SummaryThis paper describes the synthesis and application of alginate–chitosan–cyclodextrin micro- and nanoparticulate systems loaded with isoniazid (INH) and isoconazole nitrate (ISN) as antimycobacterial compounds. Preparation and morphology of the obtained particles, as well as antimycobacterial activity data of the obtained systems are presented. Docking of isoconazole into the active site of enoyl–acyl carrier protein reductase (InhA) of Mycobacetrium tuberculosis was carried out in order to predict the binding affinity and non-covalent interactions stabilizing the InhA–isoconazole complex. To assess these interactions, frontier molecular orbital calculations were performed for the active site of InhA and isoconazole obtained from docking. Isoconazole was predicted to be an active inhibitor of InhA with the analysis of the molecular docking and electron density distribution. It has been detected that alginate–chitosan–cyclodextrin microparticulate systems loaded with INH and ISN are as effective as pure INH applied in higher dosages.

Abstract. Natural polysaccharides alginate and chitosan have been used extensively, separately or in mixtures (systems), in manufacturing of pharmaceutical products (antimicrobial) and not only. Alginates usually serve as basis for antimicrobial systems, while chitosan, in certain proportions, enhances their physicochemical and antimicrobial properties. Focusing on the recent literature (mostly since 2000), this review outlines the main synthetic approaches for the preparation of systems based on both polymers as well as identify potential areas of their application as antimicrobial agents. Various techniques used for systems preparation like microparticles, fi lms, fi bers, nanoparticles, sponges, applications and usefulness of these systems as carriers of antimicrobial compounds will also be discussed.