The invention belongs to the technical field of medical preparations, and discloses nanometer 
chitosan ultrasonic microbubble targeting 
prostate cancer cells and preparation and application thereof. A method comprises the following steps of (1) mixing 
chitosan, methacryloyloxyethyl trimethyl 
ammonium chloride and N-succinimidyl 3-maleimidopropionate, and heating to react, so as to obtain modified 
chitosan; adding a 
prostate antigen, adjusting the pH (potential of 
hydrogen) value of a 
system, and continuing to react, so as to obtain a complex; (2) stirring and mixing an 
inert matter with low 
boiling point, the complex and water, so as to obtain primary 
emulsion; (3) adding a dispersant and an additive into an oil-phase 
solvent, uniformly mixing, adding the primary 
emulsion, stirring at high speed, adding a crosslinking agent to cure, adding a precipitating agent to precipitate, washing, centrifuging at high speed, and 
drying particles, so as to obtain the ultrasonic microbubble. The nanometer chitosan ultrasonic microbubble has the advantages that the targeting property is good, the 
tissue penetration ability is strong, the affinity is high, and the nanometer chitosan ultrasonic microbubble is suitable for the ultrasonic developing of the 
prostate cancer cells.