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雏菊叶龙胆苷纳米胶束的制备、表征及研究

Preparation, characterization and study of bellidifolin nano-micelles.

作者信息

Gao Fan, Chen Ziyue, Zhou Li, Xiao Xuefeng, Wang Lin, Liu Xingchao, Wang Chenggang, Guo Qiuhong

机构信息

Hebei TCM Formula Preparation Technology Innovation Center, Hebei University of Chinese Medicine Shijiazhuang 050091 People's Republic of China

School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine Tianjin 301617 People's Republic of China.

出版信息

RSC Adv. 2022 Aug 10;12(34):21982-21989. doi: 10.1039/d2ra02779h. eCollection 2022 Aug 4.

DOI:10.1039/d2ra02779h
PMID:36043071
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9364364/
Abstract

Bellidifolin (BEL), a xanthone compound, has significant therapeutic effectiveness in cardiac diseases such as arrhythmias. However, BEL is limited in clinical applications by its hydrophobicity. In this work, we used BEL as the active pharmaceutical ingredient (API), and polyethylene glycol 15-hydroxy stearate (Kolliphor HS15) as the carrier to prepare BEL nano-micelles by a solvent-volatilization method. According to an analysis by differential scanning calorimetry (DSC), BEL was successfully encapsulated in HS15 as BEL nano-micelles with a 90% encapsulation rate, and particle size was 12.60 ± 0.074 nm in the shape of a sphere and electric potential was -4.76 ± 4.47 mV with good stability and sustained release characteristics. In addition, compared with free drugs, these nano-micelles can increase cellular uptake capacity, inhibit the proliferation of human cardiac fibroblasts, and down-regulate the expression of Smad-2, α-SMA, Collagen I, and Collagen III proteins in myocardial cells to improve myocardial fibrosis. In conclusion, the BEL nano-micelles can provide a new way for the theoretical basis for the clinical application of anti-cardiac fibrosis.

摘要

雏菊叶龙胆酮(BEL)是一种呫吨酮化合物,在心律失常等心脏疾病中具有显著的治疗效果。然而,BEL因其疏水性而在临床应用中受到限制。在本研究中,我们以BEL作为活性药物成分(API),聚乙二醇15-羟基硬脂酸酯(科利凡HS15)作为载体,通过溶剂挥发法制备了BEL纳米胶束。差示扫描量热法(DSC)分析表明,BEL成功地以90%的包封率被包裹在HS15中形成BEL纳米胶束,其粒径为12.60±0.074nm,呈球形,电位为-4.76±4.47mV,具有良好的稳定性和缓释特性。此外,与游离药物相比,这些纳米胶束可提高细胞摄取能力,抑制人心脏成纤维细胞的增殖,并下调心肌细胞中Smad-2、α-SMA、I型胶原蛋白和III型胶原蛋白的表达,以改善心肌纤维化。总之,BEL纳米胶束可为抗心肌纤维化临床应用的理论基础提供新途径。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c418/9364364/1415be65f2b7/d2ra02779h-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c418/9364364/9f25499188ee/d2ra02779h-f10.jpg
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