title: Vincristine and ɛ-viniferine-loaded PLGA-b-PEG nanoparticles: pharmaceutical characteristics, cellular uptake and cytotoxicity.
abstract: The objective of this study was to prepare the ɛ-viniferine and vincristine-loaded PLGA-b-PEG nanoparticle and to investigate advantages of these formulations on the cytotoxicity of HepG2 cells. Prepared nanoparticle has shown a homogeneous distribution with 113 ± 0.43 nm particle size and 0.323 ± 0.01 polydispersity index. Zeta potential was determined as -35.03 ± 1.0 mV. The drug-loading percentages were 6.01 ± 0.23 and 2.01 ± 0.07 for ɛ-viniferine and vincristine, respectively. The cellular uptake efficiency of coumarin-6-loaded nanoparticles was increased up to 87.8% after 4 h. Nanoparticles loaded with high concentrations of both drugs showed a cytotoxic effect on HepG2 cells, having the percentage of cell viability of between 43.23% and 47.37%. Unfortunately, the percentage of apoptotic cells after treated with drugs-loaded nanaoparticles (10.93%) was similar to free forms of drugs (12.1%) that might be due to low ɛ-viniferine release in biological pH at 24 h.
authors.affiliation: a Department of Biochemistry, Faculty of Pharmacy , Anadolu University , Eskisehir , Turkey.
authors.forename: Yüksel
authors.initials: Y
authors.lastname: Öğünç
authors.affiliation: b Department of Pharmaceutical Technology, Faculty of Pharmacy , Anadolu University , Eskisehir , Turkey.
authors.forename: Müzeyyen
authors.initials: M
authors.lastname: Demirel
authors.affiliation: c Department of Chemical Engineering , Afyon Kocatepe University , Afyon , Turkey.
authors.forename: Arzu
authors.initials: A
authors.lastname: Yakar
authors.affiliation: a Department of Biochemistry, Faculty of Pharmacy , Anadolu University , Eskisehir , Turkey.
authors.forename: Zerrin
authors.initials: Z
authors.lastname: İncesu
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001572:Benzofurans / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008099:Liver / Q000187:drug effects / Q000473:pathology; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D053758:Nanoparticles / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011098:Polyglactin 910 / Q000737:chemistry*; D013267:Stilbenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D014750:Vincristine / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D001572:Benzofurans; D004337:Drug Carriers; D013267:Stilbenes; C102418:poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer; D011098:Polyglactin 910; D011092:Polyethylene Glycols; D014750:Vincristine; C091891:epsilon-viniferin
keywords: Nanoparticle; PLGA-b-PEG; passive targeting; vincristine; ɛ-viniferine