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黄芩苷PEG-PE纳米胶束的制备、表征与细胞毒性研究
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| 篇名： | 黄芩苷PEG-PE纳米胶束的制备、表征与细胞毒性研究 |
| TITLE： | |
| 摘要： | 目的：制备黄芩苷（BAI）聚乙二醇衍生化磷脂酰乙醇胺（BAI@PEG-PE）纳米胶束，并对其进行表征和细胞毒性研究。方法：采用薄膜水化法制备BAI@PEG-PE纳米胶束，观察其外观特征，检测其粒径、多分散系数（PDI）、Zeta电位、载药量、包封率。比较BAI原料药和BAI@PEG-PE纳米胶束在pH 7.4 磷酸盐缓冲液中1～84 h内的释药情况。以香豆素6为荧光探针，观察PEG-PE纳米胶束在H9c2心肌细胞中的分布。将H9c2心肌细胞分为模型组、BAI原料药组和BAI@PEG-PE纳米胶束组，用不含药或含相应药物的无血清DMEM 培养液培养0.5 h后，用异丙肾上腺素诱导心肌细胞凋亡，比较3组细胞的细胞核形态变化、细胞凋亡率和凋亡相关蛋白B淋巴细胞瘤2（Bcl-2）及其X蛋白（Bax）的蛋白表达水平。结果：所制备的BAI@PEG-PE纳米胶束呈现大小比较均一的圆球形，其粒径为（16.7±0.8） nm，PDI为0.11±0.01，Zeta电位为（－18.4±0.6） mV，载药量为（7.84±0.65）％，包封率为（85.7±4.9）％（n＝3），84 h的累积释放度为76.5％，而BAI原料药在24 h内已基本释放完全。PEG-PE纳米胶束可增强H9c2心肌细胞对香豆素6的摄取，且主要聚集在线粒体周围。与模型组比较，BAI原料药组和BAI@PEG-PE纳米胶束组细胞的凋亡形态明显改善，凋亡率明显降低，Bcl-2蛋白表达明显增强，Bax蛋白表达水平明显降低，差异均有统计学意义（P＜0.05或P＜0.01），其中BAI@PEG-PE纳米胶束组的上述效果更明显（P＜0.05或P＜0.01）。结论。成功制得BAI@PEG-PE纳米胶束，其具有明显的缓释作用、心肌靶向性，可预防心肌细胞的凋亡。 |
| ABSTRACT： | OBJECTIVE： To prepare Baicalin-loaded Polyethylene glycol-derivatized phosphatidylethanolamine （BAI@PEG-PE） nanomicelles， and to characterize it and study its cytotoxicity. METHODS： BAI@PEG-PE nanomicelles were prepared by film hydration method and their appearance characteristics were observed. The particle size， polydispersity index， Zeta potential， drug-loading amount and encapsulation efficiency of the nanomicelles were detected. Drug release of BAI raw material and BAI@PEG-PE nanomicelles in pH 7.4 phosphate buffer were compared within 1-84 h. Using coumarin 6 as fluorescent probe， the distribution of PEG-PE nanomicelles in H9c2 cardiomyocytes were observed. H9c2 cardiomyocytes were divided into model group， BAI raw material group and BAI@PEG-PE nanomicelles group. After treated with serum-free DMEM medium containing no or corresponding drugs for 0.5 h， isoproterenol was used to induce cardiomyocyte apoptosis. Nuclear morphology， cell apoptosis rate and protein expression of Bcl-2 and Bax were compared with among 3 groups. RESULTS： Prepared BAI@PEG-PE nanomicelles were uniform globular shape. The particle size was （16.7±0.8） nm， PDI was 0.11±0.01 and Zeta-potential was （－18.4±0.6） mV； drug-loading amount was （7.84±0.65）％， encapsulation efficiency was （85.7±4.9）％ （n＝3）. Accumulative release rate was 76.5％ within 84 h. BAI raw material was released completely within 24 h. PEG-PE nanomicelles could strengthen the intake of coumarin 6 in H9c2 cardiomyocytes， mainly gathering around mitochondria. Compared with model group， the apoptosis morphology of cardiomyocytes were improved significantly in BAI raw material group and BAI@PEG-PE nanomicelles group； apoptosis rate was decreased significantly； protein expression of Bcl-2 was increased significantly； protein expression of Bax was decreased significantly with statistical significance （P＜0.05 or P＜0.01）. Above effects of BAI@PEG-PE nanomicelles group were more significant （P＜0.05 or P＜0.01）. CONCLUSIONS： BAI@PEG-PE nanomicelles are prepared successfully， and show significant sustained-release effect and myocardial targeting， and can prevent cardiomyocyte apoptosis. |
| 期刊： | 2019年第30卷第11期 |
| 作者： | 宁国庆，吴洁，葛晨亮，周定荣，唐义信 |
| AUTHORS： | NING Guoqing，WU Jie，GE Chenliang， ZHOU Dingrong，TANG Yixin |
| 关键字： | 聚乙二醇衍生化磷脂酰乙醇胺；纳米胶束；黄芩苷；体外释放；H9c2心肌细胞 |
| KEYWORDS： | Polyethylene glycol-derivatized phosphatidylethanolamine； Nanomicelles； Baicalin； Release in vitro； H9c2 cardiomyocyte |
| 阅读数： | 617 次 |
| 本月下载数： | 8 次 |
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