This study aims to determine the specificity of anti-human epidermal growth factor receptor antibody (anti-HER2) modified monomethoxy polyethylene glycol-chitosan (mPEG-CS) nanoparticles (anti-HER2/mPEG-CS NPs) in delivering small interfering RNA (siRNA) to the human epidermal growth factor receptor 2 (HER2) positive cancer cells. Physicochemical properties of the siRNA-loaded anti-HER2/mPEG-CS NPs (anti-HER2/mPEG-CS-siRNA NPs), including size, surface charge, siRNA encapsulation efficiency, and in vitro release profile of siRNA from NPs, were characterized by particle size and zeta potential analyzer, and ultraviolet–visible spectrophotometer. MTT assay was used to study the in vitro cytotoxicity of the NPs. Fluorescent microscope and flow cytometer analysis results showed that anti-HER2/mPEG-CS-siRNA NPs had much efficient delivery of siRNA than the siRNA alone, Lipofectamine-siRNA complexes and mPEG-CS-siRNA NPs. These results demonstrated that anti-HER2/mPEG-CS-siRNA NPs had great potential applications as a targeted strategy for siRNA delivery.
This study explored the feasibility of using smart nanocaged carrier technology for the delivering of multifunctional mPEG-chitosan stabilized silybin nanocrystals and to enhancing the long-term stability, dissolution velocity and bioavailability of the water insoluble drugs. The methoxypoly(ethylene glycol)- b -poly(ε-caprolactone) (mPEG- b -PCL), as nanocaged carrier, was modified with propargyl and azide group and confirmed by FTIR . The methoxypolythylene glycol-grafted chitosan (PEG-CS), as multifunctional stabilizer, were applied for the silybin nanocrystals formulation. Two silybin nanocrystals formulations (PEG-CS nanocrystals and nanocaged nanocrystals) were prepared using anti-solvent precipitation method and optimized by central composite design-response surface model. The transmission electron microscopy , scanning electron microscopy and atomic force microscope revealed small and uniformed morphology. The crystalline state of the nanocrystals was confirmed by X-ray powder diffraction and differential scanning calorimetry . The drug structure was confirmed by Fourier transform infrared spectroscopy. During the long term stability study, the nanocaged nanocrystals were presented remarkable stability. Compared with the silybin solution, the nanocaged nanocrystals and the PEG-CS nanocrystals drug delivery system also exhibited 5.54 and 2.58 fold increasing in the AUC, respectively. Thus, the nanocaged nanocrystals technology with excellent stability, improved dissolution velocity and relative bioavailability was recommended as an efficient and feasible approach for water insoluble drugs delivery.
危险品化学品经营许可证（带存储）