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
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