Tamoxifen-loaded TPGS-PLGA nanoplatform for breast cancer therapy: insights into drug delivery, distribution, treatment efficacy, and ultrasound/photoacoustic imaging

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.
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.
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.
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.