The Study of the Cytotoxicity, Proliferative and Microbiological Activity of the Medicated Chewing Gum with Ascorbic Acid and Lysozyme Hydrochloride Using Different Culture of Cells.

Medicated chewing gum with lysozyme hydrochloride and ascorbic acid as active pharmaceutical ingredients was developed for application in dentistry. The aim of this research was to study the cytotoxicity, proliferative, and microbiological activities of the active ingredients in different types of cell cultures. The preclinical study of active pharmaceutical ingredients and their combinations was carried out using culture lines such as HepG2 (human hepatocarcinoma cells), Hek293 (human embryonic kidney cells), and MAEC (mouse aortic endothelial cells). MTT assays were used to analyse cytotoxicity and proliferative activity, while the state of antioxidant protection was assessed by the content of sulfhydryl groups and catalase activity. The determination of lipid peroxidation products was based on the level of TBA-active products. As a microbiological model for studying the effect of the developed dental medicine on the ability of the oral cavity microorganisms to form biofilms, the following strains were used: Streptococcus mutans, Staphylococcus aureus, Staphylococcus epidermidis, Lactobacillus plantarum, and Candida albicans. The optical density of the formed biofilm was evaluated by the intensity of the experimental sample's colour on a StatFax 303 Plus photometer at a wavelength of 630 nm. The combination of ascorbic acid and lysozyme hydrochloride in the established concentrations (20 mg and 10 mg per 1 gum, respectively) resulted in a slight stimulation of cell proliferation without any toxic effects and increased antioxidant protection, preventing the development of oxidative stress. It was found that, in contrast to the separately used active substances, the combination of lysozyme hydrochloride and ascorbic acid inhibits the biofilm formation of all studied microorganisms and shows the ability to destroy diurnal biofilms of L. plantarum and fungi of the genus Candida, indicating potentiation and summation of the active pharmaceutical ingredients' composition effects in the developed dental medicine. Due to the observed positive pharmacological and microbiological action, the combination of lysozyme hydrochloride and ascorbic acid in the medicated chewing gum serves as a promising tool for the prevention and treatment of infectious and inflammatory diseases of the periodontium and mucous membranes and the prevention of caries.

Assessing compatibility of excipients selected for a sustained release formulation of bilberry leaf extract

Abstract The study is aimed to assess the compatibility of bilberry leaf powder extract (BLPE) with six excipients selected for sustained-release (SR) tablet formulation. The BLPE was obtained with the addition of L-arginine and Myo-inositol as the carriers. Thermogravimetric (TG-DTG) analysis and Fourier-transform infrared spectroscopy (FTIR), supported by Pearson correlation analysis, were applied to detect possible interactions in the binary mixtures (1:1) of the BLPE with each excipient. The TG-DTG showed some deviations in the thermal behavior of the BLPE / excipient mixtures. However, only the thermal behavior of magnesium stearate in the mixture significantly differed from individual samples, which suggested chemical interaction for this excipient. The FTIR analysis confirmed that the BLPE is compatible with Eudragit L100, Methocel K4M, Methocel K100LV, Avicel PH-101, and Plasdone S-630. Whereas it undergoes solid-state chemical interaction in the binary mixture with magnesium stearate. According to the FTIR-spectra, it is suggested that this interaction results in the formation of stearic acid and alkalization of the medium. These findings evidence for the possibility of using TG-DTG analysis as an independent thermal technique for compatibility studies and also confirm the earlier reported interaction of basic lubricants, e.g., stearic salts, with active ingredients containing amino groups.

Impact of Compression Force on Mechanical, Textural, Release and Chewing Perception Properties of Compressible Medicated Chewing Gums.

Medicated chewing gums (MCGs) represent a beneficial platform for realizing drugs intended for dental prophylaxis and treatment. The present study aimed to investigate the impact of compression force on the mechanical, textural, release, and chewing perception characteristics of compressible MCGs with the combination of lysozyme hydrochloride (LH) and ascorbic acid (AsA). Four batches of MCGs were obtained on a laboratory single-punch tablet machine applying different forces, i.e., 5, 7, 10, and 15 kN, and evaluated by their geometrical parameters, mechanical resistance, surface and internal structure characteristics, texture profile, release behavior, and perception attributes during mastication. It was found that increasing compression force slightly affected resistance to crushing and friability of MCGs, but resulted in surface smoothing and formation of a thicker layer with highly compacted particle arrangement. According to the texture analysis, increasing compression force led to harder and more adhesive gums, indicating possible difficulties in chewing and, therefore, impairment of their consumer properties. Lower compression forces were also found to be preferable in terms of better drug release from the obtained chewing gums. The volunteers' assessment showed that an increase of compression force led to significantly raising the initial hardness and crumbliness as well as to decreasing the rate of the integral gum mass formation during mastication, which may negatively affect perceptive sensations when using MCGs. Based on the results obtained, the optimal compressing force was selected to be 7 kN, which allows obtaining MCGs with good organoleptic, mechanical, textural, and release properties.

