The invention discloses a
temozolomide spherocrystal based on nano confinement
crystallization regulation and a method and application thereof. The preparation method of the
temozolomide spherocrystal based on nano confinement
crystallization regulation and control comprises the following steps: dissolving glycyrrhizic acid and
temozolomide in pure water under an ultrasonic condition, adjusting the pH value to 3-4, heating until the solution is clear, and cooling to 0-5 DEG C under a stirring condition to obtain the temozolomide spherocrystal based on nano confinement
crystallization regulation and control. Compared with the temozolomide
raw material I
crystal form, the temozolomide spherocrystal disclosed by the invention shows excellent
nasal administration characteristics, including uniform particle size, high
sphericity and excellent fluidity.
Cell experiments show high
cytotoxicity (IC50 = 51.9 [mu] g mL <-1 >) to
glioblastoma, and
in vivo experiments prove efficient
brain targeting ability of the polypeptide. The preparation method has the characteristics of mild preparation conditions, easiness
in process control, good reproducibility, high
brain targeting property and the like, and is suitable for treating cancers delivered into the brain through the
nose.