Preparation of Temozolomide Nano SustainedRelease Microsphere Material and Its Application in Treatment of Glioma

Abstract

The polylactic acid/glycolic acid (PLGA) sustained-release microspheres are used as the main material for local sustained-release in the study. Ultrasonic emulsification-solvent evaporation method is applied to combine the sustained-release microspheres material with temozolomide to form a composite sustained-release microsphere (TMZ-PLGA-W). The ratio of lactic acid (LA) and glycolic acid (GA) was adjusted so as to test the morphological characteristics of TMZ-PLGA-W at different ratios. The amount of drug released and the encapsulation rate of the material at different time periods were calculated. The C6 glioma system was implanted into the right caudate nucleus of Wistar rats to obtain a rat intracranial glioma model. The models were divided into 5 groups according to different sustained-release materials, and each group had 10 rats. The brain tumor at different times were compared and the survival time of rats was statistically calculated. The TMZ-PLGA-W sustained-release microsphere material with LA/GA ratio of 25%/75% was selected and placed in C6 cells culturing incubator according to different drug loadings. The cell activity according to the culture time was observed. The results showed that the TMZ-PLGA-W sustained-release microspheres prepared in the study were stable in structure, uniform in size, and free of cracks. At the same time, the sustained-release curve showed that the microsphere material conformed to the biodynamic law, which could reduce the burst effect and prolong the sustained release of the drug. The application of TMZ-PLGA-W sustained-release microspheres can effectively inhibit the increase in the area of brain tumors in rats, and at the same time improve the survival rate of rats. The increase in the drug loading of the microspheres can further inhibit the growth of glioma cells.