Formulation of resveratrol into PGA-co-PDL nanoparticles increases its cytotoxic potency against lung cancer cells

Abstract

Abstract Objectives Lung cancer is the commonest cause of cancer-related deaths, and current treatment involves the use of cytotoxic drugs that have many unwanted side effects. Resveratrol, a natural polyphenol, has promising anticancer efficacy, but its therapeutic application is hindered by low bioavailability, which the present study sought to improve through encapsulation into nanoparticles (NPs). Methods Resveratrol was loaded into poly(glycerol adipate-co-ω-pentadecalactone) (PGA-co-PDL; MWt 16.5 KDa) NPs with sizes 220–230 nm, and tested against Calu-3 human lung cancer cells. Key findings About 5% and 10% resveratrol nanoparticles (RNPs) had a high encapsulation efficiency of 78 ± 0.24% and 70 ± 0.89% and a drug loading of 39 ± 0.12 µg and 70 ± 0.89 µg (w/w), respectively. The PGA-co-PDL blank NP (BNP) at 1 mg/ml had good cytocompatibility when Calu-3 cells were exposed to it for 24 h (cell viability of 87.5 ± 4.7%). Remarkably, the 5% RNP and 10% RNP lowered, up to 80%, the IC50 for 24 h cytotoxicity of resveratrol against the cells, from 158 ± 16 µM to 32 ± 10 µM and 70 ± 13 µM, respectively. Conclusions Loading of resveratrol into PGA-co-PDL NPs increases its anticancer potency, thus enhancing its prospect for treating lung cancer.