盐酸表柔比星肽普绅的配制及其体内外抗肿瘤研究  

Preparation and Its in vitro/in vivo Antitumor Activity of Epirubicin Hydrochloride TempSLE

作　　者：王光雪 王敬文 田俞伯 赵恒 郭松麒 李卓越 王景茹 王辉 于锏茗 刘骏炜 韦庆超 张烜[1] WANG Guangxue;WANG Jingwen;TIAN Yubo;ZHAO Heng;GUO Songqi;LI Zhuoyue;WANG Jingru;WANG Hui;YU Jianming;LIU Junwei;WEI Qingchao;ZHANG Xuan(Department of Pharmaceutics,School of Pharmaceutical Sciences,Peking University,Beijing 100191,China)

机构地区：[1]北京大学药学院药剂学系,北京100191

出　　处：《中国药学杂志》2024年第6期522-530,共9页Chinese Pharmaceutical Journal

摘　　要：目的经动脉化疗栓塞(transcatheter arterial chemoembolization,TACE)是Ⅱb期和Ⅲa期肝癌患者的首选治疗方案。肽普绅(TempSLE)是2020年经国家药品监督管理局批准上市的、我国自主研发的一种新型温度敏感液体栓塞剂,可用于动脉栓塞治疗肝脏肿瘤,本实验针对肽普绅载带抗肿瘤药物盐酸表柔比星及其相关抗肿瘤性能开展研究,为临床新型TACE的使用提供实验依据。方法本研究选择肽普绅为栓塞剂,注射用盐酸表柔比星为化疗药物,配制盐酸表柔比星肽普绅,对其理化性质及药物释放行为进行考察,选择人源肝癌HepG2细胞为细胞模型,考察盐酸表柔比星肽普绅的抗肿瘤细胞药效,建立荷瘤裸鼠动物模型,瘤旁注射给予盐酸表柔比星肽普绅,考察其体内抗肿瘤药效。结果盐酸表柔比星肽普绅配制方法简单;盐酸表柔比星不影响肽普绅的温敏性能;释放实验结果表明,24 h时间,药物释放百分率约为80%,随后,药物缓慢释放,216 h时间点,药物释放百分率接近100%;盐酸表柔比星肽普绅与盐酸表柔比星具有相似的抗肿瘤细胞药效;体内抗肿瘤结果表明,瘤旁注射给予盐酸表柔比星肽普绅,可产生明显的体内抗肿瘤药效。结论本实验结果为盐酸表柔比星肽普绅的TACE临床应用提供有益的数据和支持。OBJECTIVE To investigatte antitumor agent epirubicin hydrochloride loaded in TempSLE in vitro/in vivo antitumor activity and provide evidence in clinical use of transcatheter arterial chemoembolization(TACE).METHODS In this study,the TempSLE was selected as the embolic agent,and epirubicin hydrochloride for injection was used as the chemotherapy drug.Epirubicin hydrochloride TempSLE was prepared and its physical and chemical properties and drug release behavior were investigated.Human liver cancer HepG2 cells were selected.The anti-tumor activity of epirubicin hydrochloride TempSLE was evaluated in vitro HepG2 cells.The anti-tumor efficacy of EPI TempSLE in HepG2 tumor-bearing nude mice was evaluated by singly administered EPI TempSLE via peri-tumoral injection.RESULTS The method for preparation of EPI TempSLE was simple;the added EPI did not affect the temperature-sensitive characteristics of TempSLE.The released EPI from EPI TempSLE was about 80%at 24 h time point,after that,EPI was sustained release for 216h and nearly released 100%;the in vitro antitumor activity of EPI TempSLE in HepG2 cells was similar with that of EPI;the in vivo anti-tumor efficacy of EPI TempSLE was observed in HepG2 tumor-bearing nude mice.CONCLUSION The obtained results would help to support the clinical application of epirubicin hydrochloride TempSLE in TACE.

关 键 词：经动脉化疗栓塞 肽普绅 盐酸表柔比星 抗肿瘤活性 

分 类 号：R944[医药卫生—药剂学]