摘要
目的对OALA12/Taxol载药凝胶系统进行抗肿瘤作用的评价。方法采用HPLC法观测OALA12/Taxol载药凝胶材料体外药物的释放情况。建立小鼠肿瘤EAC实体瘤动物模型,分别瘤旁植入空白凝胶OALA12和载药凝胶OALA12/Tax-ol,以肿瘤生长抑制率、动物体重增长率为观察指标,来评价该凝胶系统抗肿瘤作用及毒性反应。结果拟7 d体外药物累积释放情况,绘制曲线,计算线性相关系数为:0.95。似为零级动力学释放,该凝胶系统对自身溶蚀消除具有一定的控制作用。瘤旁植入200,100,50μl后,动物的肿瘤生长抑制率分别为-2.85%,-3.63%,-4.56%;瘤旁植入OALA12/Taxol载药凝胶20 mg/kg,肿瘤生长抑制率为47.4%(P<0.001);而静脉注射同等剂量的taxol抑瘤率为4.8%(P>0.05)。结论 OALA12/Taxol载药凝胶系统具有良好的控释药物作用;其瘤旁植入与静脉注射相比,能够显著提高抗肿瘤的疗效,降低毒副反应。
Objective The aim is to evaluate the anti tumor effect of OALA12/Taxol drug-loaded gel system through the comparison with intravenous injection of Taxol. Methods ①The OALA12/Taxol drug-loaded gel is placed in a test tube at 37℃ to observe drug release through HPLC.②The establishment of tumor in mice EAC solid tumor animal model,was respectively given OALA12 gel and OALA12/Taxol drug-loaded gel to observe therapeutic effect.Animal mortality,tumor growth rate and animal growth rate were recorded to evaluate the antitumor activity of the gel system. Results ①The initial burst releases of drugs from the drug-loaded hydrogels are not observed and the quasi-linear release of drug carries on for 7days.The linear correlation coefficients of the release profiles shown was 9.5 for gel.The gel system has certain control effect on the process of their elimination.②Animal tumor growth inhibition rates after blank gel materials implanted were-2.85%(200μl);-3.63%(100 μl);-4.56%(50?l).Tumor growth inhibition rate which was 20mg/kg OALA12/Taxol gel group was 47.4%(P<0.001);the same dose intravenous injection group's tumor growth inhibition rate was 4.8%(P>0.05). Conclusion OALA12/Taxol in situ gel has been good release of drugs and controlled of gel material removing.By the comparison,OALA12/Taxol in situ gel can improve anti tumor effects,and reduce the toxic reaction.
出处
《时珍国医国药》
CAS
CSCD
北大核心
2013年第4期989-991,共3页
Lishizhen Medicine and Materia Medica Research
基金
国家高技术研究发展"863"计划(No.2009AA03Z313)