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抗人乳腺癌单克隆抗体偶联米托蒽醌白蛋白纳米球的初步研究

CONJUGATION OF MITOXANTRONE LOADED NANOSPHERES AND ANTI-C-erbB-2 MONOCLONAL ANTIBODIES

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【作者】 张志荣龚艳黄园何勤

【Author】 ZHANG Zhi rong, GONG Yan, HUANG Yuan, HE Qin (School of Pharmacy, West China University of Medical Science, Chengdu 610041, China)

【机构】 华西医科大学药学院!四川成都610041

【Abstract】 AIM To improve the treatment efficacy of anti tumor drug mitoxantrone, the conjugation of mitoxantrone loaded nanospheres and anti C erbB 2 monoclonal antibodies were prepared. METHODS Mitoxantrone loaded nanospheres were prepared with emulsion heating solidification technique. A heterobifunctional reagent, N succinimidyl 3 (2 pyridyldithio) propionate (SPDP), was used as the crosslinker of mitoxantrone loaded nanospheres and anti C erbB 2 monoclonal antibodies; pharmaceutical properties of immunonanocapsuls were studied; the conjugates of nanospheres and monoclonal antibodies was confirmed with immunological methods such as slide agglutination test, fluorescent immunossay and rosset formation test, fluorescent staining and scanning electron microscope. RESULTS Mitoxantrone loaded nanospheres were spherical, with smooth surface and median diameter of 0 665 micron. When stored at 3-5, 20-25 and 37℃, RH 75% for three months, the appearance, morphology, size distribution, drug loading and in vitro release characteristics showed no significant change and the stability was satisfactory. The size analysis demonstrated that there was no obvious increase in the particle size of nanoparticles after conjugation. Immunological tests indicate highly selective binding of antibody targeted nanospheres to C erbB 2 overexpressing cells SK BR 3. CONCLUSION The conjugation of mitoxantrone loaded nanospheres and anti C erbB 2 monoclonal antibodies can keep the activity of anti C erbB 2 and increase the therapeutic efficacy of anti mammary cancer drugs.

【基金】 国家杰出青年科学基金资助项目!(3992 5 0 39);国家自然科学基金资助项目!(396 70 86 2 )
  • 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,2001年02期
  • 【分类号】R737.9
  • 【被引频次】30
  • 【下载频次】335
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