Journal
CHEMBIOCHEM
Volume 17, Issue 12, Pages 1111-1117Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.201600092
Keywords
DNA aptamers; drug delivery; liposomes; PEG modification
Funding
- Beckman Institute of Advanced Science and Technology
- Interdisciplinary Innovation Initiative Program at the University of Illinois at Urbana-Champaign
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Aptamer-based targeted drug delivery systems have shown significant promise for clinical applications. Although much progress has been made in this area, it remains unclear how PEG coating would affect the selective binding of DNA aptamers and thus influence the overall targeting efficiency. To answer this question, we herein report a systematic investigation of the interactions between PEG and DNA aptamers on the surface of liposomes by using a series of nanoscale liposomal doxorubicin formulations with different DNA aptamer and PEG modifications. We investigated how the spatial size and composition of the spacer molecules affected the targeting ability of the liposome delivery system. We showed that a spacer of appropriate length was critical to overcome the shielding from surrounding PEG molecules in order to achieve the best targeting effect, regardless of the spacer composition. Our findings provide important guidelines for the design of aptamer-based targeted drug delivery systems.
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