<p>One of the limitations of current anticancer nanomedicines in clinical applications is the efficiency of drug delivery in their nanocarrier systems. Therefore, we aimed to develop a nano-delivery system loaded with a hydrophobic drug for lung cancer treatment. Nanoparticles (FA-CMC-GNA NPs) were prepared using an emulsion solvent evaporation method, with a disulfide bond-crosslinked thiolated carboxymethyl cellulose as the backbone, encapsulating the hydrophobic drug gambogenic acid. The preparation process was optimized through single-factor experiments and response surface methodology to determine the optimal preparation conditions. The characterization of the physicochemical properties of FA-CMC-GNA NPs was conducted using various techniques, including scanning electron microscopy, dynamic light scattering, X-ray spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. The results showed that the nanoparticles exhibited uniform dispersion and spherical morphology with a particle size of approximately 193.3&#xa0;nm. Additionally, FA-CMC-GNA NPs demonstrated significant glutathione (GSH)-responsive release behavior <i>in vitro</i>. The prepared FA-CMC-GNA NPs were internalized into A549 cells via folate receptor-mediated endocytosis and released gambogenic acid in response to GSH, resulting in a significant inhibitory effect on A549 cells. In conclusion, these findings suggest that FA-CMC-GNA NPs hold the potential to enhance the clinical application value of the hydrophobic drug gambogenic acid for lung cancer therapy.</p>

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Glutathione-responsive FA-CMC-GNA nanoparticles: a novel approach for enhanced delivery of gambogenic acid in lung cancer treatment

  • Xiaoling Xu,
  • Lisha Ye,
  • Chaohui Bao,
  • Wen Hong,
  • Kaiding Wang,
  • Shicheng Qiu,
  • Yaping Xu,
  • Jigang Piao,
  • Qinghua Yao

摘要

One of the limitations of current anticancer nanomedicines in clinical applications is the efficiency of drug delivery in their nanocarrier systems. Therefore, we aimed to develop a nano-delivery system loaded with a hydrophobic drug for lung cancer treatment. Nanoparticles (FA-CMC-GNA NPs) were prepared using an emulsion solvent evaporation method, with a disulfide bond-crosslinked thiolated carboxymethyl cellulose as the backbone, encapsulating the hydrophobic drug gambogenic acid. The preparation process was optimized through single-factor experiments and response surface methodology to determine the optimal preparation conditions. The characterization of the physicochemical properties of FA-CMC-GNA NPs was conducted using various techniques, including scanning electron microscopy, dynamic light scattering, X-ray spectroscopy, thermogravimetric analysis, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. The results showed that the nanoparticles exhibited uniform dispersion and spherical morphology with a particle size of approximately 193.3 nm. Additionally, FA-CMC-GNA NPs demonstrated significant glutathione (GSH)-responsive release behavior in vitro. The prepared FA-CMC-GNA NPs were internalized into A549 cells via folate receptor-mediated endocytosis and released gambogenic acid in response to GSH, resulting in a significant inhibitory effect on A549 cells. In conclusion, these findings suggest that FA-CMC-GNA NPs hold the potential to enhance the clinical application value of the hydrophobic drug gambogenic acid for lung cancer therapy.