64 Cu via pre or post-labeling for PET imaging of tumor tissues. One representative
example is provided by Lee et al. [59], in which azide functionalized glycol chitosan nanoparticles (CNPs) were conjugated with
64 Cu labeled DBCO via the
copper free click chemistry to yield the
64 Cu labeled CNPs. Labeled CNPs were
subsequently administrated to mice bearing the SCC tumor, and the PET imaging
results demonstrate the clear visualization of tumor tissues with this type of
64 Cu
labeled CNPs, rendering their potential clinical applications for the tumor detection.
Besides
18
F and
64 Cu,
89 Zr has also been considered as a promising radionuclide
for radiolabeling of nanoparticles for PET imaging. The major advantage of
89 Zr
includes its preferred imaging characteristics as well as its relatively long half-life
time (3.3 days), which well matches the time frame of the EPR process. Ruggiero
et al. [60] reported the
89 Zr labeling of single walled nanotubes (SWNT) for PET
imaging. In their study, SWNT conjugated with an antiVE-cad (vascular
endothelial cadherin) antibody was labeled with
89 Zr, which was subsequently
applied in the imaging of human colon adenocarcinoma on a mouse model via
targeting angiogenesis. High uptakes in targeted tissues were identified with a fast
blood clearance, demonstrating the great potential for detecting malignant tissues.
In addition to PET imaging, applications of nanoparticles in SPECT imaging for
tumor diagnosis have also been reported. Harrington et al. reported their successful
evaluation of seventeen patients with different types of cancer using
111 In-DTPA-labeled liposomes [61]. Another example was the application of
188 Re
labeled liposomes in imaging C26-colon tumor on a mice model. Results indicated
high tumor uptakes at all time points, indicating this type of nanodevice could be an
ideal diagnostic tool for tumor detection [62].
12.5.2 Applied in Image Guided Therapy
Besides diagnosis, another major application of radioisotope labeled nanoparticles
is image-guided therapy.
Feng et al. reported the construction of
64 Cu labeled mesoporous silica (mSiO 2 )
nanoparticles as well as the subsequent evaluation of its in vivo performance for
tumor-targeting drug delivery [63]. The TRC105 antibody-attached nanoparticles
exhibited excellent tumor accumulation due to the combinatory effects of passive
EPR and active TRC105 mediated tumor targeting. Further tumor targeted delivery
of Doxorubicin using this designed nanoplatform successfully improved the efficiency of drug delivery, rendering the developed mSiO 2 nanoparticles could serve
as a promising vehicle for tumor targeted drug delivery.
Another representative example could be
64 Cu labeled melanin nanoparticles
(MNPs) that has been used to investigate their efficiency on delivering sorafenib to
the tumor site [64]. PET imaging results revealed a peak tumor uptake at 4 h post
injection, which was consistent with the results obtained from in vitro cumulative
release study, where less than 20% of loaded sorafenib was released from MNPs in
the first 4 h. Those study results indicated that the designed MNPs could efficiently
12 Click Chemistry for Radionanomedicine Platform
243
example is provided by Lee et al. [59], in which azide functionalized glycol chitosan nanoparticles (CNPs) were conjugated with
64 Cu labeled DBCO via the
copper free click chemistry to yield the
64 Cu labeled CNPs. Labeled CNPs were
subsequently administrated to mice bearing the SCC tumor, and the PET imaging
results demonstrate the clear visualization of tumor tissues with this type of
64 Cu
labeled CNPs, rendering their potential clinical applications for the tumor detection.
Besides
18
F and
64 Cu,
89 Zr has also been considered as a promising radionuclide
for radiolabeling of nanoparticles for PET imaging. The major advantage of
89 Zr
includes its preferred imaging characteristics as well as its relatively long half-life
time (3.3 days), which well matches the time frame of the EPR process. Ruggiero
et al. [60] reported the
89 Zr labeling of single walled nanotubes (SWNT) for PET
imaging. In their study, SWNT conjugated with an antiVE-cad (vascular
endothelial cadherin) antibody was labeled with
89 Zr, which was subsequently
applied in the imaging of human colon adenocarcinoma on a mouse model via
targeting angiogenesis. High uptakes in targeted tissues were identified with a fast
blood clearance, demonstrating the great potential for detecting malignant tissues.
In addition to PET imaging, applications of nanoparticles in SPECT imaging for
tumor diagnosis have also been reported. Harrington et al. reported their successful
evaluation of seventeen patients with different types of cancer using
111 In-DTPA-labeled liposomes [61]. Another example was the application of
188 Re
labeled liposomes in imaging C26-colon tumor on a mice model. Results indicated
high tumor uptakes at all time points, indicating this type of nanodevice could be an
ideal diagnostic tool for tumor detection [62].
12.5.2 Applied in Image Guided Therapy
Besides diagnosis, another major application of radioisotope labeled nanoparticles
is image-guided therapy.
Feng et al. reported the construction of
64 Cu labeled mesoporous silica (mSiO 2 )
nanoparticles as well as the subsequent evaluation of its in vivo performance for
tumor-targeting drug delivery [63]. The TRC105 antibody-attached nanoparticles
exhibited excellent tumor accumulation due to the combinatory effects of passive
EPR and active TRC105 mediated tumor targeting. Further tumor targeted delivery
of Doxorubicin using this designed nanoplatform successfully improved the efficiency of drug delivery, rendering the developed mSiO 2 nanoparticles could serve
as a promising vehicle for tumor targeted drug delivery.
Another representative example could be
64 Cu labeled melanin nanoparticles
(MNPs) that has been used to investigate their efficiency on delivering sorafenib to
the tumor site [64]. PET imaging results revealed a peak tumor uptake at 4 h post
injection, which was consistent with the results obtained from in vitro cumulative
release study, where less than 20% of loaded sorafenib was released from MNPs in
the first 4 h. Those study results indicated that the designed MNPs could efficiently
12 Click Chemistry for Radionanomedicine Platform
243