Biological Effects of Drug-Free Alginate Beads Cross-Linked by
Copper Ions Prepared Using External Ionotropic Gelation

J 2017

Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation

PAVELKOVA, M., K. KUBOVA, Jakub VYSLOUŽIL, M. KEJDUSOVA, D. VETCHY et. al.

Basic information

Original name

Biological Effects of Drug-Free Alginate Beads Cross-Linked by Copper Ions Prepared Using External Ionotropic Gelation

Authors

PAVELKOVA, M. (203 Czech Republic), K. KUBOVA (203 Czech Republic), Jakub VYSLOUŽIL (203 Czech Republic), M. KEJDUSOVA (203 Czech Republic), D. VETCHY (203 Czech Republic), V. CELER (203 Czech Republic), D. MOLINKOVA (203 Czech Republic), D. LOBOVA (203 Czech Republic), A. PECHOVA (203 Czech Republic), Jan VYSLOUŽIL (203 Czech Republic, belonging to the institution) and P. KULICH (203 Czech Republic)

Edition

AAPS PHARMSCITECH, NEW YORK, SPRINGER, 2017, 1530-9932

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

Impact factor

Impact factor: 2.666

RIV identification code

RIV/00216224:14310/17:00099800

Organization unit

Faculty of Science

DOI

http://dx.doi.org/10.1208/s12249-016-0601-4

UT WoS

000404548700037

Keywords in English

alginate beads; copper's biological effects; dissolution profile; external gelation; vaginal administration

Abstract

V originále

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.

Citovat

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. 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.

@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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