Жарияланымдар / Публикации

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Автор: search.filters.author.Daniil ShepilovТема: search.filters.subject.bactericidal activity

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    DEVELOPMENT, PHARMACEUTICAL EVALUATION, AND ASSESSMENT OF THE BACTERICIDAL ACTIVITY OF THE KC-250 TABLET FORMULATION AGAINST CLINICALLY SIGNIFICANT MICROORGANISMS
    (2026-08-21)
    Daniil Shepilov
    ;
    Zhassur Taganov
    ;
    Ardak B. Jumagaziyeva
    ;
    Sabina T. Kenesheva
    ;
    Saltanat Jumabayeva
    Introduction: Conversion of iodine-containing complexes into solid dosage forms requires adequate tablet strength while preserving disintegration, release, and antimicrobial activity. This study aimed to develop a directly compressed KC-250 tablet formulation, evaluate its pharmaceutical quality, and determine its bactericidal activity against clinically significant bacteria. Methods: Tablets containing 60 mg of KC-250 at a target mass of 500 mg were prepared using MicroceLac® 100, povidone K30, and magnesium stearate. Compression forces of 3.24 and 6.96 kN were compared by friability and disintegration testing. The selected formulation was evaluated for pharmacopoeial quality attributes. Bactericidal activity against eight reference, resistant, and clinical bacterial strains was determined in triplicate by broth serial dilution followed by agar subculture. Results: Increasing compression force from 3.24 to 6.96 kN reduced friability from 0.81% to 0.21%, while disintegration increased from 1.62 to 4.62 min. Tablets produced at 6.96 kN had friability of 0.20%, a disintegration time of 4 min 54 s, a KC-250 content of 63.05 mg/tablet, and dissolution of 102.95% within 45 min. All evaluated attributes complied with the predefined acceptance criteria. Minimum bactericidal concentrations were 60 mg/mL for the tested Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa strains and 30 mg/mL for Enterococcus faecalis and Enterococcus faecium. Discussion: Compression at 6.96 kN provided the most appropriate balance between mechanical resistance and rapid disintegration without restricting KC-250 release. The retained bactericidal activity indicates that tablet formulation did not eliminate the antimicrobial function of KC-250 and supports further development of the selected MicroceLac® 100– povidone K30 matrix.
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    D/PVA/I-1 as an Antibiotic Adjuvant: In Vitro Synergy and Membrane Permeabilization in MDR Bacteria
    (Multidisciplinary Digital Publishing Institute, 2026-08-17)
    Ardak B. Jumagaziyeva
    ;
    Seitzhan Turganbay
    ;
    Anar Seisembekova
    ;
    Daniil Shepilov
    ;
    Zhanar A. Iskakbayeva
    Background: Antimicrobial resistance (AMR) is among the most pressing challenges in modern infectious medicine, driving progressive failure of standard antibacterial therapy and rising mortality from infections caused by multidrug-resistant (MDR) pathogens. Antibiotic potentiation through adjuvant compounds capable of restoring the activity of existing drugs represents a promising strategy to overcome resistance without developing fundamentally new antibacterial molecules. This study aimed to evaluate the antibiotic-potentiating activity of a dextrin/polyvinyl alcohol/iodine complex (D/PVA/I-1), developed at the Scientific Center for Anti-Infectious Drugs JSC (Almaty, Kazakhstan), against clinically relevant MDR reference strains. Methods: Nine reference strains, Staphylococcus aureus (ATCC 33591, BAA-39), Escherichia coli (ATCC BAA-196, BAA-2523), Klebsiella pneumoniae (ATCC BAA-2524, 700603), Acinetobacter baumannii (ATCC BAA-1790), Streptococcus pneumoniae (ATCC BAA-660), and Haemophilus influenzae (ATCC 33930), and two clinical isolates, P. aeruginosa SCAID PHRX1-2019 and E. coli SCAID WND1-2021, were tested. Antibiotic-potentiating activity was assessed by checkerboard assay with calculation of the fractional inhibitory concentration index (FICI); bactericidal kinetics were evaluated by time-kill analysis. The effect of D/PVA/I-1 on cytoplasmic membrane permeability was investigated using a crystal violet uptake assay. Results: Of 45 D/PVA/I-1–antibiotic combinations tested across nine antibiotics, synergy (FICI ≤ 0.5) was demonstrated in 44.4% of cases, partial synergy in 48.9%, and additive effects in 6.7%; no antagonistic interactions were detected. The most pronounced potentiating effect occurred against Gram-positive pathogens, particularly MRSA strains (66.7% synergistic combinations). Time-kill analysis confirmed suppression of the regrowth phenotype characteristic of MDR strains under monotherapy and restoration of bactericidal activity against antibiotics to which strains exhibited intrinsic resistance. D/PVA/I-1 induced a dose- and time-dependent increase in membrane permeability in both Gram-positive and Gram-negative organisms. Conclusions: D/PVA/I-1 is an effective broad-spectrum antibiotic potentiator and represents a promising basis for combination therapy regimens against MDR infections.