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叶酸修饰去甲斑蝥素隐形泡囊的制备、表征及体外药效学评价 被引量:4
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作者 刘洪月 杨红 +7 位作者 吴秀凤 冒华建 龚珠萍 万智慧 张炜 吴有明 顾睿南 韩楠楠 《中国新药杂志》 CAS CSCD 北大核心 2013年第18期2174-2178,共5页
目的:制备叶酸修饰去甲斑蝥素隐形泡囊新型给药系统,并进行表征及体外药效学评价。方法:采用改良注入法制得新型给药系统,考察其形态、粒径、包封率和体外释放特性等理化性质对其进行表征,并通过它对叶酸受体过度表达Hela细胞的体外细... 目的:制备叶酸修饰去甲斑蝥素隐形泡囊新型给药系统,并进行表征及体外药效学评价。方法:采用改良注入法制得新型给药系统,考察其形态、粒径、包封率和体外释放特性等理化性质对其进行表征,并通过它对叶酸受体过度表达Hela细胞的体外细胞摄取试验及生长抑制试验,进行体外药效学评价。结果:研制的隐形泡囊新型给药系统的平均粒径为100.87 nm,包封率为52.3%,体外释放显著缓慢于游离药物,且在模拟正常细胞pH 7.4环境下的释放t1/2是在模拟肿瘤细胞pH 5.0的1.98倍。细胞摄取试验说明叶酸泡囊能提高肿瘤细胞对药物的摄取(P<0.01)。细胞毒性试验证实,叶酸泡囊抑制肿瘤细胞生长的作用显著(P<0.01),但游离叶酸可减轻叶酸泡囊对肿瘤细胞的杀伤作用。结论:本研究采用简单易行的方法制得的叶酸修饰去甲斑蝥素隐形泡囊,体外具有pH敏感性、隐形性、叶酸受体靶向性,是一种具有良好开发前景的主动靶向抗肿瘤新型给药系统。 展开更多
关键词 去甲斑蝥素 叶酸修饰隐形泡囊 理化性质 体外细胞试验
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Effect of poly(ethylene glycol) modified polyethylenimine polyelectrolyte complex on pharmaceutical characteristics and uptake on breast cancer cell 被引量:1
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作者 刘立婷 齐宪荣 《Journal of Chinese Pharmaceutical Sciences》 CAS 2008年第4期291-296,共6页
Cationic polyethylenimine (PEI) with dextran fluorescein anionic (DFA) or oligodeoxynucleotide (ODN) could form polyelectrolyte complex by self-assembly as a gene delivery vector. This study was designed to inve... Cationic polyethylenimine (PEI) with dextran fluorescein anionic (DFA) or oligodeoxynucleotide (ODN) could form polyelectrolyte complex by self-assembly as a gene delivery vector. This study was designed to investigate the effects on pharmaceutical characteristics and cell uptake PEI after a long-circulation modification with poly(ethylene glycol) (PEG). DFA or ODN reacted with PEI or PEI-PEG to form polyelectrolyte complexes. Surface characters of these complexes and the retardation of ODN by PEI and PEI-PEG were evaluated. The uptake rates of DFA/PEI and DFA/PEI-PEG complexes by MCF-7 cells were evaluated by flow cytometry. Confocal laser scanning microscopy was utilized to visualize the internalization of these complexes. ODN/PEI complex showed the dependence of their size and ξ potential on the N/P ratio. ODN/PEI-PEG complex were much less affected by N/P ratio and their size was around 30 100 nm. PEI and PEI-PEG retarded ODN even at N/P ratio as low as 4, and complete retardation was found at N/P ratio of 8. The uptake rate by MCF-7 cells was direct correlated to the DFA concentration and incubation time, and the uptake rate could exceed 99% under the selected condition. The results in this study showed that PEI self-assembly polyelectrolyte complex after stealth or long circulation modification may increase the ability as a gene vector to delivery genes into cells. 展开更多
关键词 Polyelectrolyte complex POLYETHYLENIMINE Uptake rate SELF-ASSEMBLY Breast cancer cell
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