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Malnutrition, food security and food safety will remain major global issues as the world’s population grows and the consequences of climate change prevail, so we need to rethink how we grow and source food to create sustainable systems for future generations. Edible cities, as innovative solutions to use public spaces for urban food production, can bridge this evident gap between the present and the future. The aim of this review was to analyze the opportunities and constraints for creating edible cities and accessing wholesome functional foods in a sustainable way and explore existing solutions that can be strengthened. We can grow food in urban environments using ideas such as controlled-environment farms (CEAs), home food gardens on balconies, roofs and terraces, underground farming and foraging. As citizens become more aware of complex foods with nutritional benefits, we should take this opportunity to teach them about edible wholesome functional foods and how they can be grown instead of using plants. There are still many constraints such as pollution, a lack of government support and the economic aspects of urban farms that need to be resolved in order for edible cities and access to functional foods in them to become the standard worldwide. The goal is worthwhile as citizens would benefit from climate control, reduced resource consumption, a safer food supply, improved mental and physical health, reduced malnutrition and nutritional deficiencies and connected communities that share knowledge and resources to further innovation and welfare.

The purpose of this study was to investigate the influence of the addition of inulin (3%, 6% and 9%) to green tea-infused set type yoghurt on its sensory quality and physical properties. Yogurts were made by combining green tea with milk and inulin and inoculated with freeze-dried starter cultures YO-122. Incubation was conducted at 43 °C for approximately 4.5 h until a pH value of 4.5–4.6 was achieved. For the prepared yoghurts, a panel of experts (n = 10) was selected, characterized 35 attributes and conducted a sensory quality assessment of these yoghurts using the Quantitative Descriptive Profile method. Additionally, instrumental analyses such as yield stress, adhesiveness, firmness, physical stability and color parameters were also carried out. The use of green tea infusion increased the perception of green tea flavor, bitterness, astringency, dark color of the yoghurt and the existing whey, which worsened the overall sensory quality of the yoghurt. The addition of inulin (9%) to the green tea yoghurt, increased the perception of sweet, peach flavor and aroma and improved the firmness of the yoghurt while reducing the perception of sour taste, which improved the sensory quality of the yoghurt. Both inulin and green tea affected the physical properties of the yoghurts, causing an increase in the yield stress (43%, and 20%, respectively) and deteriorated the stability of the yoghurts. Green tea affected the color of the yoghurts, causing the lightness to decrease. The L* parameter decreased from 89.80 for the control sample to 84.42 for the green tea infused yoghurt. The use of infused green tea in yoghurt production makes it necessary to use ingredients that will neutralize its adverse effects on sensory quality and physical parameters of yoghurt, and such an additive can be prebiotic fiber–inulin at a concentration of 9%.

Background Though there are several classes of antidepressant drugs available on the pharmaceutical market, depression that affects globally over 320 million people is still undertreated. Scientists have made attempts to develop novel therapeutical strategies to maximize effectiveness of therapy and minimize undesired reactions. One of the ideas is use of either dual-action agents or combined administration of two substances that affect diverse neurotransmissions. Thus, we investigated whether the selected CB receptor ligands (oleamide, AM251, JWH133, and AM630) can have an impact on the activity of bupropion and moclobemide. Bupropion belongs to the dual acting drugs, whereas moclobemide is an inhibitor of monoamine oxidase. Methods The mice forced swim test and the tail suspension test were applied in order to determine the potential antidepressant-like activity, whereas the HPLC method was used in order to assess the brain concentrations of the tested antidepressants. Results An intraperitoneal injection of sub-effective doses of oleamide (5 mg/kg), AM251 (0.25 mg/kg), and AM630 (0.25 mg/kg) increased activity of bupropion (10 mg/kg) in both behavioural tests. Effects of moclobemide (1.5 mg/kg) were potentiated only by AM251. These results were not influenced by the hypo- or hyperlocomotion of animals. Conclusion The outcomes of the present study revealed that particularly activation or inhibition of the CB1 receptor function may augment the antidepressant activity of bupropion, whereas only inhibition of the CB1 receptor function manages to increase activity of moclobemide. Most probably, an interplay between CB receptor ligands and bupropion or moclobemide takes place at the cellular level.

