Everolimus loaded NPs with FOL targeting: preparation, characterization and study of its cytotoxicity action on MCF-7 breast cancer cell lines

Abstract

Background and objective: The mortality cases of breast cancer (BC) are probably caused by inadequate of the benefits of treatment and early detection, moreover the lack of appropriate facilities for diagnosis and detection, also high cost effective of the treatment. The preparation of Everolimus (EV) loaded PLGA-TPGS NPs (nano-EV) targeting with folate (PLGA-TPGS-EV-FOL) and investigate their toxicity effect on human MCF-7 BC cell lines may be given an appropriate lines in BC treatment. Methods: EV loaded NPs were prepared by combination of sonication and emulsification/solvent evaporation method with slight modifications into four formulations A, B, C , and D. EV loaded NPs were characterized by FESEM and TEM for particle size (PS) and zeta potential (ZP), FT-IR, drug loading (DL%), encapsulation efficiency (EE%), In vitro drug release, inhibition concentration IC50 and cell viability%, apoptosis, angiogenesis, glucose transporting, and HIF-1A mRNA gene expression. Results: Formulation B of EV loaded NPs was found to be lowest PS 100±12.7 nm, PDI 0.152, and have ZP, -23.2.5. The higher DL% content of EV was detected as 7.32±1.1% and EE% was 87± 2.6% in formulation B. The results suggested that the free EV dissolution was 80% within 4h but release profile of A, B, C, and D formulations within 4h were 34, 23, 26, 30%, respectively. EV formulated in NPs showed better effects against the MCF-7 BC cell line than EV free and EV loaded NPs formulation B achieved even better therapeutic effect than A, C, and D formulations. HIF-1A mRNA gene expression was decreased when treated the MCF-7 BC cells with EV loaded NPs formulation B compare to expression in untreated cells. Conclusion: EV loaded NPs may be useful in lowering the cost of treatment and may be involved in the decline of chemotherapy side effects.