Abstract:
INTRODUCTION:Nanoscale perfluorocarbon (PFC) droplets have been used to create imaging agents and drug delivery vehicles. However, development and characterization of new formulations of PFC droplets are hindered because of the lack of simple methods for quantitative and sensitive assessment of whole body tissue distribution and pharmacokinetics of the droplets. To address this issue, a general-purpose method for radiolabeling the inner core of nanoscale perfluorocarbon droplets with a hydrophobic and lipophobic fluorine-18 compound was developed, so that positron emission tomography (PET) and quantitative biodistribution studies can be employed to evaluate PFC nanodroplets in vivo. METHODS:A robust method to produce [18F]CF3(CF2)7(CH2)3F from a tosylate precursor using [18F]F- was developed. The product's effectiveness as a general label for different PFCs and its ability to distinguish the in vivo behavior of different PFC droplet formulations was evaluated using two types of PFC nanodroplets: fluorosurfactant-stabilized perfluorohexane (PFH) nanodroplets and lipid-stabilized perfluorooctylbromide (PFOB) nanodroplets. In vivo assessment of the 18F-labeled PFH and PFOB nanodroplets were conducted in normal mice following intravenous injection using small animal PET imaging and gamma counting of tissues and fluids. RESULTS:[18F]CF3(CF2)7(CH2)3F was produced in modest yield and was stable with respect to loss of fluoride in vitro. The labeled fluorocarbon was successfully integrated into PFH nanodroplets (~175 nm) and PFOB nanodroplets (~260 nm) without altering their mean sizes, size distributions, or surface charges compared to their non-radioactive analogues. No leakage of the radiolabel from the nanodroplets was detected after droplet formation in vitro. PET imaging and biodistribution data for the two droplet types tested showed significantly different tissue uptake and clearance patterns. CONCLUSION:A convenient method for producing 18F-labeled PFC droplets was developed. The results highlight the potential utility of the strategy for pre-clinical evaluation of different PFC droplet formulations through direct PFC core labeling using a fluorinated radiolabel.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Amir N,Green D,Kent J,Xiang Y,Gorelikov I,Seo M,Blacker M,Janzen N,Czorny S,Valliant JF,Matsuura Ndoi
10.1016/j.nucmedbio.2017.07.001subject
Has Abstractpub_date
2017-11-01 00:00:00pages
27-33eissn
0969-8051issn
1872-9614pii
S0969-8051(17)30125-7journal_volume
54pub_type
杂志文章abstract:INTRODUCTION:The remarkable stability of the 89Zr-DOTA complex has been shown in recent literature. The formation of this complex appears to require 89Zr-chloride as the complexation precursor rather than the more conventional 89Zr-oxalate. In this work we present a method for the direct isolation of 89Zr-chloride from...
journal_title:Nuclear medicine and biology
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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journal_title:Nuclear medicine and biology
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journal_title:Nuclear medicine and biology
pub_type: 杂志文章
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更新日期:1996-11-01 00:00:00
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pub_type: 杂志文章
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更新日期:2005-11-01 00:00:00
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更新日期:1998-02-01 00:00:00
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journal_title:Nuclear medicine and biology
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更新日期:2017-07-01 00:00:00
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