The Effects of Spacer Length and Composition on Aptamer-Mediated Cell-Specific Targeting with Nanoscale PEGylated Liposomal Doxorubicin

Hang Xing, Ji Li, Weidong Xu, Kevin Hwang, Peiwen Wu, Qian Yin, Zhensheng Li, Jianjun Cheng, Yi Lu

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1111-1117
Number of pages7
JournalChemBioChem
DOIs
StatePublished - Jun 16 2016

Keywords

  • DNA aptamers
  • PEG modification
  • drug delivery
  • liposomes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry

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