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EN
Conventional eye drops exhibit weak bioavailability due to the unique physiology and anatomy of the eye. In order to increase eye drops viscosity, different concentrations of Carbopol® 940 (0.08% and 0.20%) were used. The aim of the study was to indicate the advantages and examine the influence of preservatives and the concentrations of viscosity increasing agents on the quality of magistral viscous eye drops with dexpanthenol (DXP). The quality of the prepared formulations was tested using physico-chemical methods and biological tests. pH Value measurement was done by the potentiometric method). Viscosity measurements of the samples were performed according to Ph. Eur. 9.0. DXP content was determined by reversed-phase high-pressure liquid chromatography. Sterility testing was performed using direct sample inoculation. The results indicate that pH values of eye drops with preservatives are lower than pH values of preservative-free formulations. All formulations have recovery values that meet the requirements of the European Pharmacopoeia. The DXP content in preservative-free eye drops increased slightly during testing, unlike the DXP content in eye drops with preservatives. The formulations remained sterile during 45 days after preparation, stored at room temperature, protected from light. DXP viscous eye drops may be prepared in pharmaceutical practice using the proposed viscosity increasing agent (Carbopol® 940) and preparation procedure. All formulations express stability for 45 days after preparation. Preservative-free DXP eye drops with Carbopol® 940 concentrations of 0.08% and 0.20% show maximal stability, provide an optimal concentration of DXP (3.0%), and therefore have an advantage in pharmaceutical practice.
EN
Chalcones, as a large group of organic compounds, are widely implemented in various types of anti-cancer therapeutics. These plant metabolites are present in fruits, vegetables, spices, and have anti-tumor, anti-inflammation, immunomodulation, antibacterial and anti-oxidative activities, as well as many other pharmacological and biological effects. The aim of the present study was to investigate cytotoxic effects, type of cell death and mechanism of action of the newly synthesized vanillin based chalcone analogues, (CH1) and (CH2) on human colon cancer HCT-116 and noncancerous (control) MRC-5 cell lines. In order to compare effects of vanillin based chalcone analogues on investigated cell lines, as reference substances cisplatin (cisPt) and dehydrozingerone (DHZ) were used. Investigation of antitumor effect of chalcone analogues on HCT-116 cells was carried out by three methods MTT assay, flow cytometry and immunofluorescence analysis. The result of our investigation indicated that newly synthesized vanillin based chalcone analogues expressed powerful antitumor effect on cancer cells (HCT-116 cell line), while their effect on healthy cells (MRC-5 cell line) was not statistically significant. Vanillin based chalcone analogues caused overexpression and activation of mitochondrial Bax protein and caspase-3 in HCT-116 cells, indicating that their mechanism of antitumor action was mediated through activation of inner apoptotic pathway. These results indicate possible usefulness of CH1 and CH2 in antitumor therapy whether through its direct cytotoxic effect or as adjuvant therapy. Our results indicate possible usefulness of CH1 and CH2 vanillin based chalcone analogues in antitumor therapy.
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