Preparation and Characterization of MUC-30-Loaded Polymeric Micelles against MCF-7 Cell Lines Using Molecular Docking Methods and In Vitro Study

摘要

MUC-30 is a hydrophobic compound which is active against the MCF-7 cancer cell line. In this study, MUC-30 was loaded in polymeric micelles to improve the water solubility and release rate. For prolonged MUC-30 release, MUC-30 was encapsulated in polymeric micelles using PEG- b -PLA and PEG- b -PCL as materials. Micelles prepared with 1?:?9 per ratios by film hydration achieved the highest entrapment efficiency (EE%). The EE% of MUC-30-loaded PEG- b -PCL micelles was approximately 30% greater than that of PEG- b -PLA micelles, due to the different H-bond formations between MUC-30 and the polymer membrane (PCL, 4; PLA, 3). The cytotoxic activity of MUC-30 against EGFR theoretically presented 399.31?nM (IC 50 ?=?282.26?ng/mL) by molecular docking. In vitro cytotoxic activity of MUC-30 was confirmed by MTT assay. MUC-30 (IC 50 ?=?11?±?0.39?ng/mL) showed three-fold higher activity over MUC-30-loaded PEG- b -PLA micelles (IC 50 ?=?37?±?1.18?ng/mL) and two-fold higher over PEG- b -PCL micelles (IC 50 ?=?75?±?3.97?ng/mL). This was due to the higher release rate of MUC-30 from PEG- b -PLA micelles compared to PEG- b -PCL micelles. Therefore, MUC-30-loaded PEG- b -PLA micelles could be a promising candidate for breast cancer chemotherapy.