Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles
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 mic...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2019-01-01
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| Series: | Biotechnology & Biotechnological Equipment |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/13102818.2018.1537753 |
| _version_ | 1818518760338751488 |
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| author | Krassimira Yoncheva Virginia Tzankova Yordan Yordanov Borislav Tzankov Georgy Grancharov Denitsa Aluani Vassya Bankova Milena Popova Boryana Trusheva Magdalena Kondeva-Burdina Petar Petrov |
| author_facet | Krassimira Yoncheva Virginia Tzankova Yordan Yordanov Borislav Tzankov Georgy Grancharov Denitsa Aluani Vassya Bankova Milena Popova Boryana Trusheva Magdalena Kondeva-Burdina Petar Petrov |
| author_sort | Krassimira Yoncheva |
| collection | DOAJ |
| description | 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 H2O2 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. |
| first_indexed | 2024-12-11T01:14:38Z |
| format | Article |
| id | doaj.art-764a47261e0647949c020fc4acd6f87b |
| institution | Directory Open Access Journal |
| issn | 1310-2818 1314-3530 |
| language | English |
| last_indexed | 2024-12-11T01:14:38Z |
| publishDate | 2019-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Biotechnology & Biotechnological Equipment |
| spelling | doaj.art-764a47261e0647949c020fc4acd6f87b2022-12-22T01:25:55ZengTaylor & Francis GroupBiotechnology & Biotechnological Equipment1310-28181314-35302019-01-01331647410.1080/13102818.2018.15377531537753Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micellesKrassimira Yoncheva0Virginia Tzankova1Yordan Yordanov2Borislav Tzankov3Georgy Grancharov4Denitsa Aluani5Vassya Bankova6Milena Popova7Boryana Trusheva8Magdalena Kondeva-Burdina9Petar Petrov10Medical University of SofiaMedical University of SofiaMedical University of SofiaMedical University of SofiaBulgarian Academy of SciencesMedical University of SofiaBulgarian Academy of SciencesBulgarian Academy of SciencesBulgarian Academy of SciencesMedical University of SofiaBulgarian Academy of SciencesCaffeic 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 H2O2 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.http://dx.doi.org/10.1080/13102818.2018.1537753caffeic acid phenethyl esterpolymeric micellesantioxidant activityin vitro oxidative damage |
| spellingShingle | Krassimira Yoncheva Virginia Tzankova Yordan Yordanov Borislav Tzankov Georgy Grancharov Denitsa Aluani Vassya Bankova Milena Popova Boryana Trusheva Magdalena Kondeva-Burdina Petar Petrov Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles Biotechnology & Biotechnological Equipment caffeic acid phenethyl ester polymeric micelles antioxidant activity in vitro oxidative damage |
| title | Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| title_full | Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| title_fullStr | Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| title_full_unstemmed | Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| title_short | Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| title_sort | evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles |
| topic | caffeic acid phenethyl ester polymeric micelles antioxidant activity in vitro oxidative damage |
| url | http://dx.doi.org/10.1080/13102818.2018.1537753 |
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