Depression is a serious mental disease that, according to statistics, affects 320 million people worldwide. Additionally, a current situation related to the COVID-19 pandemic has led to a significant deterioration of mental health in people around the world. So far, rodents have been treated as basic animal models used in studies on this disease, but in recent years, Danio rerio has emerged as a new organism that might serve well in preclinical experiments. Zebrafish have a lot of advantages, such as a quick reproductive cycle, transparent body during the early developmental stages, high genetic and physiological homology to humans, and low costs of maintenance. Here, we discuss the potential of the zebrafish model to be used in behavioral studies focused on testing agents with antidepressant potential.

Set type yoghurts are characterised by a semi-solid texture, which is created during the fermentation process. The tea infusion in this type of yoghurt production can influence the quality of the final product. Therefore, the aim of the experiment was to evaluate the influence of the addition of 3, 6 and 9% inulin to oolong tea-infused yoghurts on the sensory quality. It has been evaluated by trained experts using a Quantitative Descriptive Profile analysis and by consumers using hedonic scaling, as well as on instrumentally evaluated features such as texture, stability and visual parameters. The addition of oolong tea to yoghurt resulted in positive changes in the perception of sweet, peach and nectar odours and flavours, and also creaminess, as well as negative changes in the presence of a bitter taste, the whey presence and a colour intensification towards dark cream (p ≤ 0.05). The addition of inulin to the tested oolong tea yogurts caused a decrease in the whey presence and brightened the yoghurt’s colour (6% and 9%, p ≤ 0.05, respectively), as well as an improved creaminess and an increase in the sweet taste of the yoghurt. It was also observed that the addition of oolong tea deteriorated the instrumentally evaluated texture of the set yoghurts, while inulin at a higher concentration (9%, p ≤ 0.05) increased the firmness and adhesiveness. Moreover, the addition of inulin also had a positive effect on the yoghurt’s stability. The addition of inulin to oolong tea-infused set yoghurts may be valuable both as a source of prebiotic fibre in functional products and as a factor improving the quality of these products.

The purpose of the study was to investigate whether the co-administration of Mg2+ and Zn2+ with selective A1 and A2A receptor antagonists might be an interesting antidepressant strategy. Forced swim, tail suspension, and spontaneous locomotor motility tests in mice were performed. Further, biochemical and molecular studies were conducted. The obtained results indicate the interaction of DPCPX and istradefylline with Mg2+ and Zn2+ manifested in an antidepressant-like effect. The reduction of the BDNF serum level after co-administration of DPCPX and istradefylline with Mg2+ and Zn2+ was noted. Additionally, Mg2+ or Zn2+, both alone and in combination with DPCPX or istradefylline, causes changes in Adora1 expression, DPCPX or istradefylline co-administered with Zn2+ increases Slc6a15 expression as compared to a single-drug treatment, co-administration of tested agents does not have a more favourable effect on Comt expression. Moreover, the changes obtained in Ogg1, MsrA, Nrf2 expression show that DPCPX-Mg2+, DPCPX-Zn2+, istradefylline-Mg2+ and istradefylline-Zn2+ co-treatment may have greater antioxidant capacity benefits than administration of DPCPX and istradefylline alone. It seems plausible that a combination of selective A1 as well as an A2A receptor antagonist and magnesium or zinc may be a new antidepressant therapeutic strategy.

In the present study, the potential to design natural tea-infused set yoghurt was investigated. Three types of tea (Camellia sinensis): black, green and oolong tea as well as lemon balm (Melissa officinalis L.) were used to produce set yoghurt. The sensory quality (using Quantitative Descriptive Profile analysis and consumer hedonic test) and texture analysis, yield stress, physical stability and colour analysis were assessed to describe the profile of the yoghurt and influence of quality attributes of the product on the consumer acceptability of infused yoghurts in comparison with plain yoghurt. Among the analyzed plant additives for yoghurt, addition of 2% oolong tea to the yoghurt allows a functional food to be obtained with satisfactory texture and sensory properties, accepted by consumers at the same level as for control yoghurt. Both types of yoghurt were also characterised by high consumer willingness to buy, which confirms the legitimacy of using oolong tea as a natural, functional yoghurt additive that improves the sensory quality of the product. The high overall quality of yoghurt with oolong tea in comparison to other plant extracts was associated with the intensive peach flavour and odour, nectar and sweet odour and flavour, and the highest creaminess and thickness. That was confirmed by principal component analysis (PCA) where the overall sensory quality of yoghurts was mainly positively correlated with peach flavour and odour, sweet odour and yoghurt odour, while it was negatively correlated with herbs flavor and odour, and green tea flavour and odour. The sensory profile confirmed no differences in textural profile between plain yoghurt and the tea-infused one measured in the mouth, which corresponds to the result of textural properties such as firmness and adhesiveness.

