The invention belongs to the technical field of medicines, and in particular relates to a nanosuspension of annonaceous
acetogenin drugs prepared from such amphiphilic stabilizers as mPEG PCL, mPEG PLA, mPEG
PLGA, mPEG DSPE, mPEG Chol, SPC, Tween80, BSA, TPGS and the like, as well as a preparation method and an application of the nanosuspension. The annonaceous
acetogenin total
lactone nanosuspension is prepared by virtue of a
solvent precipitation-ultrasonic injection method, and according to a prescription, the proportioning ratio of the annonaceous
acetogenin drugs to the stabilizer is at 1 to (0.02-10) (in percentage by weight). The prepared annonaceous acetogenin nanosuspension can reach a load-loading capacity to 90% to the greatest extent and can reach a minimum grain size to 123.2nm, and the nanosuspension is good in polydispersity. The nanosuspension is stable in both gastrointestinal fluid and
plasma, and the nanosuspension is applicable to
oral administration and injection administration; the nanosuspension has a good in-vitro sustained-release effect and is free from burst release; the
nanoparticle, in comparison with a
crude drug solution, is more obvious in tumor
cell inhibitory rate
in vitro; the nanosuspension, in in-vivo
tissue distribution, shows tumor passive targeting; therefore, the nanosuspension is beneficial for enhancing
efficacy and reducing toxic and side effects. Meanwhile, an in-vivo
efficacy experiment shows that the nanosuspension is outstanding in antineoplastic
efficacy, and the nanosuspension has a broad development prospect.