Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles. Issue 1 (1st January 2019)

• Record Type: Journal Article
• Authors: Yoncheva, Krassimira; Tzankova, Virginia; Yordanov, Yordan; Tzankov, Borislav; Grancharov, Georgy; Aluani, Denitsa; Bankova, Vassya; Popova, Milena; Trusheva, Boryana; Kondeva-Burdina, Magdalena; Petrov, Petar
• Is Part Of: Biotechnology, biotechnological equipment. Volume 33:Issue 1(2019)
• Page Start: 64
• Page End: 74
• Publication Date: 2019-01-01
• Subjects: Caffeic acid phenethyl ester -- polymeric micelles -- antioxidant activity -- in vitro oxidative damage; Biotechnology -- Periodicals; Biotechnology -- Periodicals; Biotechnology -- instrumentation -- Periodicals; Periodicals; 660.605
• DOI: 10.1080/13102818.2018.1537753
• Languages: English
• ISSNs: 1310-2818

Abstract

Abstract: Caffeic acid phenethyl ester (CAPE), a hydrophobic constituent of poplar propolis of valuable biological activity, was immobilized in poly(ethylene oxide)-b-poly(ε-caprolactone)-b-poly(ethylene oxide) (PEO-b-PCL-b-PEO) copolymer micelles to improve its solubility in water. CAPE was loaded in the micelles by dialysis, achieving ca. 50% encapsulation efficiency. The drug loaded micelles were characterized with a mean diameter of 39 nm, narrow size distribution and slightly positive zeta-potential (approximately 2 mV). The in vitro release profile showed an improved dissolution behavior of micellar CAPE than pure CAPE. In vitro studies on human hepatoma HepG2 and neuronal SH-SY5Y cells demonstrated that the empty PEO-b-PCL-b-PEO micelles were not cytotoxic, whereas the drug loaded micelles exerted cytotoxic effects proportional to CAPE content. The protective activity of pure and micellar CAPE was investigated in a model of H2 O2 induced oxidative damage in HepG2 and SH-SY5Y cells. In both cell types, micellar CAPE exhibited better protective activity against the oxidative damage than pure CAPE at very low concentrations (0.1 µg/mL), which is far from the cytotoxic concentration of CAPE-loaded micelles (71 µg/mL). Consequently, the developed micellar formulation has an improved activity against oxidative damage in hepatic and neuronal cells as comparing to pure CAPE.