH provides a new idea for the construction of a new generation of stimuli-responsive nano-carrier system. [ABSTRACT FROM AUTHOR]