iRGD-conjugated DSPE-PEG2000 nanomicelles for targeted delivery of salinomycin for treatment of both liver cancer cells and cancer stem cells.

Abstract

AIMS:

To develop novel iRGD (internalizing Arg-Gly-Asp peptide)-conjugated DSPE-PEG2000 nanomicelles (M-SAL-iRGD) for delivery of salinomycin to both liver cancer cells and cancer stem cells (CSCs).

MATERIALS & METHODS:

The characterization, antitumor activity and mechanism of action of M-SAL-iRGD were evaluated.

RESULTS & CONCLUSION:

M-SAL-iRGD possessed a small size of around 10 nm, and drug encapsulation efficacy higher than 90%. M-SAL-iRGD showed significantly increased cytotoxic effect toward both nontargeted M-SAL (salinomycin-loaded DSPE-PEG2000 nanomicelles) and salinomycin in both liver cancer cells and CSCs. The tissue distribution and antitumor assays in mice bearing liver cancer xenograft confirmed the superior penetration tumor efficacy and antitumor activity of M-SAL-iRGD. M-SAL-iRGD represent a potential effective nanomedicine against liver cancer.

• Authors: Xiaoli Mao, Junjie Liu, Zhirong Gong, He Zhang, Ying Lu, Hao Zou, Yuan Yu, Yan Chen, Zhiguo Sun, Wei Li, Bohua Li, Jie Gao, Yanqiang Zhong
• Journal: Nanomedicine (London, England) (Nanomedicine (Lond)) Vol. 10 Issue 17 Pg. 2677-95 ( 2015) ISSN: 1748-6963 [Electronic] England
• PMID: 26355733 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000)
• AC133 Antigen
• Antigens, CD
• Drug Carriers
• Glycoproteins
• Liposomes
• Micelles
• Oligopeptides
• Peptides
• Phosphatidylethanolamines
• Pyrans
• Neuropilin-1
• Polyethylene Glycols
• salinomycin
• arginyl-glycyl-aspartic acid

Topics

• AC133 Antigen
• Animals
• Antigens, CD (metabolism)
• Cell Line, Tumor
• Drug Carriers (chemistry)
• Drug Delivery Systems
• Gene Expression Regulation, Neoplastic
• Glycoproteins (metabolism)
• Hep G2 Cells
• Humans
• Liposomes (chemistry)
• Liver Neoplasms (drug therapy)
• Male
• Mice
• Mice, Inbred BALB C
• Mice, Nude
• Micelles
• Nanomedicine
• Neoplasm Metastasis
• Neoplasm Transplantation
• Neoplastic Stem Cells (drug effects)
• Neuropilin-1 (metabolism)
• Oligopeptides (chemistry)
• Peptides (metabolism)
• Phosphatidylethanolamines (chemistry)
• Polyethylene Glycols (chemistry)
• Pyrans (administration & dosage, chemistry)
• Rats
• Rats, Sprague-Dawley
• Tissue Distribution