摘要
目的优化替莫唑胺胶束的制备工艺,并评价其质量。方法采用薄膜水化法,以PAH-AM为载体制备莫唑胺胶束,通过Box-Behnken效应面设计优化制备工艺。观察替莫唑胺胶束的外观,测定粒径、电位,考察稳定性和体外释放,评价替莫唑胺胶束的质量。结果按最佳工艺条件制备的替莫唑胺胶束的粒径为157.70 nm,电位为7.225 mV,多分散指数为0.12,包封率为77.42%,载药量为33.51%,在20日内保存性质稳定。替莫唑胺胶束降解较慢,在PBS缓冲液(pH2.5)中释放较慢,12 h的释放率约60%。结论将替莫唑胺制备成胶束后可有效提高药物的稳定性,为后续药物的靶向修饰提供了参考。
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.
作者
曹俊如
苏峰
张俊丽
张瑶瑶
鲁胜男
何广卫
CAO Juru;SU Feng;ZHANG Junli;ZHANG Yaoyao;LU Shengnan;HE Guangwei(School of Pharmacy,Anhui Medical University,Hefei,Anhui,230032 P.R.China;Anhui Provincial Key Laboratory of Drug Innovation and Advanced Pharmaceuticals,Hefei Industrial Pharmaceutical Institute Co.,Ld.,Hefei,Anhui,230088 P.R.China;School of Pharmacy,China Pharmaceutical University,Nanjing,Jiangsu,210009 P.R.China)
出处
《华西药学杂志》
CAS
CSCD
北大核心
2024年第5期533-538,共6页
West China Journal of Pharmaceutical Sciences
