Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation
Language English Country United States Media print-electronic
Document type Journal Article
PubMed
27502404
DOI
10.1208/s12249-016-0601-4
PII: 10.1208/s12249-016-0601-4
Knihovny.cz E-resources
- Keywords
- alginate beads, copper’s biological effects, dissolution profile, external gelation, vaginal administration,
- MeSH
- Alginates chemistry pharmacology MeSH
- Anti-Bacterial Agents pharmacology MeSH
- Gels chemistry MeSH
- Cations MeSH
- Glucuronic Acid chemistry pharmacology MeSH
- Hexuronic Acids chemistry pharmacology MeSH
- Copper chemistry pharmacology MeSH
- Polymers chemistry MeSH
- Solubility MeSH
- Cattle MeSH
- Particle Size MeSH
- Animals MeSH
- Check Tag
- Cattle MeSH
- Female MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Alginates MeSH
- Anti-Bacterial Agents MeSH
- Gels MeSH
- Cations MeSH
- Glucuronic Acid MeSH
- Hexuronic Acids MeSH
- Copper MeSH
- Polymers MeSH
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.
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