Background The purpose of the study was to evaluate the in vitro antibacterial effect of experimental eye drops with bacteriophages in elimination of Staphylococcus spp. isolated from dogs with bacterial conjunctivitis.. The bacterial material was collected from dogs with independent clinical signs of bacterial conjunctivitis. Staphylococcus spp. were identified by phenotypic and genotypic methods (MALDI-TOF MS mass spectrometry). Antibiotic resistance was determined by the disc-diffusion method. Phage activity (Plaque forming units, PFU) was determined on double-layer agar plates. Phages with lytic titres > 108 PFU were used to prepare eye drops. The stability of the antibacterial titre was evaluated for preparations stored in sealed bottles as well as after opening and reclosing. Results The tests confirmed the occurrence of Staphylococcus spp. strains as etiological agents of bacterial conjunctivitis in dogs. A high percentage of strains were resistant to more than three antibiotics. The experimental phage eye drops used in the study exhibited 100% efficacy in vitro against the tested Staphylococcus isolates. Particularly noteworthy is the long duration of activity and constant antibacterial lytic titre of ≥108 PFU/mL of two eye drop solutions, nos. 7 and 12, after the bottle had been opened (21 days) and after hermetically sealed packaging (28 days) at 4–8 °C. Conclusions The results represent the first stage of research and require continuation in vivo. If positive effects are obtained in animals, the results can be used in applied research in humans and animals.

The article Long-term vigabatrin treatment modifies pentylenetetrazole-induced seizures in mice: focused on GABA brain concentration.

Available data support the notion that cannabinoids, whose therapeutic value is limited due to severe adverse reactions, could be beneficial as adjunctive agents in the management of mood disorders. Polytherapy, which is superior to monotherapy in the terms of effectiveness, usually requires lower doses of the individual components. Therefore, the main objective of our study was to determine whether administration of cannabinoid (CB) receptor ligands would enhance the antidepressant activity of atypical antidepressant drugs, i.e. agomelatine and tianeptine. To evaluate the antidepressant-like potential of the tested combinations, the mouse forced swim test (FST) and the tail suspension test (TST) were used. The HPLC method was applied to assess the brain levels of agomelatine and tianeptine. Both behavioural tests demonstrated that per se an ineffective intraperitoneal dose of oleamide (CB1 receptor agonist, 5 mg/kg) potentiated the anti-immobility activity of tianeptine (15 mg/kg), whereas AM251 (CB1 receptor inverse agonist/antagonist, 0.25 mg/kg) enhanced the antidepressant effects of tianeptine and agomelatine (20 mg/kg). Intraperitoneal co-administration of per se inactive doses of AM630 (CB2 receptor inverse agonist/antagonist) and agomelatine or tianeptine significantly reduced the immobility time of animals only in the FST. CB receptor ligands did not affect the brain levels of the tested atypical antidepressants. In summary, the outcomes of the present study showed that activation and inhibition of CB1 receptors as well as inhibition of CB2 receptors may increase the antidepressant activity of tianeptine, whereas only inhibition of CB1 and CB2 receptors has a potential to augment the antidepressant activity of agomelatine.

The purpose of this work was to determine the effect of starch hydrolysates (SH) on the physicochemical properties of suppositories. The study was conducted with suppositories with acetaminophen (AAP) a typical antipyretic analgesic, as model drug on lipophilic (cocoa butter) and hydrophilic base (polyethylene glycol 1500+400). The suppositories with and without the addition of SH were examined for physicochemical tests according to European Pharmacopoeia 8th edition (Ph. Eur.): the uniformity of mass of single-dose preparation test, the softening time determination of lipophilic suppositories test, the disintegration of suppositories test, and dissolution test with flow-through apparatus. The results confirm the possibility of using starch hydrolysates as a cheap and safe addition to modify physicochemical properties of suppositories.

