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7-乙基-10-羟基喜树碱聚合物胶束的肿瘤靶向性研究

Study on tumor targeting of 7-ethyl-10-hydroxycamptothecin polymer micelles
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摘要 目的研究7-乙基-10-羟基喜树碱/聚乙二醇-聚天冬氨酸聚合物胶束(7-ethyl-10-hydroxycamptothecin/polyethylene glycol-polyaspartic acid polymer micelles,SN-38/PEG-pasp)在荷瘤小鼠体内的组织分布特点。方法采用LC-MS法测定荷瘤小鼠血浆和组织中7-乙基-10-羟基喜树碱(7-ethyl-10-hydroxycamptothecin,SN-38)的质量浓度,并用SPSS13.0统计学软件对测定的数据进行分析。结果药物在肿瘤组织中相对摄取率(r_e)达到10,远远高于其他组织,除去肝其余组织作为非靶向组织时,肿瘤的靶向效率(t_e)均大于1,呈现出明显的肿瘤靶向特征,胶束组药物在体内质量浓度排布顺序:肿瘤>肝>肺>脾>肾>心>血。结论 SN-38/PEG-pasp在肿瘤组织中药物浓度明显高于除肝脏外的其他各组织,具有明确的肿瘤靶向性。 Objective To study the tissue characteristics of SN-38/PEG-pasp in tumor-bearing mice. Methods The concentration of SN- 38 in the plasma and tissue of tumor-bearing mice was measured by LC-MS. These measured datas were analyzed by SPSS13.0 statistical software. Results In the tumor tissue,the relative uptake rate( re )of the drug reached 10, much higher than other tissues. When removing the liver tissue and the rest of the organization as targeted tissues, the tumor targeting efficiency ( t, ) was more than 1, showing obvious tumor targeting characteristic. The concentration of micelles in mice was sorted as follows: tumour 〉 liver 〉 lung 〉 spleen 〉 kidney 〉 heart 〉 blood. Conclusions In tumor tissue, the concentration of SN-38/PEG-Pasp was significantly higher than that in other tissues except liver, with definite tumor targeting.
出处 《沈阳药科大学学报》 CAS CSCD 北大核心 2018年第2期83-88,共6页 Journal of Shenyang Pharmaceutical University
基金 内蒙古自治区自然科学基金面上资助项目(2013MS1209) 内蒙古科技创新奖励资金资助项目(1639002)
关键词 7-乙基-10-羟基喜树碱 组织分布 靶向性 7-ethyl- 10- hydroxycamptothecin tissue distribution targeting
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参考文献3

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