聚酸酐-吡柔比星长效植入剂在动物模型体内的抑瘤活性

背景:实验证明聚酸酐-吡柔比星植入剂可长时间保持体内血药浓度相对恒定。目的:观察聚酸酐-吡柔比星植入剂在膀胱肿瘤大鼠体内的抑瘤作用。方法:通过N-正丁基-N-(4-羟基-丁基)亚硝胺喂饲构建SD大鼠膀胱癌模型,随机分为实验组与对照组,分别将聚酸酐-吡柔比星植入剂和相同剂量吡柔比星植入模型动物体内膀胱黏膜下,用高效液相色谱仪检测动物体内吡柔比星血药浓度及肿瘤大小变化。结果与结论:实验组吡柔比星在释放过程中无突释效应,基本满足长效局部植入剂应用于膀胱癌治疗的基本要求,可持续释放80d以上;对照组吡柔比星浓度开始明显升高,5d后迅速降低,不能维持有效治疗浓度1.0-3.0mg/L。植入后30d,实验组肿瘤体积较植入前明显缩小,抑瘤率高于对照组(P<0.05),且实验组动物平均存活期长于对照组(P<0.05)。

In vivo antitumor activity of the polyanhydride-pirarubicin long-term implant in animal models

BACKGROUND：Experimental studies have shown that polyanhydride-pirarubicin implants can maintain relatively constant blood concentration for a long term. OBJECTIVE：To observe the in vivo antitumor effect of polyanhydride-pirarubicin implants in the bladder tumors in rats. METHODS：Sprague-Dawley rat bladder cancer models were built by the N-butyl-N-（4-hydroxy-butyl） nitrosamine feeding, and then were randomly divided into experimental and control groups. Polyanhydride-pirarubicin implants and the same dose of pirarubicin implants were implanted into the bladder submucosathe of rat models. High performance liquid chromatography detection was done for monitoring plasma concentration and changes in tumor size. RESULTS AND CONCLUSION：In the experimental group, there was no burst effect during the release of pirarubicin, basically meeting the requirements of long-acting local implants used in the treatment of bladder cancer （sustained release of over 80 days）. In the control group, pirarubicin concentration significantly increased firstly, then decreased rapidly after 5 days and it was unable to maintain the effective therapeutic concentrations （1.0-3.0 mg/L）. Thirty days after implantation, the tumor size in the experimental group was significantly reduced, and the inhibition rate in the experimental group was higher than that in the control group （P 0.05）. Rats in the experimental group had a longer average survival period than those in the control group （P 0.05）.