| 贝伐单抗介导的阿霉素白蛋白纳米粒的制备与优化 |
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| 引用本文： | 李磊,赵秀丽,乔明曦,胡海洋,陈大为,杨春荣.贝伐单抗介导的阿霉素白蛋白纳米粒的制备与优化[J].中南药学,2011,9(9):641-644. |
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| 作者姓名： | 李磊 赵秀丽 乔明曦 胡海洋 陈大为 杨春荣 |
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| 作者单位： | 1. 沈阳药科大学药学院,沈阳,110016
2. 佳木斯大学药学院,黑龙江,佳木斯,154001 |
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| 摘 要： | 目的采用Box-Behnken效应面法优化贝伐单抗介导的阿霉素白蛋白纳米粒制备工艺。方法在采用去溶剂化-固化交联法制备出的阿霉素白蛋白纳米粒的基础上,用异型双功能交联剂NHS-PEG3500-MAL作为偶联剂,将贝伐单抗偶联到载药白蛋白纳米粒表面。以2-亚氨基硫烷盐酸盐用量、载药白蛋白纳米粒与贝伐单抗质量比、NHS-PEG3500-MAL用量为影响因素,以纳米粒粒径、载药量和包封率作为评价指标,用三因素三水平的Box-Be-hnken效应面法设计试验,并对免疫纳米粒的制备进行优化;考察制备出的免疫纳米粒的抗体活性保存率及稳定性。结果优化后的处方是2-亚氨基硫烷盐酸盐50μg、DOX-A-NPs与Bevacizumab质量比为27.5 mg.mg-1、NHS-PEG3500-MAL用量为8.8 mg,以此处方制得的免疫纳米粒粒径为(216.1±2.31)nm、载药量为(28.93±0.94)%、包封率为(80.39±2.83)%,测得值与预测值相差较小。结论采用Box-Behnken效应面法优化并制备阿霉素白蛋白免疫纳米粒是可行的。
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| 关 键 词： | 贝伐单抗 阿霉素 免疫纳米粒 Box-Behnken效应面法 制备工艺 |
Preparation optimization of bevacizumab-mediated,doxorubicin-loaded albumin nanoparticles |
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| LI Lei,ZHAO Xiu-li,QIAO Ming-xi,HU Hai-yang,CHEN Da-wei,YANG Chun-rong.Preparation optimization of bevacizumab-mediated,doxorubicin-loaded albumin nanoparticles[J].Central South Pharmacy,2011,9(9):641-644. |
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| Authors: | LI Lei ZHAO Xiu-li QIAO Ming-xi HU Hai-yang CHEN Da-wei YANG Chun-rong |
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| Affiliation: | LI Lei1,ZHAO Xiu-li1,QIAO Ming-xi1,HU Hai-yang1,CHEN Da-wei1,YANG Chun-rong2(1.School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,2.School of Pharmacy,Jiamusi University,Jiamusi Heilongjiang 154001) |
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| Abstract: | Objective To optimize the preparation of bevacizumab-mediated,doxorubicin-loaded albumin nanoparticles with Box-Behnken design-response surface methodology.Methods Based on the preparation of doxorubicin-loaded albumin nanoparticles,hetero-bifunctional crosslinker NHS-PEG3500-MAL was employed to couple bevacizumab with drug-loaded albumin nanoparticles.The amount of 2-iminothiolane,weight-ratio of drug-loaded albumin nanoparticles and bevacizumab,and the amount of crosslinker were used as influencing factor... |
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| Keywords: | bevacizumab doxorubicin immuno-nanoparticle Box-Behnken response surface methodology preparation technique |
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