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. ORCID; K. KUBOVA ORCID; Jakub VYSLOUŽIL ORCID; M. KEJDUSOVA; D. VETCHY; V. CELER; D. MOLINKOVA; D. LOBOVA; A. PECHOVA; Jan VYSLOUŽIL a P. KULICH

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

Označené pro přenos do RIV

Ano

Kód RIV

RIV/00216224:14310/17:00099800

Organizační jednotka

Přírodovědecká fakulta

EID Scopus

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.