Polylactide-Meso-Substituted Arylporphyrin Composites: Structure, Properties and Antibacterial Activity.

The structural features and antibacterial properties of polymer-porphyrin composites were investigated. Meso-substituted arylporphyrin 0.2-0.5 wt.% was immobilized in a polylactide matrix. The immobilization of porphyrin causes a bathochromic shift and splitting of the Soret band. This study of the morphology of the obtained composites demonstrated a uniform distribution of the meso-substituted arylporphyrin in the polylactide matrix. It was determined by the X-ray diffraction analysis that porphyrin does not affect the α-form of polylactide crystalline formations. However, its addition into the polymer somewhat reduces the melting point (by 1-2 °C) and the degree of crystallinity of polylactide (by 3-4%). The elastic characteristics of the resulting systems were determined by the ultrasonic method, and a decrease in the density of the samples with an increase of the arylporphyrin content was shown. According to the results of the biological test, the dark toxicity of the obtained composites against the microorganisms Staphylococcus aureus, Salmonella Typhimurium and Escherichia coli was shown. Immobilizates containing 0.4 and 0.5 wt.% porphyrin showed the best antibacterial effect. The antibacterial activity of the studied composites makes it possible to attribute the polylactide-porphyrin systems to promising materials in the field of medicine and bioengineering.

A New Approach to the Synthesis of Nanocrystalline Cobalt Boride in the Course of the Thermal Decomposition of Cobalt Complexes [Co(DMF)6]2+ with Boron Cluster Anions.

In the course of the study, nanocrystalline cobalt monoboride was prepared by thermal decomposition of precursors [Co(DMF)6][An], where [An] = [B12H12]2- (1), [trans-B20H18]2- (2) or [B10Cl10]2- (3) in an argon atmosphere. Three new salt-like compounds 1-3 were prepared when Co(NO3)2 was allowed to react with (Et3NH)2[An]. Compound 1 is new; the structures of compounds 2 and 3 have been previously reported. Samples 1-3 were annealed at 900 °C in argon to form samples 1a-3a, which were characterized by single crystal XRD for 1 and powder XRD for 1-3. Powder XRD on the products showed the formation of BN and CoB for 1a in a 1:1 ratio; 2a gave a higher CoB:BN ratio but an overall decreased crystallinity. For 3a, only CoB was found. IR spectra of samples 1a-3a as well as X-ray spectral fluorescence analysis for 3a confirmed these results. The nanoparticular character of the decomposition products 1a-3a was shown using TEM; quite small particle sizes of about 10-15 nm and a quite normal size distribution were found for 1a and 2a, while the decomposition of 3 gave large particles with 200-350 nm and a broad distribution.

Non-Covalent Interactions in the Crystal Structures of Perbrominated Sulfonium Derivatives of the closo-Decaborate Anion.

A new series of compounds based on perbrominated disubstituted sulfonium derivatives of the closo-decaborate anion (n-Bu4N)[2-B10Br9SR2] (R = n-Pr, i-Pr, n-Bu, n-C8H17, n-C12H25, n-C18H37) was obtained, characterised by modern physicochemical methods of analysis. According to the results of an X-ray diffraction study, some of the anions and solvate molecules were disordered. The cations (n-Bu4N)+ and anions [2-B10Br9SR2]- were associated via C-H…Br and H…H contacts. In addition, Br…Br interactions between anions were revealed. The role of these contacts was analysed in terms of Hirshfeld surface analysis, QTAIM theory and the NCI method using quantum chemical calculations. An increase in the size of the alkyl R moiety led to significant strengthening of the total energy of H…H interactions. In the case of R = -n-C18H37, a parallel mutual orientation of alkyl moieties was established that was similar to the packing of salts of fatty acids. The nature of C-H…Br and Br…Br interionic interactions was found to be attractive, in contrast to the repulsive nature of intermolecular Br…Br interactions.

Development of novel darunavir amorphous solid dispersions with mesoporous carriers.

The aim of this work was to compare mesoporous carriers based on silica and magnesium aluminosilicate in the amorphous solid dispersion production. Darunavir has been selected as an active pharmaceutical ingredient that is classified as a Class 2 BCS substance and exists in two commercially available forms: crystalline ethanolate and amorphous. In the course of the study, the conditions for the preparation of amorphous samples with the selected carriers were evaluated within the framework of the most common methods for obtaining solid dispersions - hot-melt extrusion, solvent wetting, and spray drying. It was determined that the obtained dispersion properties almost completely repeat the properties of the corresponding carriers. The resulting dispersions were examined in a dissolution test and the best ones was used to formulate tablets, which were studied in an in vitro dissolution test with the original Prezista. The proposed tablet formulation showed improved dissolution compared to the original one. It was also found that silica supports have a greater positive contribution to darunavir dissolution - both ethanolate or amorphous forms.