Showing papers by "Katarina Kralova published in 2018"

Activity of ring-substituted 8-hydroxyquinoline-2-carboxanilides against intestinal sulfate-reducing bacteria Desulfovibrio piger

Abstract: Desulfovibrio genus is dominant among sulfate-reducing bacteria (SRB) in the large intestine of healthy people and animals. It is mostly isolated from patients with inflammatory bowel disease (IBD) and can be involved in the disease initiation. Primary in vitro screening of 8-hydroxyquinoline-2-carboxanilides was performed against Desulfovibrio piger Vib-7 representing SRB. The most effective compounds with MIC90/MBC values in the range of 17–23 µM/20–23 µM, respectively, were substituted in C’(3) by CF3, OCH3, CH3 and in C’(4) by CF3. Their activity was twofold higher than that of ciprofloxacin. These compounds did not express any significant cytotoxic effect on THP-1 cells up to the tested concentration of 30 µM. The antibacterial efficacy of the most active C’(3)-substituted compounds practically did not change with increasing compound lipophilicity, indicating that this position of substitution is favorable for significant antimicrobial effect, while the antibacterial activity of most of C’(2) and C’(4)-substituted derivatives decreased linearly with increasing compound lipophilicity. In addition, the dependence of activity on electronic Hammett’s σ parameter of the substituent R was quasi-parabolic for the most effective C’(3)-substituted compounds.

Application of Nanobioformulations for Controlled Release and Targeted Biodistribution of Drugs

Abstract: This chapter focuses on natural-based biocompatible and biodegradable materials that are used as matrices/carriers for controlled release or targeted biodistribution of nanoscale active pharmaceutical ingredients with low toxicity and favorable pharmacokinetics. Nanoformulations can be considered as a complex of various materials in nanoscale. The biodegradability of matrices/formulating stabilizers is connected not only with toxicity but also with formulation stability. Cyclodextrin (CD)-based nanosponges are innovative cross-linked CD polymers nanostructured within a three-dimensional (3D) network that are proposed as new nanoscale delivery systems. In relation to the rapid development of nanotechnology and applications of functionalized biodegradable biocompatible nanomaterials, controlled release and targeted delivery nanoformulations not only enhance bioavailability, decrease toxicity for non-target tissues and "pill burden," but also protect active ingredients against decomposition and deactivation. Nanoparticles in biomedical branches can be used as nanodiagnostics, as nanomaterials for tissue engineering, as drug carriers for specific delivery/targeted biodistribution or controlled release, and as agents/drugs for prevention/treatment of diseases.