Available data support the notion that cannabinoids, whose therapeutic value is limited due to severe adverse reactions, could be beneficial as adjunctive agents in the management of mood disorders. Polytherapy, which is superior to monotherapy in the terms of effectiveness, usually requires lower doses of the individual components. Therefore, the main objective of our study was to determine whether administration of cannabinoid (CB) receptor ligands would enhance the antidepressant activity of atypical antidepressant drugs, i.e. agomelatine and tianeptine. To evaluate the antidepressant-like potential of the tested combinations, the mouse forced swim test (FST) and the tail suspension test (TST) were used. The HPLC method was applied to assess the brain levels of agomelatine and tianeptine. Both behavioural tests demonstrated that per se an ineffective intraperitoneal dose of oleamide (CB

Background The goal of our study was to examine the long-term effect of vigabatrin (VGB), a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor on clonazepam (CLO), ethosuximide (ETX) and valproate (VPA) anticonvulsive activity against pentylenetetrazole (PTZ)-induced seizures in mice. Methods VGB was administered for 3 and 7 days. Convulsions were evoked by PTZ at its CD97 (99 mg/kg). The influence of CLO, ETX and VPA alone or in combination with VGB on motor performance and long-term memory was analyzed. γ-aminobutyric acid (GABA) concentration in mice brain and plasma as well as glutamate decarboxylase (GAD) activity was measured. Results After 3 days of treatment, VGB in doses up to 500 mg/kg increased PTZ-induced seizure threshold, whereas after 7 days VGB (at the dose of 125 mg/kg) inhibited clonic seizures in experimental mice. 7 days of VGB administration did not change the protective effect of CLO, ETX and VPA against PTZ-induced seizures. 7 days of VGB treatment at a subthreshold dose of 75 mg/kg decreased TD50 of ETX and CLO in the chimney test, but did not affect TD50 value for VPA. 7 days of VGB administration in combination with AEDs did not affect long-term memory in mice. VGB after 3 days or 7 days of administration increased brain GABA concentration. GAD activity was decreased after 3 and 7 days of VGB administration. Conclusions The presented results confirm anticonvulsive activity of VGB through GABA metabolism alteration and suggest care when combining VGB with ETX or CLO in the therapy.

Unsatisfactory therapeutic effects of currently used antidepressants force to search for new pharmacological treatment strategies. Recent research points to the relationship between depressive disorders and the adenosinergic system. Therefore, the main goal of our studies was to evaluate the effects of DMPX (3 mg/kg, i.p.), which possesses selectivity for adenosine A2A receptors versus A1 receptors, on the activity of imipramine (15 mg/kg, i.p.), escitalopram (2.5 mg/kg, i.p.), and reboxetine (2 mg/kg, i.p.) given in subtherapeutic doses. The studies carried out using the forced swim and tail suspension tests in mice showed that DMPX at a dose of 6 and 12 mg/kg exerts antidepressant-like effect and does not affect the locomotor activity. Co-administration of DMPX at a dose of 3 mg/kg with the studied antidepressant drugs caused the reduction of immobility time in both behavioral tests. The observed effect was not associated with an increase in the locomotor activity. To evaluate whether the observed effects were due to a pharmacokinetic/pharmacodynamic interaction, the levels of the antidepressants in blood and brain were measured using high-performance liquid chromatography. It can be assumed that the interaction between DMPX and imipramine was exclusively pharmacodynamic in nature, whereas an increased antidepressant activity of escitalopram and reboxetine was at least partly related to its pharmacokinetic interaction with DMPX.

