DSPE-PEG-Cholic acid胆酸修饰脂质体(功能性脂质体)负载DOX·HCl的特性
参考文献:Novel DSPE-PEG-Cholic Acid-Modified Liposomes with Hepatic Targeting Properties Improve the Anti-Tumor Efficacy of Oral Doxorubicin Hydrochloride for Liver Tumor-Bearing MiceDOI: 笔者: Li, Ying; Yang, Dandan; Zhang, Yun; Zhu, Chunyan论文摘要: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.