Co-delivery of quercetin and caffeic-acid phenethyl ester by polymeric nanoparticles for improved antitumor efficacy in colon cancer cells

• Published in: Journal of microencapsulation Vol. 38; no. 6; pp. 381 - 393
• Main Authors: Colpan, Reyhan Dilsu, Erdemir, Aysegul
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 18.08.2021
• Subjects: anti-cancer; caffeic-acid phenethyl ester; colon cancer; Colonic Neoplasms - drug therapy; Esters; Humans; nanoparticle; Nanoparticles; Particle Size; Polyglycolic Acid; Quercetin; Quercetin - pharmacology; nanoparticle; caffeic-acid phenethyl ester; anti-cancer; colon cancer; Quercetin
• ISSN: 0265-2048; 1464-5246; 1464-5246
• DOI: 10.1080/02652048.2021.1948623

This study aimed to synthesise quercetin- caffeic-acid phenethyl ester (CAPE)-co-loaded poly(lactic-co-glycolic-acid) (PLGA) nanoparticles (QuCaNP) and investigate their anti-cancer activity on human colorectal carcinoma HT-29 cells. QuCaNPs were synthesised using single-emulsion (o/w) solvent evaporation method. Particle size, zeta potential, polydispersity index, in vitro release profile, and surface morphology of QuCaNPs were determined. Cytotoxicity, anti-migration, anti-proliferation and apoptotic activities of QuCaNPs were studied. Mean diameter of QuCaNP was 237.8 ± 9.670 nm, with a polydispersity index (PDI) of 0.340 ± 0.027. Encapsulation efficiency was 74.28% (quercetin) and 65.24% (CAPE). Particle size and drug content of QuCaNP remained stable for 30 days at −20 °C. The half-maximal inhibitory concentration (IC 50 ) values of QuCaNP-treated HT-29 cells were calculated as 11.2 µg/mL (24 h) and 8.2 µg/mL (48 h). QuCaNP treatment increased mRNA levels of caspase-3 (2.38 fold) and caspase-9 (2-fold) and expressions of key proteins in the intrinsic apoptosis pathway in HT-29 cells. Overall, our results demonstrated QuCaNPs exhibits improved anti-cancer activity on HT-29 cells.