The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated. The model with optimal characteristics was included in a bigel formulation. The bigel was characterized in terms of pH, rheological behavior, spreadability, and in vitro drug release. Acute skin toxicity, antinociceptive activity, anti-inflammatory activity, and antihyperalgesic effects of the prepared bigel with ketoprofen-loaded polymer carrier were evaluated. The carriers of ketoprofen were characterized by a high yield and drug loading. The particle size distribution varied widely according to the polymer used, and a sustained release was provided for up to 6 hours. The polymer mixture poly(vinyl acetate) and hydroxypropyl cellulose as a drug carrier, alone or included in the bigel composition, improved the photostability of the drug compared with unprotected ketoprofen. The bigel with ketoprofen-loaded particles provided sustained release of the drug and had optimal rheological parameters. In vivo experiments on the bigel showed no skin inflammation or irritation. Four hours after its application, a well-defined analgesic, anti-inflammatory, and antihyperalgesic effect was registered. The polymer mixture of poly(vinyl acetate) and hydroxypropyl cellulose as a carrier of ketoprofen and the bigel in which it was included provided an enhanced photostability and sustained drug release.
Until now, the interest to plants from genus Scutellaria in Bulgaria has been focused mainly on the terpenes in them. The purpose of this study is to enrich the information on the composition of the Bulgarian Scutellaria species in terms of both polyphenolic content as well as primary metabolites such as mono-, oligosaccharides and organic acids. An aerial part of three Scutellaria species growing in four low mountain regions of Southern Bulgaria was used. The flavonoids scutellarin, baicalin, baicalein, wogonin, wogonoside, luteolin, chrysin and a caffeoyl phenylethanoid glycoside-verbascoside have been identified via HPLC in different extracts from Scutellaria altissima, Scutellaria albida and Scutellaria galericulata. The antioxidant activity of the extracts has been evaluated. The Scutellaria altissima from Mezek and Scutellaria galericulata from Parvenets we studied, which are the richest in flavonoids (represented mainly by baicalin, scutellarin and wogonoside), show the highest Oxygen Radical Absorption Capacity. Hydroxyl Radical Averting Capacity of Scutellaria albida from Mezek and Scutellaria altissima from Bachkovo is the most pronounced, probably due to the content of scutellarin and luteolin and chrysin, respectively. Antioxidant activity of aqueous, methanolic and 70% and 96% ethanol extracts were also determined by the electrochemical method.
The aim of the study was to investigate the influence of the nature and composition of the monomer feed, added to the reaction system indomethacin/vinyl acetate/3-dimethyl (methacryloyloxyethyl) aminopropyl sulfonate (IMC/VAc/DMAPS) and the characteristics of the obtained polymer latexes on indomethacin In-situ loading, its kinetic release properties, and drug stability. Indomethacin loaded nanoparticles were obtained by an emulsifier-free emulsion radical copolymerization of the monomers, in presence of the drug. Transmission electron microscopy, Attenuated Total Reflection Fourier Transform Infrared spectroscopic analyses, Particle size distribution and zeta potential analysis were carried out to characterize the In-situ loaded nanocarriers. High-performance liquid chromatography and UV/VIS spectroscopic analyses were applied to determine the drug loading, In vitro release properties and stability studies of the drug used. High yield of 90 to 96% was obtained for the tested In-situ loaded nanocarriers. They possess a spherical shape with diameter ranging from 100 to 900 nm and zeta potential from -3.25 mV to -20.3 mV. Mono-modal and bi-modal particle size distribution was observed depending on monomer feed, added to the reaction system. It also influenced the drug loading and its release characteristics. Indomethacin was released from the investigated patterns following first order release. The nature and composition of the monomer feed, added to the reaction system IMC/VAc/DMAPS are an effective factors for the control of the indomethacin loading and also affect the rate and extent of drug-releasing but do not influence the kinetic model and drug transport mechanism. Stability studies indicated the stabilizing role of the polymer carrier on the In-situ included indomethacin.
