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.

Základní údaje

Originální název

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

Autoři

PAVELKOVA, M. (203 Česká republika), K. KUBOVA (203 Česká republika), Jakub VYSLOUŽIL (203 Česká republika), M. KEJDUSOVA (203 Česká republika), D. VETCHY (203 Česká republika), V. CELER (203 Česká republika), D. MOLINKOVA (203 Česká republika), D. LOBOVA (203 Česká republika), A. PECHOVA (203 Česká republika), Jan VYSLOUŽIL (203 Česká republika, domácí) a P. KULICH (203 Česká republika)

Vydání

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

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 2.666

Kód RIV

RIV/00216224:14310/17:00099800

Organizační jednotka

Přírodovědecká fakulta

UT WoS

000404548700037

Klíčová slova anglicky

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

Štítky

Změněno: 29. 3. 2018 11:19, Ing. Nicole Zrilić

Anotace

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.