Adenosine, an endogenous nucleoside, modulates the release of monoamines, e.g., noradrenaline, serotonin, and dopamine in the brain. Both nonselective and selective stimulation of adenosine receptors produce symptoms of depression in some animal models. Therefore, the main objective of our study was to assess the influence of a selective adenosine A1 receptor antagonist (DPCPX) and a selective adenosine A2A receptor antagonist (DMPX) on the activity of agomelatine and tianeptine. The forced swim test (FST) and tail suspension test (TST) were performed to assess the effects of DPCPX and DMPX on the antidepressant-like activity of agomelatine and tianeptine. Drug serum and brain levels were analyzed using HPLC. Co-administration of agomelatine (20 mg/kg) or tianeptine (15 mg/kg) with DMPX (3 mg/kg), but not with DPCPX (1 mg/kg), significantly reduced the immobility time both in the FST and TST in mice. These effects were not associated with an enhancement in animals’ spontaneous locomotor activity. The observed changes in the mouse behavior after concomitant injection of DMPX and the tested antidepressant agents were associated with elevated brain concentration of agomelatine and tianeptine. Our study shows a synergistic action of the selective A2A receptor antagonist and the studied antidepressant drugs, and a lack of such interaction in the case of the selective A1 receptor antagonist. The interaction between DMPX and agomelatine/tianeptine at least partly occurs in the pharmacokinetic phase. A combination of a selective A2A receptor antagonist and an antidepressant may be a new strategy for treating depression.

Adenosine, an endogenous nucleoside, modulates the release of monoamines, e.g., noradrenaline, serotonin, and dopamine in the brain. Both nonselective and selective stimulation of adenosine receptors produce symptoms of depression in some animal models. Therefore, the main objective of our study was to assess the influence of a selective adenosine AThe forced swim test (FST) and tail suspension test (TST) were performed to assess the effects of DPCPX and DMPX on the antidepressant-like activity of agomelatine and tianeptine. Drug serum and brain levels were analyzed using HPLC.Co-administration of agomelatine (20 mg/kg) or tianeptine (15 mg/kg) with DMPX (3 mg/kg), but not with DPCPX (1 mg/kg), significantly reduced the immobility time both in the FST and TST in mice. These effects were not associated with an enhancement in animals' spontaneous locomotor activity. The observed changes in the mouse behavior after concomitant injection of DMPX and the tested antidepressant agents were associated with elevated brain concentration of agomelatine and tianeptine.Our study shows a synergistic action of the selective A

Background β2-Adrenergic receptor agonists are widely used agents in the treatment of asthma or preterm labor. Since prevalence of asthma was shown to be higher in patients with epilepsy and modulation of noradrenergic system activity may modify epilepsy course, the aim of the present study was to examine the effect of salbutamol (SALB), one of the most commonly used β2-adrenergic receptor agonist on the anticonvulsant potency of four classical antiepileptic drugs (AEDs): valproate (VPA), carbamazepine (CBZ), phenytoin (DPH) and phenobarbital (PB) in mice subjected to the maximal electroshock (MES)-induced seizures. Methods Seizures were caused by a current delivered through ear-clip electrodes. The influence of AEDs and SALB on animals’ motor coordination and memory processes was also evaluated. Results Single SALB injection did not change, whereas 7 days SALB administration decreased seizure threshold in the MES-induced seizures in mice. Moreover, SALB injected ip for 1 day and for 7 days lowered the antiepileptic activity of PB in the MES-induced seizures in mice, but did not change the effect of other analyzed AEDs: VPA, CBZ or DPH. Butoxamine, a selective β2-adrenergic receptor antagonist, reversed SALB influence on the activity of PB. SALB given alone or in combination with the tested AEDs did not affect animals’ motor performance and memory after both single and 7 days administration. Conclusions Presented results show that SALB may decrease the antiepileptic efficacy of PB. A special caution is advised to patients with epilepsy receiving β2-adrenergic receptors agonists in the pharmacotherapy of pulmonary and obstetrical disorders.

