Thermosensitive Poloxamer Liposomal Gel for Sustained FTA Delivery Enhances Anti-Breast Cancer Efficacy and Biosafety.

Authors

Yongqiang Jiang, Meiting Zhang, Mingxuan Liu, Zhilian Su, Yuqian Pu, Wen Li, Hong Shao, Peng Shi, Rong Zhang, Ling Zhao, Yumeng Wei

Published in

International journal of nanomedicine. Volume 21. Pages 616943. Epub Jul 29, 2026.

Abstract

FTA is a new FT derivative developed by our team by modifying FT with aspirin, and it has been shown to boost anti-breast cancer activity.
To significantly enhance the anti-breast cancer efficacy and biosafety of FTA, this study employed Poloxamer F127 and Poloxamer F68 to construct a composite carrier system, successfully prepared FTA-loaded liposomes (FTA-LN) and their thermosensitive gel formulation (FTA-LN-TSG), with systematic in vitro and in vivo assessments performed.
Simultaneously, FTA-LN exhibited an average particle size of 131.03 ± 4.35 nm, polydispersity index (PDI) of 0.265 ± 0.003, zeta potential of -21.46 ± 2.49 mV, and encapsulation efficiency of 94.55 ± 1.10%. FTA-LN followed first-order kinetics, with a cumulative release rate of 68.48% within 4 hours. Conversely, FTA-LN-TSG displayed sustained release characteristics consistent with Higuchi kinetics, reaching a cumulative release of 52.56% at 8 hour. In vitro efficacy evaluation revealed that FTA-LN-TSG exhibited significantly superior inhibitory effects against breast cancer cells compared to FTA (24 h and 48 h inhibition rates: 2.72- and 5.02-fold of FTA; cell migration rate: 37% of FTA). Furthermore, FTA-LN-TSG demonstrated significant differences in inducing apoptosis and cell cycle arrest (Total apoptosis rate of FTA: 25.74, total apoptosis rate of FTA-LN-TSG: 48.84%). Pharmacokinetic results indicated that FTA-LN-TSG exhibited a 3.5-fold prolongation in half-life (t_1/2), and a 6-fold extension in time to peak concentration (T_max) compared with FTA group. In tumor model mice, The FTA-LN-TSG injected beside the tumor was achieved a tumor inhibition rate of 64.42 ± 5.60% (1.82-fold of the FTA group, 1.45-fold of the S-1 group) with favorable biosafety.
In summary, as a novel drug delivery system, FTA-LN-TSG may represent a promising option for breast cancer therapy.

PMID:
42544163
Bibliographic data and abstract were imported from PubMed on 03 Aug 2026.

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