Pharmacokinetics and Biodistribution of Novel Aptamer Compositions

Healy, Judith M.; Lewis, Scott D.; Kurz, Markus; Boomer, Ryan M.; Thompson, Kristin M.; Wilson, Charles B.; McCauley, Thomas G.

doi:10.1007/s11095-004-7676-4

Cited by 258 publications

(235 citation statements)

References 44 publications

(60 reference statements)

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“…This result is in accordance with previous studies which showed that aptamers are not able to cross the BBB passively [35][36][37]. There were no significant differences between the two HER2 aptamers and the negative control aptamer, except a significant increase in kidney uptake for the negative control aptamer, which may be related to the difference in nucleotide sequence and therefore difference in hydrophilicity.…”

Section: Tissue Biodistributionsupporting

confidence: 92%

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Gijs¹,

Becker

Plenevaux

et al. 2016

J Nucl Med Radiat Ther

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Section: Tissue Biodistributionsupporting

confidence: 92%

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Gijs¹,

Becker

Plenevaux

et al. 2016

J Nucl Med Radiat Ther

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“…To retard clearance and improve bioavailability, a cholesterol or polyethylene glycol moiety can be conjugated to one end of the aptamer. 6,7 Still, bioavailability may best be achieved not by making the aptamer drug circulate longer in the system but by increasing its avidity (binding capacity or apparent affinity for its target), which can be realized by multimerizing the aptamers in a controlled fashion. 8 The development of useful therapeutics requires testing in animals before human trials can be carried out, and aptamer development may stall if crossreactivity of the selected human aptamer sequence with the animal model of choice is poor.…”

Section: Prospectsmentioning

confidence: 99%

Gene therapy progress and prospects: RNA aptamers

2007

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Aptamers are oligonucleotides evolved in vitro or in nature to bind target ligands with high affinity and specificity. They are emerging as powerful tools in the fields of therapeutics, drug development, target validation and diagnostics. Aptamers are attractive alternatives to antibody-and small-moleculebased therapeutics owing to their stability, low toxicity, low immunogenicity and improved safety. With the recent approval of the first aptamer drug Macugen by the US FDA, there is great impetus to develop therapeutic aptamers that can target a wide array of disease states. The recent demonstration that aptamer activity can be reversed by the administration of a simple antidote greatly enhances the potential value of aptamers as therapeutic agents.

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“…26,40 Second, the modification of the peptide by PEGylation may enhance nanoprobe hydrophilicity, reduce nonspecific binding, and thus improve bioavailability and clearance when used in vivo. 41,42 For in vivo imaging, Oyster-800 dye was chosen for its biocompatibility and high wavelength (∼800 nm) and because it has minimal tissue absorbance and background with improved fluorescence sensitivity. 43,44 The in vitro experiments demonstrate that the FPRtargeting nanoprobe has high affinity and can specifically bind to neutrophils.…”

Section: Discussionmentioning

confidence: 99%

Real-time detection of implant-associated neutrophil responses using a formyl peptide receptor-targeting NIR nanoprobe

Zhou

Tsai

Hong

et al. 2012

IJN

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Neutrophils play an important role in implant-mediated inflammation and infection. Unfortunately, current methods which monitor neutrophil activity, including enzyme measurements and histological evaluation, require many animals and cannot be used to accurately depict the dynamic cellular responses. To understand the neutrophil interactions around implant-mediated inflammation and infection it is critical to develop methods which can monitor in vivo cellular activity in real time. In this study, formyl peptide receptor (FPR)-targeting nearinfrared nanoprobes were fabricated. This was accomplished by conjugating near-infrared dye with specific peptides having a high affinity to the FPRs present on activated neutrophils. The ability of FPR-targeting nanoprobes to detect and quantify activated neutrophils was assessed both in vitro and in vivo. As expected, FPR-targeting nanoprobes preferentially accumulated on activated neutrophils in vitro. Following transplantation, FPR-targeting nanoprobes preferentially accumulated at the biomaterial implantation site. Equally important, a strong relationship was observed between the extent of fluorescence intensity in vivo and the number of recruited neutrophils at the implantation site. Furthermore, FPR-targeting nanoprobes may be used to detect and quantify the number of neutrophils responding to a catheter-associated infection. The results show that FPR-targeting nanoprobes may serve as a powerful tool to monitor and measure the extent of neutrophil responses to biomaterial implants in vivo.

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Pharmacokinetics and Biodistribution of Novel Aptamer Compositions

Cited by 258 publications

References 44 publications

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Biodistribution of Novel 68Ga-Radiolabelled HER2 Aptamers in Mice

Gene therapy progress and prospects: RNA aptamers

Real-time detection of implant-associated neutrophil responses using a formyl peptide receptor-targeting NIR nanoprobe

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