The main goal of the present study was to evaluate the influence of the adenosine A1 receptor (A1R) antagonist — DPCPX — on depressive-like behavior in mice, as well as the effect of DPCPX on the activity of imipramine, escitalopram, and reboxetine, each at non-effective doses. The influence of DPCPX on behavior and its influence on the activity of selected antidepressants was evaluated in the forced swim test (FST) and the tail suspension test (TST) in mice. Locomotor activity was measured to verify and exclude false-positive data obtained in the FST and TST. Moreover, serum and brain concentrations of tested antidepressants were determined using HPLC. DPCPX, at doses of 2 and 4 mg/kg, exhibited antidepressant activity in the FST and TST, which was not related to changes in the spontaneous locomotor activity. Co-administration of DPCPX with imipramine, escitalopram, or reboxetine, each at non-active doses, significantly reduced the immobilization period in the FST and TST in mice, which was not due to the increase in locomotor activity. Both antagonists of 5-HT receptors (WAY 100635 and ritanserin) completely antagonized the effect elicited by DPCPX in the behavioral tests. Results of assessment of the nature of the interaction between DPCPX and test drugs show that in the case of DPCPX and imipramine or reboxetine, there were pharmacodynamic interactions, whereas the DPCPX-escitalopram interaction is at least partially pharmacokinetic in nature. Presented outcomes indicate that an inhibition of A1Rs and an increase of monoaminergic transduction in the CNS may offer a novel strategy for the development of antidepressant drugs.

Objective The main goal of our study was to investigate whether a selective antagonism of the adenosine A1 or A2A receptors is able to enhance the antidepressant activity of commonly prescribed drugs. Materials and methods All experiments were carried out on male Albino Swiss mice. The forced swim test and the tail suspension test were used to evaluate the antidepressant-like potential. Drug concentrations in animals’ serum and brains were measured by high-performance liquid chromatography. Key findings The antidepressant potential of moclobemide (1.5 mg/kg), venlafaxine (1 mg/kg) and bupropion (10 mg/kg) was enhanced by a co-administration with 3,7-dimethyl-1-propargylxanthine (DMPX; an antagonist of adenosine A2A receptors; 3 mg/kg) or 8-cyclopentyl-1,3-dipropylxanthine (an antagonist of adenosine A1 receptors; 1 mg/kg). However, significant interactions between the tested substances were detected only in the experiments with DMPX. The nature of the observed interplays is rather pharmacodynamic than pharmacokinetic, because neither serum nor brain concentrations of the used drugs were significantly increased. Conclusions Blockage of the adenosine receptors (particularly the A2A subtypes) could be considered in future as a novel, promising part of the combined antidepressant therapy. However, further studies on this subject are needed.

The roasting stage constitutes a key component in the manufacturing process of natural coffee because temperature elicits changes in bioactive compounds such as polyphenols and that Maillard-reaction compounds appear, thus affecting the product’s sensory and antioxidant properties. Actual contents of these compounds may depend on which region the coffee is cultivated as well as the extent to which the beans are roastedTo determine polyphenols content and antioxidant activity in the ‘Arabica’ coffee type coming from various world regions of its cultivation and which have undergone industrial roasting. Also to establish which coffee, taking into account the degree of roasting (ie. light, medium and strong), is nutritionally the most beneficialThe study material was natural coffee beans (100% Arabica) roasted to various degrees, as aforementioned, that had been cultivated in Brazil, Ethiopia, Columbia and India. Polyphenols were measured in the coffee beans by spectrophotometric means based on the Folin-Ciocalteu reaction, whereas antioxidant activity was measured colourimetrically using ABTS+ cat-ionic radicalsPolyphenol content and antioxidant activity were found to depend both on the coffee’s origin and degree of roasting. Longer roasting times resulted in greater polyphenol degradation. The highest polyphenol concentrations were found in lightly roasted coffee, ranging 39.27 to 43.0 mg/g, whereas levels in medium and strongly roasted coffee respectively ranged 34.06 to 38.43 mg/g and 29.21 to 36.89 mg/g. Antioxidant activity however significantly rose with the degree of roasting, where strongly roasted coffee had higher such activity than lightly roasted coffee. This can be explained by the formation of Maillard-reaction compounds during roasting, leading then to the formation of antioxidant melanoidin compounds which, to a large extent, compensate for the decrease in polyphenols during roastingPolyphenols levels and antioxidant activities in the studied Arabica coffee beans that had undergone roasting depended on the cultivation region of the world. Longer roasting caused a significant decline in polyphenols compound levels (from 7.3% to 32.1%) in the coffee beans. Antioxidant activities of coffee increased with roasting, despite reduced levels of natural antioxidants. From a nutritional standpoint, the most favoured coffees are those lightly or medium roasted

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.

