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.
ASJC Scopus subject areas
- Molecular Medicine
- Biomedical Engineering
- Applied Microbiology and Biotechnology
- Medicine (miscellaneous)
- Pharmaceutical Science
Lin, Y. L., Chen, C. H., Wu, H. Y., Tsai, N. M., Jian, T. Y., Chang, Y. C., Lin, C. H., Wu, C. H., Hsu, F. T., Leung, T-K., & Liao, K. W. (2016). Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex. Journal of Nanobiotechnology, 14(1), . https://doi.org/10.1186/s12951-016-0163-3