In Vivo Targeting of Metabolically Labeled Cancers with Ultra-Small Silica Nanoconjugates
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Published on: May 8, 2020
Hua Wang1, Li Tang1, Yang Liu1
11. Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, Illinois 61801, USA.
Abstract:
Unnatural sugar-mediated metabolic labeling of cancer cells, coupled with efficient Click chemistry, has shown great potential for in vivo imaging and cancer targeting. Thus far, chemical labeling of cancer cells has been limited to the small-sized azido groups, with the large-sized and highly hydrophobic dibenzocyclooctyne (DBCO) being correspondingly used as the targeting ligand. However, surface modification of nanomedicines with DBCO groups often suffers from low ligand density, difficult functionalization, and impaired physiochemical properties. Here we report the development of DBCO-bearing unnatural sugars that could directly label LS174T colon cancer cells with DBCO groups and subsequently mediate cancer-targeted delivery of azido-modified silica nanoconjugates with easy functionalization and high azido density in vitro and in vivo. This study, for the first time, demonstrates the feasibility of metabolic labeling of cancer cells with large-sized DBCO groups for subsequent, efficient targeting of azido-modified nanomedicines.
Insights
Researchers developed a new method for labeling cancer cells with large DBCO groups using unnatural sugars. This enables efficient, targeted delivery of nanomedicines, overcoming limitations of previous small-labeling techniques for cancer imaging and therapy.
Area of Science:
- Bioconjugation Chemistry
- Cancer Nanomedicine
- Metabolic Labeling
Background:
- Metabolic labeling and click chemistry show promise for in vivo cancer imaging and targeting.
- Current methods are limited to small azido groups, with large dibenzocyclooctyne (DBCO) ligands used for targeting.
- Surface modification of nanomedicines with DBCO often results in low ligand density and poor properties.
Purpose of the Study:
- To develop DBCO-bearing unnatural sugars for direct metabolic labeling of cancer cells.
- To enable targeted delivery of azido-modified nanomedicines to cancer cells using this novel labeling strategy.
- To overcome limitations associated with traditional DBCO functionalization of nanomedicines.
Main Methods:
- Synthesis of DBCO-bearing unnatural sugars.
- Metabolic labeling of LS174T colon cancer cells with DBCO-modified sugars.
- Functionalization of silica nanoconjugates with azido groups.
- In vitro and in vivo evaluation of targeted nanomedicine delivery.
Main Results:
- Successful direct metabolic labeling of colon cancer cells with large DBCO groups.
- Demonstrated easy functionalization and high azido density on nanomedicines.
- Achieved efficient in vitro and in vivo cancer-targeted delivery of azido-modified nanoconjugates.
Conclusions:
- This study pioneers the metabolic labeling of cancer cells with large DBCO groups.
- The developed method facilitates efficient targeting of azido-modified nanomedicines.
- This approach offers a promising strategy for advancing cancer imaging and targeted therapy.
