Radiolabeling of Poly(lactic-co-glycolic acid) (PLGA) Nanoparticles with Biotinylated F-18 Prosthetic Groups and Imaging of Their Delivery to the Brain with Positron Emission Tomography | Zendy

Rachael W. Sirianni | Zendy; MingQiang Zheng | Zendy; Toral Patel | Zendy; Thomas Shafbauer | Zendy; Jiangbing Zhou | Zendy; W. Mark Saltzman | Zendy; Richard E. Carson | Zendy; Yiyun Huang | Zendy

Open Access

Radiolabeling of Poly(lactic-co-glycolic acid) (PLGA) Nanoparticles with Biotinylated F-18 Prosthetic Groups and Imaging of Their Delivery to the Brain with Positron Emission Tomography

Author(s) -

Rachael W. Sirianni,

MingQiang Zheng,

Toral Patel,

Thomas Shafbauer,

Jiangbing Zhou,

W. Mark Saltzman,

Richard E. Carson,

Yiyun Huang

Publication year - 2014

Publication title -

bioconjugate chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.279

H-Index - 172

eISSN - 1520-4812

pISSN - 1043-1802

DOI - 10.1021/bc500315j

Subject(s) - biotinylation , chemistry , avidin , plga , biotin , positron emission tomography , radioligand , nanoparticle , biodistribution , glycolic acid , biophysics , lactic acid , nanotechnology , biochemistry , nuclear medicine , materials science , medicine , binding site , biology , bacteria , in vitro , genetics

The avidin-biotin interaction permits rapid and nearly irreversible noncovalent linkage between biotinylated molecules and avidin-modified substrates. We designed a biotinylated radioligand intended for use in the detection of avidin-modified polymer nanoparticles in tissue with positron emission tomography (PET). Using an F-18 labeled prosthetic group, [(18)F]4-fluorobenzylamine, and a commercially available biotin derivate, NHS-PEG4-biotin, [(18)F]-fluorobenzylamide-poly(ethylene glycol)4-biotin ([(18)F]NPB4) was prepared with high purity and specific activity. The attachment of the [(18)F]NPB4 radioligand to avidin-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles was tested by using PET imaging to measure the kinetics of convection-enhanced delivery (CED) of nanoparticles of varying size to the rat brain. PET imaging enabled the direct observation of nanoparticle delivery by measurement of the spatial volume of distribution of radiolabeled nanoparticles as a function of time, both during and after the infusion. This work thus validates new methods for radiolabeling PEG-biotin derivatives and also provides insight into the fate of nanoparticles that have been infused directly into the brain.

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