title: Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation.
abstract: External ionotropic gelation offers a unique possibility to entrap multivalent ions in a polymer structure. The aim of this experimental study was to prepare new drug-free sodium alginate (ALG) particles cross-linked by Cu2+ions and to investigate their technological parameters (particle size, sphericity, surface topology, swelling capacity, copper content, release of Cu2+ions, mucoadhesivity) and biological activity (cytotoxicity and efficiency against the most common vaginal pathogens-Herpes simplex, Escherichia coli, Candida albicans) with respect to potential vaginal administration. Beads prepared from NaALG dispersions (3 or 4%) were cross-linked by Cu2+ions (0.5 or 1.0 M CuCl2) using external ionotropic gelation. Prepared mucoadhesive beads with particle size over 1000 μm exhibited sufficient sphericity (all ˃0.89) and copper content (214.8-249.07 g/kg), which increased with concentration of polymer and hardening solution. Dissolution behaviour was characterized by extended burst effect, followed by 2 h of copper release. The efficiency of all samples against the most common vaginal pathogens was observed at cytotoxic Cu2+concentrations. Anti-HSV activity was demonstrated at a Cu2+concentration of 546 mg/L. Antibacterial activity of beads (expressed as minimum inhibition concentration, MIC) was influenced mainly by the rate of Cu2+release which was controlled by the extent of swelling capacity. Lower MIC values were found for E. coli in comparison with C. albicans. Sample ALG-3_1.0 exhibited the fastest copper release and was proved to be the most effective against both bacteria. This could be a result of its lower polymer concentration in combination with smaller particle size and thus larger surface area.
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 612 42, Brno, Czech Republic.
authors: M
authors: M
authors: Pavelková
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 612 42, Brno, Czech Republic. dvorackovak@vfu.cz.
authors: K
authors: K
authors: Kubová
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 612 42, Brno, Czech Republic.
authors: J
authors: J
authors: Vysloužil
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 612 42, Brno, Czech Republic.
authors: M
authors: M
authors: Kejdušová
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackého tř. 1, 612 42, Brno, Czech Republic.
authors: D
authors: D
authors: Vetchý
authors: Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1-3, 612 42, Brno, Czech Republic.
authors: V
authors: V
authors: Celer
authors: Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1-3, 612 42, Brno, Czech Republic.
authors: D
authors: D
authors: Molinková
authors: Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1-3, 612 42, Brno, Czech Republic.
authors: D
authors: D
authors: Lobová
authors: Department of Biochemistry and Biophysics, Faculty of Veterinary Hygiene and Ecology, University of Veterinary and Pharmaceutical Sciences Brno, Palackého 1-3, 612 42, Brno, Czech Republic.
authors: A
authors: A
authors: Pechová
authors: Department of Biochemistry, Faculty of Science, Masaryk University, Kotlářská 267/2, 611 37, Brno, Czech Republic.
authors: J
authors: J
authors: Vysloužil
authors: Department of Chemistry and Toxicology, Veterinary Research Institute, Hudcova 296/70, 621 00, Brno, Czech Republic.
authors: P
authors: P
authors: Kulich
mesh_terms: D000464:Alginates / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D002412:Cations; D002417:Cattle; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D005782:Gels / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry / Q000494:pharmacology; D006603:Hexuronic Acids / Q000737:chemistry / Q000494:pharmacology; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D012995:Solubility
chemical_list: D000464:Alginates; D000900:Anti-Bacterial Agents; D002412:Cations; D005782:Gels; D006603:Hexuronic Acids; D011108:Polymers; D003300:Copper; D020723:Glucuronic Acid
keywords: alginate beads; copper’s biological effects; dissolution profile; external gelation; vaginal administration