The invention provides a nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and belongs to the field of pharmaceutical preparations. The present invention uses poloxamer P188, Poloxamer P407, Poloxamer P124, one or more of poloxamer P237 and poloxamer P338 are adjuvants, By limiting the kinds and dosage of excipients, the problems of insoluble and difficult administration of annonolactone are solved, and more importantly, the anti-tumor effect in vivo is improved, at the same time, it has better safety, breaks through the bottleneck problem of narrow window of treatment of annonolactone, and provides a feasible solution for clinical application.