Preparation of PEG-PLA-PBCL micelles loaded with chrysin and evaluation of their anticancer effects in B16 cells

Abstract

Chrysin (5,7-dihydroxyflavone) is a natural polyphenol, found in many plants and honey. Chryain has been found to have various biological effects including anti-cancer, anti-metastatic, immune balancing and antioxidant. Chrysin has been also shown to reduce neurotoxicity, neuroinflammation and oxidative stress. The main limitation for the clinical use of Chrysin in the treatment of cancer is the poor aqueous solubility of this compound, which reduces its bioavailability and thus overshadows its therapeutic effects. An important strategy to challenges associated with chrysin poor water solubility is to use nanoparticles. Objective: In this study, chrysin was loaded in PEG-PLA-PCL and PEG-PLA-PBCL nanoparticles and the anticancer effects of prepared Chrysin loaded nanoparticles were evaluated on B16 melanoma cell line.Methods:In this study, chrysin-loaded micelles were prepared with PEG-PLA-PBCL polymer and their physicochemical and anti-cancer properties were evaluated. Crycin was loaded into PEG-PLA-PCL and PEG-PLA-PBCL polymers by acetone common solvent evaporation. For each formulation, particle size was determined by zeta-sizer method and the amount of drug loaded by UV method was determined. To evaluate the anti-cancer effects, B16 cells were cultured as monolayers in RPMI medium containing serum and MTT assays were conducted using standard protocol. The cell viability was determined in order to evaluate the IC50 values for loaded-drug micelles and free drug. Results: Based on the obtained results, the average size of nanoparticles containing drugs was about 35.455±0.84 nm with a plydispersitydispersion rate of 0.602. The drug release profile at 37 °C after 48 hours showed that the percentage of chrysin release was about 34%. The results of the evaluation of cytotoxicity illustrated that the encapsulated drug in the mecile is more cytotoxic compared to that of the free drug. Conclusion: This study indicates the efficiency of encapsulated micelles PEG-PLA-PBCL as a controlled drug delivery system for cryisin in the treatment of cancer