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

[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.

[MATERIALS AND METHODS] TAM@TPGS-PLGA-NPs were developed using the emulsion-solvent evaporation method. Furthermore, various physicochemical characterizations were performed. In addition, cytotoxicity, 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. 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. 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.