The use of conventional chemotherapeutic drugs was emerged as challenging for breast cancer therapy, because breast cancer stem cells cannot be destroyed due to their great nature of drug resistance. In this study, a novel nanoparticulate system of Herceptin (HER)-immobilized salinomycin (SAL)-encapsulated poly(lactic-co-glycolic acid) (PLGA) (HER-SAL-PLGA) nanoparticles were constructed and investigated for breast cancer targeting. SAL-encapsulated PLGA nanoparticles were characterized for their particle size, morphology, structural and thermal properties, and drug-encapsulation efficiency. HER-SAL-PLGA nanoparticles were characterized via particle size, surface chemistry, and herceptin-immobilization efficiency. In vitro release studies were performed for both nontargeting and targeting SAL-PLGA nanoparticles, which demonstrated a controlled release of SAL from nanoparticles. Cellular uptake of the HER-SAL-PLGA nanoparticles was assessed by fluorescence and optical microscopy and flow cytometry, which showed that the HER-SAL-PLGA nanoparticles were successfully uptaken by MCF7 cells. In conclusion, this novel drug-delivery system, HER-SAL-PLGA, was suggested as a promising targeting system for breast cancer therapy.
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