To improve therapeutic effect and reduce severely side effects of carboplatin (CBP), the gas-generating nanocapsules were developed to accelerate CBP lysosome release and nucleus delivery. CBP/SB-NC was prepared by co-loading CBP and NaHCO (SB) in nanocapsules using w/o/w emulsification solvent evaporation. They exhibited vesicle-like spherical morphology, uniform particle size and negative zeta potential. Reaching the tumor site with a relatively high concentration is the first step for CBP delivery and the results showed that CBP/SB-NC could effectively increase drug accumulation at tumor site. After that, the drug delivery carriers need to be internalized into tumor cells and the cellular uptake ability results showed CBP/SB-NC could be internalized into RM-1 cells more efficient than CBP solution. After internalized by RM-1 cells, the gas-blasting release process was tested in acid environment. It was demonstrated that 5 mg/ml NaHCO was optimal to achieve pH-responsive gas-blasting release. release results showed that CBP significantly rapid release in acid environment (pH 5.0) compared to neutral pH (pH 7.4) ( < 0.05). Meanwhile, TEM and the change of the concentration of H results exhibited that the explosion of CBP/SB-NC was more easily happened in lysosome acid environment (pH 5.0). The blasting release can accelerate CBP lysosome release to cytoplasm. Furthermore, the nucleus delivery results showed CBP/SB-NC can promote pH-triggered rapid nucleus delivery. And the results of Pt-DNA adduct assay showed that the binding efficiency between CBP and DNA of CBP/SB-NC was higher than CBP solution. At last, and anti-tumor efficacy proved that CBP/SB-NC could enhance anti-tumor activity for prostate cancer therapy. CBP/SB-NC also showed superior safety and by hemolysis assay and histopathological study. All of the results demonstrate that CBP/SB-NC would be an efficient gas-blasting release formulation to enhance prostate cancer treatment.