To achieve a better release effect of hydrophobic drugs and spontaneous nanocarrier disintegration by dissolution as well as the CO production of NaCO further, improving the therapeutic effect of hydrophobic drugs, and thereby avoiding the accumulation of the nanocarrier to produce organ toxicity, effervescent SiO-drug-NaCO composite nanoparticles (ESNs) were prepared in this study using a tetraethyl orthosilicate hydrolysis method. Sodium carbonate was used as the effervescent disintegrant to respond to the acidic microenvironment of the tumor. The properties of ESNs were assessed and TEM images were taken to verify the self-disintegration characteristics of nanocarrier materials. The anticancer efficacy of ESNs was evaluated in human breast cancer MCF-7 cells. ESNs loaded with hydrophobic drugs were successfully constructed, and showed high entrapment efficiency and drug loading. The nanocarrier successfully achieved self-disintegration in a PBS environment of pH value at 5.0, and showed excellent antitumor effect . ESNs can effectively load hydrophobic drugs and achieve self-disintegration, while avoiding toxicity from the accumulation of the nanocarrier. These results suggest that ESNs are a promising drug delivery system capable of maximizing the anticancer therapeutic efficacy and minimizing the systemic toxicity.