OBJECTIVE To optimize the preparation process of Temozolomide(TMZ)micelle,and to evaluate its quality.METHODS TMZ micelles were prepared with PAH-AM using the thin film hydration method,and the preparation process was optimized through Box-Behnken design.The appearance of TMZ micelle was observed,the particle size and potential were measured.The stability and release in vitro were investigated,and the quality of TMZ micelle was evaluated.RESULTS The size of TMZ micelle prepared under optimized conditions was 157.70 nm,with the PDI of 0.12 and the potential of 7.225 mV.The encapsulation rate was 77.42％,the drug load efficiency was 33.51％,and the storage property was stable within 20 days.The degradation of TMZ micelle was slow.Release rate was slow in PBS buffers(pH2.5),with a cumulative release of about 60％at 12 h.CONCLUSION TMZ micelles can effectively improve the stability of TMZ.After improving its stability,it can provide a reference for subsequent targeted modification.
关键词
替莫唑胺/胶束/PAH-AM/Box-Behnken效应面/薄膜水化法/处方/稳定性/体外释放
Key words
Temozolomide/Micelle/PAH-AM/Box-Behnken/Film hydration method/Prescription/Stability/Release in vitro
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万方数据