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@article{1406140,
author = {Pavelkova, M. and Kubova, K. and Vysloužil, Jakub and Kejdusova, M. and Vetchy, D. and Celer, V. and Molinkova, D. and Lobova, D. and Pechova, A. and Vysloužil, Jan and Kulich, P.},
article_location = {NEW YORK},
article_number = {4},
doi = {http://dx.doi.org/10.1208/s12249-016-0601-4},
keywords = {alginate beads; copper's biological effects; dissolution profile; external gelation; vaginal administration},
language = {eng},
issn = {1530-9932},
journal = {AAPS PHARMSCITECH},
title = {Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation},
volume = {18},
year = {2017}
}
TY - JOUR
ID - 1406140
AU - Pavelkova, M. - Kubova, K. - Vysloužil, Jakub - Kejdusova, M. - Vetchy, D. - Celer, V. - Molinkova, D. - Lobova, D. - Pechova, A. - Vysloužil, Jan - Kulich, P.
PY - 2017
TI - Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation
JF - AAPS PHARMSCITECH
VL - 18
IS - 4
SP - 1343-1354
EP - 1343-1354
PB - SPRINGER
SN - 15309932
KW - alginate beads
KW - copper's biological effects
KW - dissolution profile
KW - external gelation
KW - vaginal administration
N2 - 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 fromNaALGdispersions (3 or 4%) were crosslinked by Cu2+ ions (0.5 or 1.0 M CuCl2) using external ionotropic gelation. Prepared mucoadhesive beads with particle size over 1000 mu m 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-HSVactivity 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.
ER -
PAVELKOVA, M., K. KUBOVA, Jakub VYSLOUŽIL, M. KEJDUSOVA, D. VETCHY, V. CELER, D. MOLINKOVA, D. LOBOVA, A. PECHOVA, Jan VYSLOUŽIL and P. KULICH. Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation. \textit{AAPS PHARMSCITECH}. NEW YORK: SPRINGER, 2017, vol.~18, No~4, p.~1343-1354. ISSN~1530-9932. Available from: https://dx.doi.org/10.1208/s12249-016-0601-4.
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