Abstract
Nanotargeted liposomes may be modified with targeting peptide on the surface of a prepared liposome to endow specificity and elevate targeting efficiency. The aim of this study was to develop a radioactive targeted nanoparticle, the 111In-cyclic RGDfK-liposome, and its advantage of recognizing the αVβ3 integrin was examined. The cyclic RGDfK modified liposomes were demonstrated the ability to bind the αVβ3 integrin expressed on the surface of human melanoma cell in vitro and in vivo. The effects of the cyclic RGDfK-liposome on the functioning of phagocytes was also examined, showing no considerable negative effects on the engulfment of bacteria and the generation of reactive oxygen species. Based upon these findings, the cyclic RGDfK- liposome is said to be a promising agent for tumor imaging.
Highlights
Liposome is one of nanomedicines originally designed to improve the distribution and target site accumulation of systemically administered therapeutic agents [1,2,3,4]
To generate the cyclic RGDfK-liposome, the peptide was first conjugated to NHSPEG-DSPE to generate PEG-linked-peptide conjugates; the conjugates were inserted into conventional liposome (Figure 1A)
We tested the effect of the cyclic RGDfK-liposome on the αV β3 integrin -mediated cellular adhesion using human malignant melanoma
Summary
Liposome is one of nanomedicines originally designed to improve the distribution and target site accumulation of systemically administered therapeutic agents [1,2,3,4] They are spherical, self-closed formed lipid bilayer with phospholipids in which entrapped radionuclides [5] or pharmaceuticals [6]. 247 keV characteristic X-ray emission), is a commonly used radionuclide for single-photon emission computed tomography (SPECT) imaging. Harrington and his colleague report about the biodistribution and SPECT/CT imaging of 111 In-DTPA-labeled PEGylated liposomes in advanced cancer patients [10]. The quality of generated images was not high enough to be used in patient selection and treatment evaluation
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