Abstract

Several reports have demonstrated that cantharidin is a strong anticancer compound in vitro; however, its in vivo usefulness is often limited due to its high systemic toxicity. In this study, we encapsulated cantharidin into pegylated liposomes and studied its activity against human breast cancer MCF-7 cells in vitro and its systemic toxicity in mice. Another two methods were also used to reduce the dosage of cantharidin, including labeling liposomal cantharidin with octreotide and exposing cells to hyperbaric oxygen. The cytotoxic activity of pegylated liposomal cantharidin was drastically reduced compared with free cantharidin in vitro. Octreotide-labeled pegylated liposomal cantharidin induced cell death by specifically targeting somatostatin receptors in MCF-7 cells. Cell death was augmented with a low dose of cantharidin under hyperbaric oxygen. Liposomal cantharidin had significantly less systemic toxicity than free cantharidin in vivo and also exhibited a high efficacy against antitumor growth in nude mice. These results suggest that the systemic toxicity of cantharidin can be mitigated by liposome encapsulation; however, that did not decrease its antitumor activity.

Original languageEnglish
Pages (from-to)3116-3121
Number of pages6
JournalFood and Chemical Toxicology
Volume46
Issue number9
DOIs
Publication statusPublished - Sep 2008

Fingerprint

Cantharidin
cantharidin
encapsulation
Encapsulation
Liposomes
Toxicity
toxicity
octreotide
Octreotide
MCF-7 Cells
Cell death
cell death
Cell Death
Oxygen
oxygen
Somatostatin Receptors
mice
cells
dosage
Nude Mice

Keywords

  • Cantharidin
  • Hyperbaric oxygen
  • Liposome
  • Octreotide
  • Toxicity

ASJC Scopus subject areas

  • Food Science
  • Toxicology

Cite this

Liposome encapsulation reduces cantharidin toxicity. / Chang, Chun Chao; Liu, Der Zen; Lin, Shyr Yi; Liang, Hong Jen; Hou, Wen Chi; Huang, Wei Jan; Chang, Chih Hsiang; Ho, Feng Ming; Liang, Yu Chih.

In: Food and Chemical Toxicology, Vol. 46, No. 9, 09.2008, p. 3116-3121.

Research output: Contribution to journalArticle

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