文献：DSPE-MPEG2000修饰的七叶素纳米结构脂质载体的体内外评价及*结肠炎活性

链接：https://www.tandfonline.com/doi/abs/10.1080/02652048.2023.2215345

作者：冯石，殷文雄，迈克尔·阿杜-弗林蓬，李潇潇，夏晓丽，孙伟刚，浩吉，埃尔穆拉特·托列尼亚佐夫，王启龙，夏草ORCID图标，江南于&徐熙明

节选：

客观的

将七叶亭封装于DSPE-MPEG2000载体中，以提高其水溶性和口服生物利用度，并增强其对葡聚糖硫酸钠（DSS）诱发的小鼠溃疡性结肠炎模型的*炎作用。

方法

建立了七叶素体内外高效液相色谱(HPLC)分析方法；采用薄膜分散法制备七叶素纳米结构脂质载体(Esc-NLC)，用粒度分析仪测定Esc-NLC的粒径(PS)和电位(ZP)，用透射电子显微镜(TEM)观察其形貌，用HPLC测定其载药量(DL)、包封率(EE)和制剂的体外释放度，并考察药代动力学参数。此外，通过HE染色切片组织病理学检查和ELISA试剂盒检测血清中*坏死因子-α(TNF-α)、白细胞介素(IL)-1β(β)、IL-6的浓度，评价其*结肠炎作用。

Objective

Encapsulation of esculetin into DSPE-MPEG2000 carrier was performed to improve its water solubility and oral bioavailability, as well as enhance its anti-inflammatory effect on a mouse model of ulcerative colitis that was induced with dextran sulphate sodium (DSS).

Methods

We determined the in-vitro and in-vivo high-performance liquid chromatographic (HPLC) analysis method of esculetin; Esculetin-loaded nanostructure lipid carrier (Esc-NLC) was prepared using a thin-film dispersion method, wherein a particle size analyser was used to measure the particle size (PS) and zeta potential (ZP) of the Esc-NLC, while a transmission electron microscope (TEM) was employed to observe its morphology. Also, HPLC was used to measure its drug loading (DL), encapsulation efficiency (EE) and the in-vitro release of the preparation, as well as investigate the pharmacokinetic parameters. In addition, its anti-colitis effect was evaluated via histopathological examination of HE-stained sections and detection of the concentrations of tumour necrosis factor-alpha (TNF-α), interleukin (IL)-1 beta (β), and IL-6 in serum with ELISA kits.

西安齐岳生物提供相关产品：

DSPE-PEG-Glycine triarginine

DODMA

DSPE-PEG-TH（二硬脂酰基磷脂酰乙醇胺-聚乙二醇-PH响应性细胞穿膜肽)

DMPE-PEG-NH2

m-PEG8-DSPE

Pentacosadiynoic acid-MPEG

C18-PEGn-OH

DSPE-PEG-c(RGDfK)-FITC

iRGD-PEG-MAL

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