期刊
BIOMATERIALS
卷 34, 期 33, 页码 8491-8503出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.biomaterials.2013.07.055
关键词
Cubosomes; Hexosomes; In vivo; Radio labeling methods; SPECT/CT-imaging; Theranostics
资金
- European Community's Seventh Framework Programme CALIPSO [312284]
- Danish Natural Sciences Research Council (Danscatt)
- University of Eastern Finland
- Academy of Finland [260316]
- Academy of Finland (AKA) [260316, 260316] Funding Source: Academy of Finland (AKA)
We have developed a highly efficient method for the radiolabeling of phytantriol (PHYT)/oleic acid (OA)-based hexosomes based on the surface chelation of technetium-99m (Tc-99m) to preformed hexosomes using the polyamine 1, 12-diamino-3, 6, 9-triazododecane (SpmTrien) as chelating agent. We also report on the unsuccessful labeling of cubosomes using the well-known chelating agent hexamethylpropyleneamine oxime (HMPAO). The Tc-99m-labeled SpmTrien-hexosomes (Tc-99m-SpmTrien-hexosomes) were synthesized with good radiolabeling (84%) and high radiochemical purity (>90%). The effect of radiolabeling on the internal nanostructure and the overall size of these aqueous dispersions was investigated by using synchrotron small angle X-ray scattering (SAXS), dynamic light scattering (DLS), and transmission electron cryo microscopy (cryo-TEM). Further, we show the utility of Tc-99m-SpmTrien-hexosomes for the in vivo imaging of healthy mice using single photon emission computed tomography (SPECT) in combination with computed tomography (CT), i.e. SPECT/CT. SPECT/CT experiments of subcutaneously administered Tc-99m-SpmTrien-hexosomes to the flank of mice showed a high stability in vivo allowing imaging of the distribution of the radiolabeled hexosomes for up to 24 h. These injected Tc-99m-SpmTrien-hexosomes formed a deposit within the subcutaneous adipose tissue, displaying a high biodistribution of similar to 343% injected dose/g tissue (%ID/g), with negligible uptake in other organs and tissues. The developed Tc-99m labeling method for PHYT/OA-based hexosomes could further serve as a useful tool for investigating and imaging the in vivo performance of cubosomal and hexosomal drug nanocarriers. (C) 2013 Elsevier Ltd. All rights reserved.
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