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Tamoxifen-loaded TPGS-PLGA nanoplatform for breast cancer therapy: insights into drug delivery, distribution, treatment efficacy, and ultrasound/photoacoustic imaging
Tamoxifen-loaded TPGS-PLGA nanoplatform for breast cancer therapy
Abstract
Aims
The objective of the present study was to develop and characterize tamoxifen (TAM)-loaded TPGS-PLGA nanoparticles (NPs) for more effective breast cancer treatment than conventional therapy.
Highlights
- Tamoxifen-loaded TPGS–PLGA nanoparticles were effectively fabricated via an emulsion-solvent evaporation technique to enhance breast cancer treatment.
- The nanoparticles demonstrated a nanoscale dimension (~171 nm), a positive surface charge, and a high drug entrapment efficiency (>93%).
- TAM@TPGS-PLGA nanoparticles exhibited marked pH-responsive drug release, with substantially increased release under acidic conditions that emulate the tumor microenvironment.
- In vitro cytotoxicity assessments demonstrated that TAM@TPGS-PLGA nanoparticles exhibited a 6.21-fold greater cytotoxic effect, compared to free tamoxifen against MCF-7 breast cancer cells.
- The nanoparticles demonstrated exceptional hemocompatibility and organ safety, indicating strong biocompatibility for systemic administration.
- In vivo ultrasound and photoacoustic imaging verified the tumor-specific accumulation of the nanoparticles within a DMBA-induced breast cancer rat model.
- Treatment with TAM@TPGS-PLGA nanoparticles markedly inhibited tumor progression relative to free drug and control groups.
- The integrated therapeutic and imaging functionalities underscore the potential of TAM@TPGS-PLGA nanoparticles as a theranostic platform for targeted breast cancer therapy.
Materials and methods
TAM@TPGS-PLGA-NPs were developed using the emulsion-solvent evaporation method. Furthermore, various physicochemical characterizations were performed. In addition, cytotoxicity, in vitro hemocompatibility, histopathological, and imaging studies were conducted to evaluate the safety and efficacy of the formulation.
Results
TAM@TPGS-PLGA-NPs had a particle size of 171.5 ± 7.3 nm, zeta potential of +34.08 ± 3.14 mV, and an entrapment efficiency was found to be 93.64 ± 1.86%, respectively. At an acidic pH of 5.5, TAM@TPGS-PLGA-NPs exhibited higher drug release compared to pH 7.4. In vitro cytotoxicity study revealed that TAM@TPGS-PLGA-NPs were 6.21-fold more cytotoxic than free TAM. The formulation exhibited excellent hemocompatibility and organ safety. In vivo ultrasound/photoacoustic imaging confirmed tumor‐selective accumulation and significantly suppressed tumor progression in the DMBA-induced female SD rats breast cancer model.
Discussion
The developed TAM@TPGS-PLGA-NPs demonstrated enhanced drug release in the tumor microenvironment, significantly improved cytotoxicity, and excellent biocompatibility compared to the free drug. These findings indicate their strong potential for tumor-targeted breast cancer therapy with reduced systemic toxicity and enhanced therapeutic efficacy.
Continue reading here
Patil, D., Vaishali, Randhave, N. V., Setia, A., Kumar, V., Rani, K., … Muthu, M. S. (2026). Tamoxifen-loaded TPGS-PLGA nanoplatform for breast cancer therapy: insights into drug delivery, distribution, treatment efficacy, and ultrasound/photoacoustic imaging. Nanomedicine, 1–12. https://doi.org/10.1080/17435889.2026.2624743
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