Self assembled spherical microparticles and Temozolomide (TMZ) loaded microcapsules were successfully prepared based on biodegradable dendrimers by dialysis method using Temozolomide saturated solution as selective solvents. The drug loaded microspheres were characterized by dynamic light scattering (DLS), scanning electronic microscope (SEM) and UV spectrophotometer to determine their sizes, morphology, drug loading and in vitro release behavior. The results showed that the mean diameter of the drug loaded microcapsules was under 800 nm, and the drug loading reached 39.9%. Preliminary in vitro release studies revealed a prolonged release, which could last about 900 h. Meanwhile, the release behavior could be better predicted via n level dynamics velocity equation. MTT assay demonstrated that TMZ loaded microcapsules offered a greater tumor inhibitory effect than TMZ to SHG 44 human glioblastoma cells growth.