文獻(xiàn)：DSPE-MPEG2000修飾的七葉素納米結(jié)構(gòu)脂質(zhì)載體的體內(nèi)外評(píng)價(jià)及*結(jié)腸炎活性

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

作者：馮石，殷文雄，邁克爾·阿杜-弗林蓬，李瀟瀟，夏曉麗，孫偉剛，浩吉，埃爾穆拉特·托列尼亞佐夫，王啟龍，夏草ORCID圖標(biāo)，江南于&徐熙明

節(jié)選：

客觀的

將七葉亭封裝于DSPE-MPEG2000載體中，以提高其水溶性和口服生物利用度，并增強(qiáng)其對(duì)葡聚糖硫酸鈉（DSS）誘發(fā)的小鼠潰瘍性結(jié)腸炎模型的*炎作用。

方法

建立了七葉素體內(nèi)外高效液相色譜(HPLC)分析方法；采用薄膜分散法制備七葉素納米結(jié)構(gòu)脂質(zhì)載體(Esc-NLC)，用粒度分析儀測(cè)定Esc-NLC的粒徑(PS)和電位(ZP)，用透射電子顯微鏡(TEM)觀察其形貌，用HPLC測(cè)定其載藥量(DL)、包封率(EE)和制劑的體外釋放度，并考察藥代動(dòng)力學(xué)參數(shù)。此外，通過(guò)HE染色切片組織病理學(xué)檢查和ELISA試劑盒檢測(cè)血清中*壞死因子-α(TNF-α)、白細(xì)胞介素(IL)-1β(β)、IL-6的濃度，評(píng)價(jià)其*結(jié)腸炎作用。

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pg電子官方生物提供相關(guān)產(chǎn)品：

DSPE-PEG-Glycine triarginine

DODMA

DSPE-PEG-TH（二硬脂�；�磷脂酰乙醇胺-聚乙二醇-PH響應(yīng)性細(xì)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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