Heparin-deoxycholic acid chemical conjugate as an anticancer drug carrier and its antitumor activity

Kyeongsoon Park, Gee Young Lee, Yoo Shin Kim, Mikyung Yu, Rang Woon Park, In San Kim, Sang Yoon Kim, Youngro Byun

Research output: Contribution to journalArticlepeer-review

158 Citations (Scopus)


A chemically modified heparin-DOCA (HD) conjugate was developed as a drug carrier for cancer therapy. HD conjugate was found to have markedly low anticoagulant activity and to form self-assembled nanoparticles in aqueous condition. We observed that HD conjugate prevented squamous cell carcinoma (SCC) and human umbilical vascular endothelial cell (HUVEC) proliferation during BrdU incorporation assays. Here, we prepared doxorubicin-loaded heparin nanoparticles by entrapping doxorubicin into the amphiphilic HD conjugate by physical interaction and characterized the properties of these nanoparticles using Dynamic Light Scattering (DLS) and Atomic Force Microscope (AFM). In this study, doxorubicin-loaded heparin nanoparticles were designed to improve the antitumor effects of nano-sized particles (range of 180 to 210 nm) at high drug-loading efficiencies in the range 64% to 96%. These doxorubicin-loaded heparin nanoparticles displayed sustained drug release patterns. It was confirmed in vivo toxicity studies that HD conjugate did not induce unexpected side effects and that DHN 20 was safer than free DOX. An in vivo study showed that HD conjugate, doxorubicin and DHN 20 (one of doxorubicin-loaded heparin nanoparticles) induced tumor volume reductions of 43%, 56% and 74%, respectively, relative to the saline treated control. These results suggest that the drug-entrapped with heparin nanoparticles might provide a novel therapy for SCC.

Original languageEnglish
Pages (from-to)300-306
Number of pages7
JournalJournal of Controlled Release
Issue number3
Publication statusPublished - 2006 Sept 12
Externally publishedYes

Bibliographical note

Funding Information:
This study was supported by the Next Generation New Technology Development Program of the Ministry of Commerce, Industry, and Energy in Korea (Grant: # 10011353).


  • Antitumor effects
  • Doxorubicin
  • Heparin nanoparticles
  • SCC

ASJC Scopus subject areas

  • Pharmaceutical Science


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