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Chemoselective Modification of Viral Surfaces via Bioorthogonal Click Chemistry
Published on: August 19, 2012
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In vivo targeting through click chemistry
Yevgeny Brudno1, Rajiv M Desai, Brian J Kwee
1Wyss Institute for Biologically Inspired Engineering, Harvard University, 3 Blackfan Cir., Boston, MA 02115 (USA); School of Engineering and Applied Sciences, Harvard University, 29 Oxford St., Cambridge, MA 02138 (USA).
Chemmedchem
|February 24, 2015
Summary
This study shows bioorthogonal click chemistry can precisely target circulating drugs to diseased tissues using injectable hydrogels. This method allows repeated drug delivery and spatial control, advancing therapeutic applications.
Area of Science:
- Biomedical Engineering
- Drug Delivery
- Chemical Biology
Background:
- Targeting small molecules to diseased tissues for therapy or diagnosis remains a significant challenge in drug delivery.
- Current drug-eluting devices are surgically implanted and lack post-implantation modification capabilities.
Purpose of the Study:
- To demonstrate the utility of bioorthogonal click chemistry for targeting circulating small molecules to intramuscular hydrogels in diseased tissues.
- To show repeated targeting of small molecules to diseased areas over an extended period.
- To illustrate spatial control of drug delivery using multiple bioorthogonal reactions.
Main Methods:
- Utilized bioorthogonal click chemistry to functionalize hydrogels implanted in diseased tissues.
- Administered circulating small molecules for targeted delivery to the hydrogels.
- Employed two distinct bioorthogonal reactions to achieve spatial segregation of co-injected small molecules in a mouse model.
Main Results:
- Successfully targeted circulating small molecules to intramuscular hydrogels in diseased tissues.
- Achieved repeated targeting of small molecules to the same diseased area for over a month.
- Demonstrated the ability to spatially segregate two different small molecules to distinct locations using two bioorthogonal reactions.
Conclusions:
- Bioorthogonal click chemistry offers a versatile platform for targeted pharmacological drug delivery.
- This approach has potential applications in refilling drug depots for cancer therapy, wound healing, and advanced drug-eluting vascular grafts and stents.

