Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex

Yu Ling Lin, Chia Hung Chen, Hsin Yi Wu, Nu Man Tsai, Ting Yan Jian, Yuan Ching Chang, Chi Hsin Lin, Chih Hsiung Wu, Fei Ting Hsu, Ting-Kai Leung, Kuang Wen Liao

Research output: Contribution to journalArticlepeer-review

36 Citations (Scopus)


Background: Tamoxifen is currently used for the treatment of both early and advanced estrogen receptor (ER) positive breast cancer in pre- and post-menopausal women. However, using tamoxifen routinely to inhibit endogenous or exogenous estrogen effects is occasionally difficult because of its potential side effects. Objectives: The aim of this study is to design a local drug delivery system to encapsulate tamoxifen for observing their efficacy of skin penetration, drug accumulation and cancer therapy. Methods: A cationic liposome-PEG-PEI complex (LPPC) was used as a carrier for the encapsulation of tamoxifen and forming 'LPPC/TAM' for transdermal release. The cytotoxicity of LPPC/TAM was analyzed by MTT. The skin penetration, tumor growth inhibition and organ damages were measured in xenograft mice following transdermal treatment. Results: LPPC/TAM had an average size less than 270nm and a zeta-potential of approximately 40mV. LPPC/TAM displayed dramatically increased the cytotoxic activity in all breast cancer cells, especially in ER-positive breast cancer cells. In vivo, LPPC drug delivery helped the fluorescent dye penetrating across the skim and accumulating rapidly in tumor area. Administration of LPPC/TAM by transdermal route inhibited about 86% of tumor growth in mice bearing BT474 tumors. This local treatment of LPPC/TAM did not injury skin and any organs. Conclusion: LPPC-delivery system provided a better skin penetration and drug accumulation and therapeutic efficacy. Therefore, LPPC/TAM drug delivery maybe a useful transdermal tool of drugs utilization for breast cancer therapy.

Original languageEnglish
Article number11
JournalJournal of Nanobiotechnology
Issue number1
Publication statusPublished - Feb 19 2016


  • Breast cancer
  • Lipo-PEG-PEI complex
  • Tamoxifen
  • Transdermal treatment

ASJC Scopus subject areas

  • Bioengineering
  • Medicine (miscellaneous)
  • Molecular Medicine
  • Biomedical Engineering
  • Applied Microbiology and Biotechnology
  • Pharmaceutical Science


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