Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment

In this research, KLA-modified liposomes co-loaded with 5-fluorouracil and paclitaxel (KLA-5-FU/PTX Lps) were developed, and their antitumor activity against triple-negative breast cancer (TNBC) was evaluated. KLA-5-FU/PTX Lps were prepared using the thin-film dispersion method, and their in vitro a...

Full description

Bibliographic Details
Main Authors: Tianyu Chen, Hui Chen, Yichun Jiang, Qi Yan, Shuling Zheng, Min Wu
Format: Article
Language:English
Published: MDPI AG 2022-07-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/15/7/881
_version_ 1797433200297902080
author Tianyu Chen
Hui Chen
Yichun Jiang
Qi Yan
Shuling Zheng
Min Wu
author_facet Tianyu Chen
Hui Chen
Yichun Jiang
Qi Yan
Shuling Zheng
Min Wu
author_sort Tianyu Chen
collection DOAJ
description In this research, KLA-modified liposomes co-loaded with 5-fluorouracil and paclitaxel (KLA-5-FU/PTX Lps) were developed, and their antitumor activity against triple-negative breast cancer (TNBC) was evaluated. KLA-5-FU/PTX Lps were prepared using the thin-film dispersion method, and their in vitro anticancer efficacy was assessed in human breast cancer cells (MDA-MB-231). An MDA-MB-231 tumor-bearing mouse model was also established to evaluate their antitumor efficacy in vivo. KLA-5-FU/PTX Lps showed enhanced cytotoxicity against MDA-MB-231 cells, improved drug delivery to mitochondria, and induced mitochondria-mediated apoptosis. The modified liposomes also showed favorable antitumor activity in vivo due to their strong ability to target tumors and mitochondria. The liposomes showed no obvious systemic toxicity. Our results suggest that KLA-5-FU/PTX Lps are a promising system with which to target the delivery of antitumor drugs to mitochondria as a treatment for TNBC.
first_indexed 2024-03-09T10:13:39Z
format Article
id doaj.art-9e28965e97a342cf83f0bae2b3d65caa
institution Directory Open Access Journal
issn 1424-8247
language English
last_indexed 2024-03-09T10:13:39Z
publishDate 2022-07-01
publisher MDPI AG
record_format Article
series Pharmaceuticals
spelling doaj.art-9e28965e97a342cf83f0bae2b3d65caa2023-12-01T22:33:44ZengMDPI AGPharmaceuticals1424-82472022-07-0115788110.3390/ph15070881Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer TreatmentTianyu Chen0Hui Chen1Yichun Jiang2Qi Yan3Shuling Zheng4Min Wu5School of Pharmacy, Chengdu Medical College, No. 783 Xindu Avenue, Xindu District, Chengdu 610500, ChinaSchool of Healthcare Technology, Chengdu Neusoft University, No. 1 Neusoft Avenue, Dujiangyan District, Chengdu 611830, ChinaSchool of Pharmacy, Chengdu Medical College, No. 783 Xindu Avenue, Xindu District, Chengdu 610500, ChinaSchool of Pharmacy, Chengdu Medical College, No. 783 Xindu Avenue, Xindu District, Chengdu 610500, ChinaSchool of Pharmacy, Chengdu Medical College, No. 783 Xindu Avenue, Xindu District, Chengdu 610500, ChinaSchool of Pharmacy, Chengdu Medical College, No. 783 Xindu Avenue, Xindu District, Chengdu 610500, ChinaIn this research, KLA-modified liposomes co-loaded with 5-fluorouracil and paclitaxel (KLA-5-FU/PTX Lps) were developed, and their antitumor activity against triple-negative breast cancer (TNBC) was evaluated. KLA-5-FU/PTX Lps were prepared using the thin-film dispersion method, and their in vitro anticancer efficacy was assessed in human breast cancer cells (MDA-MB-231). An MDA-MB-231 tumor-bearing mouse model was also established to evaluate their antitumor efficacy in vivo. KLA-5-FU/PTX Lps showed enhanced cytotoxicity against MDA-MB-231 cells, improved drug delivery to mitochondria, and induced mitochondria-mediated apoptosis. The modified liposomes also showed favorable antitumor activity in vivo due to their strong ability to target tumors and mitochondria. The liposomes showed no obvious systemic toxicity. Our results suggest that KLA-5-FU/PTX Lps are a promising system with which to target the delivery of antitumor drugs to mitochondria as a treatment for TNBC.https://www.mdpi.com/1424-8247/15/7/8815-fluorouracilpaclitaxelliposomesmitochondrial targetingTNBC
spellingShingle Tianyu Chen
Hui Chen
Yichun Jiang
Qi Yan
Shuling Zheng
Min Wu
Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
Pharmaceuticals
5-fluorouracil
paclitaxel
liposomes
mitochondrial targeting
TNBC
title Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
title_full Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
title_fullStr Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
title_full_unstemmed Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
title_short Co-Delivery of 5-Fluorouracil and Paclitaxel in Mitochondria-Targeted KLA-Modified Liposomes to Improve Triple-Negative Breast Cancer Treatment
title_sort co delivery of 5 fluorouracil and paclitaxel in mitochondria targeted kla modified liposomes to improve triple negative breast cancer treatment
topic 5-fluorouracil
paclitaxel
liposomes
mitochondrial targeting
TNBC
url https://www.mdpi.com/1424-8247/15/7/881
work_keys_str_mv AT tianyuchen codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment
AT huichen codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment
AT yichunjiang codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment
AT qiyan codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment
AT shulingzheng codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment
AT minwu codeliveryof5fluorouracilandpaclitaxelinmitochondriatargetedklamodifiedliposomestoimprovetriplenegativebreastcancertreatment