Preparation and characterization of Chrysin loaded nanoparticles and evaluation of their growth inhibitory effects in B16 melanoma cell line

Abstract

Introduction: Chrysin is a natural compound, which is mostly extracted from plants. It demonstrated useful effects in treatment of human diseases especially cancer [1, 2]. The poor water solubility of chrysin results in low bioavailability and therapeutic efficacy of this compound in cancer treatment [3].

Objective: In the present study, we examined the potential of poly (ethylene glycol) (PEG)-poly (ε-caprolactone) (PCL) and PEG-poly (α-benzylcarboxylate-ε-caprolactone) (PBCL) nanoparticles (NPs) to improve water solubility and anticancer effect of chrysin.

Methods: Co-solvent evaporation method was applied for the synthesis of chrysin-loaded PEG-PCL and PEG-PBCL nanoparticles. Subsequently, UV spectroscopy, dynamic light scattering and dialysis bag method were applied for evaluation of encapsulation efficiency, particle size, PDI and drug release profile, respectively. Anticancer activity of chrysin-loaded NPs was assessed in B16 melanoma cells using MTT assay.

Results: Chrysin-loaded PEG-PBCL and PEG-PCL NPs with 1mg initial drug indicated encapsulation efficiency of 97%±1% and 53%±2%, respectively. Furthermore, chrysin loaded PEG-PBCL and PEG-PCL NPs with 2mg initial drug demonstrated encapsulation efficiency of 91.5±0.71% and 31.33±2.52%, respectively. Chrysin-loaded PEG-PBCL NPs with 1 mg initial drug (PEG-PBCL-1) were 38.18+3.96 nm in size with polydispersity index (PDI) being 0.62±0.23. Furthermore, chrysin-loaded PEG-PBCL NPs with 2 mg initial drug (PEG-PBCL-2) indicated size of 1022.97±62.38 nm and polydispersity index (PDI) of 0.54±0.22. In terms of release profile, PEG-PBCL-1 NPs, showed 24h sustained release (41±8.4%) after a burst release in 30 minutes (26±1.41%). A lower IC50 value (127.9± 4.85 µm) was reported for encapsulated chrysin in PEG-PBCL NPs, when compared to free drug (179.3± 9.05 μM).

Conclusion: These findings revealed that PEG-PBCL micellar NPs can be beneficial vehicles for delivery of chrysin to cancer cells.