Evaluation of EGFR targeting cetuximab conjugated temozolomide loaded poly (lactic-co-glycolic acid) nanoparticles for the treatment of cancer.
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초록
내용
Overexpression of the epidermal growth factor receptor (EGFR) is known to accelerate the growth of cancer cells. In this study, cetuximab (Cmab) conjugated temozolomide (TMZ) loaded poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs), termed Cmab-TMZ-PLGA NPs was developed to target EGFR overexpressing cancer cells. TMZ loaded PLGA NPs (TMZ-PLGA NPs) were prepared by the emulsion solvent evaporation method. Cmab was conjugated to PLGA-NPs by EDC/NHS cross-linking chemistry. The mean particle size of Cmab-TMZ-PLGA NPs was 162.26 ± 5.09 nm with spherical surface morphology. Further study showed that Cmab-TMZ-PLGA NPs have higher cellular uptake, higher cytotoxicity, higher apoptotic effect, and upregulated γ-H2A.X expression than TMZ-PLGA NPs and free TMZ in U-87MG, SW480 and SK-Mel 28 cancer cells. Thus, Cmab-TMZ-PLGA-NPs offer a versatile nanoplatform to treat EGFR overexpressing cancers.