The Influence of pH Values on the Rheological, Textural and Release Properties of Carbomer Polacril® 40P-Based Dental Gel Formulation with Plant-Derived and Synthetic Active Components.

The physicochemical properties, especially pH value of dental medicines, have significant influence on the health of oral cavity tissues. The pH of formulations should correspond to the value of saliva pH (5.5-8.0). For carbomer-based gels, the required pH value is obtained by neutralizing them with alkaline components, which leads to their structuring (thickening). This affects the physical properties of the gel, its residence time at the application site and the rate of release of active pharmaceutical ingredient. Therefore, the main purpose of this study is to evaluate the rheological, textural, and biopharmaceutical properties of Carbomer Polacril® 40P-based dental gel depending on the pH value. Evaluation of the rheological properties of gel preparations were performed by measuring the structural viscosity of the samples as a function of pH and temperature. The textural properties of the gel were evaluated by performing tests regarding back extrusion and spreadability. Carbomer Polacril® 40P-based gels haven't shown noticeable thixotropic behavior, and were characterized by plastic flow in the whole studied pH range. The structural viscosity at the selected average pH value hasn't differed at storage (25 °C) and application (37 °C) temperature. Texture studies of dental gels have shown a strong correlation with rheoparameters. Their rheological behavior and textural properties haven't changed significantly between the pH range of 5.5-6.6. The relatively narrow range of working pH values does not affect the change in the viscosity of the preparation significantly and, consequently, does not affect the release of APIs from the developed Carbomer Polacril® 40P-based dental gel.

Evaluation of anti-obesity and lipid-lowering properties of Vaccinium myrtillus leaves powder extract in a hamster model.

Background Vaccinium myrtillus leaves are known to be rich in phenols and have been used in traditional medicine as an antidiabetic remedy. This study evaluated the powder extract of V. myrtillus leaves obtained with the use of L-arginine and myo-inositol for anti-obesity and lipid-lowering potential in hamsters. Methods Standard phytochemical methods were used to determine the total phenolic and total flavonoid contents of the extract. The obesity condition was induced in Syrian hamsters by feeding them with highly palatable fat- and sugar-rich diet (40.3 kcal% fat) for 12 weeks. From the 10th week of diet feeding, the obese hamsters were treated with the powder extract of V. myrtillus leaves (15, 25 and 35 mg/kg/day, respectively) and "Styfimol" (6.2 mg/kg/day of hydroxycitric acid) as a positive control drug. At the end of the treatment period, the biochemical parameters as well as visceral fat mass were determined. Results Vaccinium myrtillus leaves powder extract at 25 and 35 mg/kg/day caused a significant reduction in body weight gain and visceral fat mass in obese hamsters. Serum triacylglycerols, free fatty acids, total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels were also significantly lower. Besides, the hamsters treated with powder extract at 25 and 35 mg/kg/day had the closest intact value ratio of high-density lipoprotein cholesterol and LDL-C compared with positive control animals. Conclusions The results showed that V. myrtillus leaves powder extract is a promising therapeutic agent for the treatment of obesity and obesity-induced diseases.

Comparative Characteristics of Anti-depressant, Anti-hypoxic Action, and Effect on the Physical Endurance of Scutellaria baicalensis Drugs.

OBJECTIVES: The influence of original drugs from Scutellaria baicalensis (SB) Georgi (dry extract, powder of rhizomes and roots, tablets "Scutex" on the basis of the dry extract and capsules "Scutella", which contain powder of rhizomes with roots) was studied on depressive behavior, physical endurance and anti-hypoxic activity in mice. MATERIALS AND METHODS: The used dry extract SB (SBDE), powder of roots and rhizomes from SB (SBRP), tablets from dry extract of SB named "Scutex", and hard gelatin capsules from the crushed root of SB named "Scutella" were obtained from National University of Pharmacy, Department of Industrial Technology of Drugs. In the experiment, 94 random-breed white male mice weighing 20-29 g were used and kept in standard sanitary and laboratory conditions. RESULTS: The experiments revealed that SBDE had anti-depressant action. Powder from rhizomes and roots of SB and "Scutella" capsules had anti-hypoxic action. All test drugs showed no influence on the physical endurance of mice. These results suggest the possible use of SBDE as an anti-depressant drug, and rhizomes with roots and "Scutella" capsules as an anti-hypoxic remedy. CONCLUSION: SBDE at a dose 50 mg/kg shows anti-depressant activity that exceeds the activity of the comparison drug "Bilobil". SBDE, SBRP, "Scutex" tablets and "Scutella" capsules do not affect the physical endurance of mice. SBDE at a dose 50 mg/kg and SBRP at a dose of 173 mg/kg and 260 mg/kg exhibit anti-hypoxic activity. "Scutex" tablets show no anti-hypoxic action and "Scutella" capsules cause probable anti-hypoxic action that exceeds the effect of the reference drug "Bilobil".