Part IV
Targeted Delivery with Click Chemistry
Chapter 12: Click Chemistry for Radionanomedicine Platform
Chapter 13: Preservation of Ligand Functionality by Click Chemistry
Chapter 14: Bioorthogonal Reaction for Fluorine-18 Labeling
Surface-modified and radiolabeled nanomaterials are now to be delivered to the
targets, i.e., tumors in destructive therapy and injured/degenerative tissues in
regenerative therapy. Targeted delivery is the goal of administering the radionanomaterials or radionanomedicines, in another word, the radiolabeled nanomaterials as pharmaceuticals, to the body. Preserving the functional integrity of the
targeting ligand is now essential for the desired success of targeted delivery, which
will be the bottleneck of the entire endeavor of developing, introducing and
translating the radionanomedicines to humans and clinics. There have been and are
controversy that nanomaterials reach targets by passive delivery or active targeting.
One needs to prove the effectiveness of active targeting over the passive delivery
and this is also the case with radiolabeled nanomaterials. Click chemistry especially
copper-free reaction is now well established so that the remaining works are finding
wider application and optimization for each nanomaterial of interest.
Copper-catalyzed click chemistry should have been avoided because surplus coppers are going to interact with bodily peptides and macromolecules and prevent the
use of Cu-64 or other radiometals competing with the chelation. This meant that
click chemistry should have been aloof from intrinsic biomacromolecules which is
later expressed as “bioorthogonal”. Bioorthogonal reaction among cycloaddition
click chemistry even allowed two-step approach for targeted delivery and their
imaging. Using bioorthogonal reaction and click chemistry, one could follow the
biodistribution of pretargeted biomolecules and nanomaterials by injecting later the
radiolabeled tracer. This could overcome the difference of long half-time of
clearance or accumulation of nanomaterials and the short half-life of tracer.
In this part, the readers will find the multifaceted interpretation, the first of which
in Chap. 12 emphasized the incorporation of proper kinds of click chemistry to
Targeted Delivery with Click Chemistry
Chapter 12: Click Chemistry for Radionanomedicine Platform
Chapter 13: Preservation of Ligand Functionality by Click Chemistry
Chapter 14: Bioorthogonal Reaction for Fluorine-18 Labeling
Surface-modified and radiolabeled nanomaterials are now to be delivered to the
targets, i.e., tumors in destructive therapy and injured/degenerative tissues in
regenerative therapy. Targeted delivery is the goal of administering the radionanomaterials or radionanomedicines, in another word, the radiolabeled nanomaterials as pharmaceuticals, to the body. Preserving the functional integrity of the
targeting ligand is now essential for the desired success of targeted delivery, which
will be the bottleneck of the entire endeavor of developing, introducing and
translating the radionanomedicines to humans and clinics. There have been and are
controversy that nanomaterials reach targets by passive delivery or active targeting.
One needs to prove the effectiveness of active targeting over the passive delivery
and this is also the case with radiolabeled nanomaterials. Click chemistry especially
copper-free reaction is now well established so that the remaining works are finding
wider application and optimization for each nanomaterial of interest.
Copper-catalyzed click chemistry should have been avoided because surplus coppers are going to interact with bodily peptides and macromolecules and prevent the
use of Cu-64 or other radiometals competing with the chelation. This meant that
click chemistry should have been aloof from intrinsic biomacromolecules which is
later expressed as “bioorthogonal”. Bioorthogonal reaction among cycloaddition
click chemistry even allowed two-step approach for targeted delivery and their
imaging. Using bioorthogonal reaction and click chemistry, one could follow the
biodistribution of pretargeted biomolecules and nanomaterials by injecting later the
radiolabeled tracer. This could overcome the difference of long half-time of
clearance or accumulation of nanomaterials and the short half-life of tracer.
In this part, the readers will find the multifaceted interpretation, the first of which
in Chap. 12 emphasized the incorporation of proper kinds of click chemistry to