Antistress II possesses antidepressant effect and improves the recognition memory while Antistress I doesn't demonstrate any of the above-described effects.
Assessing the iodine status, we found a negative correlation between the levels of iodine and thiocyanates in urine (R=-0.717, р<0.0001), a positive correlation between nitrates and TSH (R=0.487, р=0.003) and a negative correlation between nitrates and FT4 (R=-0.312, р=0.06). For the iron status, we found a negative correlation between nitrates and SF (R=-0.429, р=0.009) and between nitrates and Hb (R=-0.383, р=0.021). The Mann-Whitney U-test showed that in women with nitrate levels higher than the mean value there was low FT4 level (р=0.06), high TSH level (р=0.013), low Hb concentration (р=0.061) and low SF concentration (р=0.005). The combined effects of environmental factors (elevated nitrate levels and low selenium level) on the iodine and iron status are manifested by low concentrations of FT4 (р=0.033), Hb (р=0.06) and SF (р=0.05) and high level of TSH (р=0.05). In conclusion, we found that environmental factors, especially when combined, have a negative impact on the iron and iodine status of females.
The current study investigates the content of sugars, organic acids, phenolic acids and flavonoids, as well as antioxidant and antimicrobial activity of Balkan-endemic Micromeria frivaldszkyana. Glucose was the most abundant sugar in the plant (2.77%), followed by fructose (1.18%) and galactose (0.82%). Eight organic acids were detected with quinic acid being in the highest content—556.3 mg/100 g DW. From the individual phenolic acids, rosmarinic acid was found in the most significant amounts (2040.1 ± 1.97 mg/100 g) and hesperidin was the major representative of flavonoids with content 131.2 ± 5.6 mg/100 g DW. The antioxidant activity of the plant was studied by six methods: 2,2′-diphenylpicrylhydrazyl (DPPH)—286.4 ± 10.43 mM TE/g, 2,2′azinobis (3)-ethylbenzthiazoline-6-sulfonic acid (ABTS)—358.4 ± 10.4 mM TE/g, ferric reducing antioxidant power (FRAP)—388.0 ± 32.4 mM TE/g, cupric reducing antioxidant capacity (CUPRAC)—905.6 ± 19.2 mM TE/g, Oxygen Radical Absorbance Capacity (ORAC)—3250.5 ± 208.1 µmol TE/g and Hydroxyl Radical Averting Capacity (HORAC)—306.1 ± 23.5 µmol GAE/g. In vitro antimicrobial activity against nine microorganism was evaluated but the extract displayed antimicrobial activity only against Listeria monocytogenes ATCC 19111 with inhibition zone diameter 9 mm and minimal inhibitory concentration (MIC) 10 mg/mL.
Anxiety is a significant social problem that could deteriorate the quality of life of individuals. It disturbs the normal circadian rhythms, leading to an increase of cardio-vascular diseases and distortions in the functions of the immune system. Antistress I and Antistress II are herbal combinations containing in different proportions dry extracts obtained from Serratula coronata, Hypericum perforatum, Valeriana officinalis, Crataegus monogyna and Melissa officinalis. The present study evaluates the acute toxicity and the anxiolytic effect of these combinations and the individual extracts which they contain after their oral administration to male Wistar rats. Doses of 5g/kg b.w. and 10g/kg b.w. are used for the evaluation of acute toxicity. Assessment of the anxiolytic effect is carried out at three doses – 100, 250 and 500 mg/kg b.w. by using the test - Elevated plus maze. The results about the acute toxicity show a survival rate of 100% for all extracts at a dose up to10g/kg b.w. The evaluation of the anxiolytic effect on an acute stress model in rats demonstrates that both combinations Antistress I and Antistress II possess anxiolytic properties which are significant only at the highest dose. The results also give us the reason to conclude that the effect of Antistress II on anxiety is better compared to Antistress I.
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