Tetraiodothyroacetic acid-tagged liposomes for enhanced delivery of anticancer drug to tumor tissue via integrin receptor

Sangbin Lee, Jiyeon Kim, Gayong Shim, Sunil Kim, Su Eun Han, Kwangmeyung Kim, Ick Chan Kwon, Yongseok Choi, Young Bong Kim, Chan Wha Kim, Yu Kyoung Oh

Research output: Contribution to journalArticlepeer-review

24 Scopus citations


Nanoparticles have demonstrated potential for promoting drug delivery to tumor sites and enhancing uptake. Here, we report tetraiodothyroacetic acid (tetrac) as a promising new targeting moiety for delivery of anticancer drugs to tumor tissues. Tetrac, an antagonist that blocks the binding of thyroid hormone to integrin αvβ3, was covalently linked to the activated end of pegylated lipid and used to formulate tetrac-tagged pegylated liposomes (TPL). After incubating with TPL for 9 h, cellular accumulation efficiency into A375 human melanoma cells, which express integrin αvβ3 at high density, was high (98.5% ± 0.5% of cells), whereas that in KB cells, which express integrin at a very low density, was much lower (35.1% ± 4.5%). Molecular imaging revealed that TPL preferentially distributed to tumor tissues after systemic administration in mice, where as non-targeting pegylated liposomes were distributed to tumors at background levels. Treatment with the alkyl lysophospholipid anticancer drug edelfosine, encapsulated in TPL, significantly reduced the survival of A375 tumor cells compared to cells treated with edelfosine in pegylated liposomes or with lysophosphatidylcholine encapsulated in TPL. Moreover, intravenous administration of edelfosine in TPL significantly reduced the growth of tumors and prolonged the survival of A375-xenografted mice, providing 100% protection for up to 50 days and some protection until 66 days (0% survival endpoint). In contrast, no untreated mice or mice treated with edelfosine-loaded pegylated liposomes survived up to 50 or 48 days, respectively, after tumor inoculation. These results suggest the potential of tetrac as a new ligand moiety for enhancing the delivery of anticancer drug-loaded nanoparticles to tumors and enhancing the therapeutic efficacy of encapsulated anticancer drugs.

Original languageEnglish
Pages (from-to)213-220
Number of pages8
JournalJournal of Controlled Release
Issue number2
StatePublished - 10 Dec 2012

Bibliographical note

Funding Information:
This work has been financially supported by grants from Ministry of Education, Science and Technology (Nos. 2011K000809 , 2012007005 ), and from the Bio & Medical Technology Development Program of the National Research Foundation funded by the Korean government (MEST) (No. 20110019640 ).


  • Anticancer drug
  • Edelfosine
  • Integrin receptor
  • Liposome
  • Tetraiodothyroacetic acid


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