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 journalArticle

13 Citations (Scopus)

Abstract

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
Volume14
Issue number1
DOIs
Publication statusPublished - Feb 19 2016

Fingerprint

Polyetherimides
Liposomes
Tamoxifen
Polyethylene glycols
Breast Neoplasms
Tumors
Skin
Neoplasms
Drug delivery
Estrogen Receptors
Pharmaceutical Preparations
Bearings (structural)
Therapeutics
Cells
poly(ethylene glycol)-co-poly(ethyleneimine)
Drug Utilization
Zeta potential
Drug Delivery Systems
Cytotoxicity
Growth

Keywords

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

ASJC Scopus subject areas

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

Cite this

Lin, Y. L., Chen, C. H., Wu, H. Y., Tsai, N. M., Jian, T. Y., Chang, Y. C., ... Liao, K. W. (2016). Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex. Journal of Nanobiotechnology, 14(1), [11]. https://doi.org/10.1186/s12951-016-0163-3

Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex. / Lin, Yu Ling; Chen, Chia Hung; Wu, Hsin Yi; Tsai, Nu Man; Jian, Ting Yan; Chang, Yuan Ching; Lin, Chi Hsin; Wu, Chih Hsiung; Hsu, Fei Ting; Leung, Ting-Kai; Liao, Kuang Wen.

In: Journal of Nanobiotechnology, Vol. 14, No. 1, 11, 19.02.2016.

Research output: Contribution to journalArticle

Lin, YL, Chen, CH, Wu, HY, Tsai, NM, Jian, TY, Chang, YC, Lin, CH, Wu, CH, Hsu, FT, Leung, T-K & Liao, KW 2016, 'Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex', Journal of Nanobiotechnology, vol. 14, no. 1, 11. https://doi.org/10.1186/s12951-016-0163-3
Lin, Yu Ling ; Chen, Chia Hung ; Wu, Hsin Yi ; Tsai, Nu Man ; Jian, Ting Yan ; Chang, Yuan Ching ; Lin, Chi Hsin ; Wu, Chih Hsiung ; Hsu, Fei Ting ; Leung, Ting-Kai ; Liao, Kuang Wen. / Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex. In: Journal of Nanobiotechnology. 2016 ; Vol. 14, No. 1.
@article{79e09fb5858045c88e2c1878a5270e58,
title = "Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex",
abstract = "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.",
keywords = "Breast cancer, Lipo-PEG-PEI complex, Tamoxifen, Transdermal treatment",
author = "Lin, {Yu Ling} and Chen, {Chia Hung} and Wu, {Hsin Yi} and Tsai, {Nu Man} and Jian, {Ting Yan} and Chang, {Yuan Ching} and Lin, {Chi Hsin} and Wu, {Chih Hsiung} and Hsu, {Fei Ting} and Ting-Kai Leung and Liao, {Kuang Wen}",
year = "2016",
month = "2",
day = "19",
doi = "10.1186/s12951-016-0163-3",
language = "English",
volume = "14",
journal = "Journal of Nanobiotechnology",
issn = "1477-3155",
publisher = "BioMed Central",
number = "1",

}

TY - JOUR

T1 - Inhibition of breast cancer with transdermal tamoxifen-encapsulated lipoplex

AU - Lin, Yu Ling

AU - Chen, Chia Hung

AU - Wu, Hsin Yi

AU - Tsai, Nu Man

AU - Jian, Ting Yan

AU - Chang, Yuan Ching

AU - Lin, Chi Hsin

AU - Wu, Chih Hsiung

AU - Hsu, Fei Ting

AU - Leung, Ting-Kai

AU - Liao, Kuang Wen

PY - 2016/2/19

Y1 - 2016/2/19

N2 - 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.

AB - 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.

KW - Breast cancer

KW - Lipo-PEG-PEI complex

KW - Tamoxifen

KW - Transdermal treatment

UR - http://www.scopus.com/inward/record.url?scp=84959355232&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84959355232&partnerID=8YFLogxK

U2 - 10.1186/s12951-016-0163-3

DO - 10.1186/s12951-016-0163-3

M3 - Article

C2 - 26892504

AN - SCOPUS:84959355232

VL - 14

JO - Journal of Nanobiotechnology

JF - Journal of Nanobiotechnology

SN - 1477-3155

IS - 1

M1 - 11

ER -