DSPE-PEG-Cholic acid胆酸修饰脂质体（功能性脂质体）负载DOX·HCl的特性-UDP糖丨MOF丨金属有机框架丨聚集诱导发光丨荧光标记推荐西安齐岳生物

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DSPE-PEG-Cholic acid胆酸修饰脂质体（功能性脂质体）负载DOX·HCl的特性

发布时间：2025-06-20 作者：zyl 分享到：

文献：Novel DSPE-PEG-Cholic Acid-Modified Liposomes with Hepatic Targeting Properties Improve the Anti-Tumor Efficacy of Oral Doxorubicin Hydrochloride for Liver Tumor-Bearing Mice

DOI: https://doi.org/10.1166/jbn.2017.2382

作者: Li, Ying; Yang, Dandan; Zhang, Yun; Zhu, Chunyan

摘要：

DSPE-PEG-cholic acid-modified liposomes (functional liposomes) with hepatic targeting via oral administration properties were explored for the loading of DOX·HCl. DSPE-PEG-cholic acid-modified DOX·HCl liposomes (functional DOX·HCl liposomes) were developed as an oral therapy that targets hepatic cancers. Subsequently, the effects of liposome formulations were investigated using in vitro HepG2 cell uptake assays, in vivo intestine distribution and targeting efficacy experiments in orthotopic HepG2 nude mice xenograft tumors and subcutaneous H22 mice xenograft tumors. Functional DOX·HCl liposomes of approximately 100 nm in diameter significantly increased the intracellular uptake of DOX·HCl, revealing strong inhibitory effects on HepG2 cells. Moreover, orally administered functional DOX·HCl liposomes demonstrated stronger antitumor efficacy than DOX·HCl and DOX·HCl liposomes in orthotopic HepG2 xenograft mice, but similar antitumor efficacy to DOX·HCl liposomes in subcutaneous H22 xenograft mice. In further analyses, cardiac and kidney toxicities were significantly reduced after orally administering functional DOX·HCl liposome formulations. The present data indicate that the oral administration of functional DOX·HCl liposomes increases hepatic targeting, provides superior efficacy of suppressing xenograft tumor, and overcomes limited cardiac and kidney toxicity.

探索了通过口服给药具有肝靶向性的DSPE-PEG-胆酸修饰脂质体（功能性脂质体）负载DOX·HCl的特性。开发了DSPE-PEG-胆酸修饰的DOX·HCl脂质体（功能性DOX·HCl-脂质体）作为靶向肝癌的口服疗法。

随后，使用体外HepG2细胞摄取试验、体内肠道分布和原位HepG2裸鼠异种移植肿瘤和皮下H22小鼠异种移植肿瘤的靶向疗效实验研究了脂质体制剂的影响。直径约为100 nm的功能性DOX·HCl脂质体显著增加了DOX·HCI的细胞内摄取，对HepG2细胞显示出强烈的抑制作用。

此外，在原位HepG2异种移植物小鼠中，口服功能性DOX·HCl脂质体比DOX·HCI和DOX·HCl脂质体具有更强的抗肿瘤作用，但在皮下H22异种移植物鼠中，其抗肿瘤作用与DOX·盐酸脂质体相似。在进一步的分析中，口服功能性DOX·HCl脂质体制剂后，心脏和肾脏毒性显著降低。目前的数据表明，口服功能性DOX·HCl脂质体可增加肝靶向性，提供抑制异种移植物肿瘤的优越疗效，并克服有限的心脏和肾脏毒性。