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The nutraceutical system of curcumin-piperine in 2-hydroxypropyl-β-cyclodextrin was prepared by using the kneading technique. Interactions between the components of the system were defined by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), infrared spectroscopy (FT-IR), nuclear magnetic resonance (NMR). Application of hydroxypropyl-β-cyclodextrin as a carrier-solubiliser improved solubility of the curcumin–piperine system, its permeability through biological membranes (gastrointestinal tract, blood–brain barrier) as well as the antioxidant, antimicrobial and enzyme inhibitory activities against acetylcholinesterase and butyrylcholinesterase. [ABSTRACT FROM AUTHOR]

The influence of ionizing radiation on the physicochemical properties of panipenem in the solid-state was studied. In the first part of our studies, we evaluated the possibility of applying radiosterilization to obtain sterile panipenem. Spectroscopic (FT-IR, Raman), chromatography (HPLC and HPLC-MS) and X-ray powder diffraction (XRPD) studies have shown that irradiation of panipenem with the 25 kGy, the dose required to achieve sterility, does not change the physicochemical properties of the studied compound. The antimicrobial activity of panipenem irradiated with the dose of 25 kGy was reduced for three species. It was confirmed that the decrease in antimicrobial activity might be related to the isomerization of panipenem. [ABSTRACT FROM AUTHOR]

Progressive increase in bacterial resistance has caused an urgent need to introduce new antibiotics, one of them being oxazolidinones with their representative tedizolid. Despite the broad spectrum of activity of the parent tedizolid, it is characterized by low water solubility, which limits its use. The combination of the active molecule with a multifunctional excipient, which is cyclodextrins, allows preservation of its pharmacological activity and modification of its physicochemical properties. Therefore, the aim of the study was to change the dissolution rate and permeability through the model membrane of tedizolid by formation of solid dispersions with a cyclodextrin. The research included identification of tedizolid-hydroxypropyl-β-cyclodextrin (tedizolid/HP-β-CD) inclusion complex by thermal method (Differential Scanning Colorimetry), spectroscopic methods (powder X-ray diffraction, Fourier-Transform Infrared spectroscopy), and molecular docking. The second part of the research concerned the physicochemical properties (dissolution and permeability) and the biological properties of the system in terms of its microbiological activity. An increase in the dissolution rate was observed in the presence of cyclodextrin, while maintaining a high permeation coefficient and high microbiological activity. The proposed approach is an opportunity to develop drug delivery systems used in the treatment of resistant bacterial infections, in which, in addition to modifying the physicochemical properties caused by cyclodextrin, we observe a favorable change in the pharmacological potential of the bioactives. [ABSTRACT FROM AUTHOR]

For the first time, the influence of ionising radiation on the physicochemical properties of ertapenem in solid state was studied. During our studies, we evaluated the possibility of applying radiosterilization to obtain sterile ertapenem. Spectroscopic (Fourier Transform Infrared (FT-IR)), thermal (differential scanning calorimetry (DSC), chromatography (High-Performance Liquid Chromatography (HPLC) and HPLC-MS), and X-ray powder diffraction (XRPD) studies shown that irradiation of ertapenem with the 25 kGy, the dose required to achieve sterility, does not change the physicochemical properties of the studied compound. The antimicrobial activity of ertapenem irradiated with the dose of 25 kGy was only reduced for one species. Based on the received results, we can conclude that radiostelization is a promising alternative method of obtaining sterile ertapenem. In our studies, ertapenem was also exposed to e-beam radiation with a dose of 400 kGy. It was determined that two novel degradation products that are structurally differently to degradants formed during hydrolysis and thermolysis. [ABSTRACT FROM AUTHOR]

Biapenem is parenteral carbapenem antibiotic with a broad spectrum of activity. The objective of the study was to confirm that β -radiation irradiation with electron beam with a delivered dose of 25 kGy allows to obtain a sterile biapen, characterized by unchanged physicochemical and microbiological properties. Biological and chemical changes of biapenem were only observed when 400 kGy was used (the dose 16 times higher than dose needed to sterilization). The degradation product from radiolysis was identified by the LC-MS/MS method. Radiosterilization Radiation sterilization is safe and effective method of biapenem sterilization. • Radiosterilization is a safe and effective method for obtaining sterile biapenem. • The safety of radiosterilization was studied by FT-IR, Raman, XRPD techniques. • The effectiveness of biapenem radiosterilization was confirmed by microbiological tests. [ABSTRACT FROM AUTHOR]