Recent preclinical and clinical data suggest that low dose of caffeine enhances the effects of common antidepressants. Here we investigated the effects of chronic administration of caffeine (5mg/kg, twice daily for 14days) and its withdrawal on day 15th on the activity of per se ineffective doses of fluoxetine (5mg/kg) and escitalopram (2mg/kg) given on day 15th. We found decreased immobility time in the forced swim and tail suspension tests in mice in which caffeine was administered simultaneously with antidepressants on day 15th following a 14-day caffeine treatment and no alterations in the spontaneous locomotor activity. A decrease in the level of escitalopram and an increase in the level of caffeine in serum were observed after concomitant administration of these compounds, while the joint administration of caffeine and fluoxetine was not associated with changes in their levels in serum or brain. Caffeine withdrawal caused a decrease in Adora1 mRNA level in the cerebral cortex (Cx). Administration of escitalopram or fluoxetine followed by caffeine withdrawal caused an increase in this gene expression, whereas administration of escitalopram, but not fluoxetine, on day 15th together with caffeine caused a decrease in Adora1 mRNA level in the Cx. Furthermore, antidepressant-like activity observed after joint administration of the tested drugs with caffeine was associated with decreased Slc6a15 mRNA level in the Cx. The results show that withdrawal of caffeine after its chronic intake may change activity of antidepressants with concomitant alterations within monoamine, adenosine and glutamate systems.

Pre-clinical and clinical studies indicated that a blockade of the NMDA receptor complex creates new opportunities for the treatment of affective disorders, including depression. The aim of the present study was to assess the influence of traxoprodil (10 mg/kg) on the activity of desipramine (10 mg/kg), paroxetine (0.5 mg/kg), milnacipran (1.25 mg/kg), and bupropion (10 mg/kg), each at sub-therapeutic doses. Moreover, brain levels of traxoprodil and tested agents were determined using HPLC. The obtained results were used to ascertain the nature of occurring interaction between traxoprodil and studied antidepressants. The experiment was carried out on naïve adult male Albino Swiss mice. Traxoprodil and other tested drugs were administered intraperitoneally. The influence of traxoprodil on the activity of selected antidepressants was evaluated in forced swim test (FST). Locomotor activity was estimated to exclude false positive/negative data. To assess the influence of traxoprodil on the concentration of used antidepressants, their levels were determined in murine brains using HPLC. Results indicated that traxoprodil potentiated activity of all antidepressants examined in FST and the observed effects were not due to the increase in locomotor activity. Only in the case of co-administration of traxoprodil and bupropion, increased bupropion concentrations in brain tissue were observed. All tested agents increased the traxoprodil levels in the brain. Administration of a sub-active dose of traxoprodil with antidepressants from different chemical groups, which act via enhancing monoaminergic transduction, caused the antidepressant-like effect in FST in mice. The interactions of traxoprodil with desipramine, paroxetine, milnacipran, and bupropion occur, at least partially, in the pharmacokinetic phase.

Dissolution rate of an active substance from suppositories may be altered by the qualitative and quantitative selection of suitable excipients. Thus, the accelerated-release or sustained-release suppositories can be manufactured. The objective of our study was to prepare the suppositories containing paracetamol in Novata BD and Novata BCF bases by the fusion method as well as to evaluate the influence of addition of the bioadhesive substances, namely: hydroxypropyl methyl cellulose (HPMC) and methylcellulose (MC) at concentrations of 5, 10, 15 and 20%, on the physico-chemical properties of suppositories. Assessment of the preparations were based on the outcomes of the following tests: uniformity of mass, uniformity of content of active substance, hardness of suppositories, softening time determination and the disintegration time of suppositories. Release of the active substance into the phosphate buffer at pH 7.2 was also performed. Content of the active substance was determined spectrophotometrically at 243 nm. On the basis of the obtained results it may be concluded that the addition of MC at concentrations of 15%, 20% and HPMC at concentrations of 5%, 10%,15%, 20% delays the release of active substance from suppositories. The physical properties of the prepared suppositories met the requirements of the Polish Pharmacopoeia, 9th edition.

The aim of the study was preparing the skin formulations with ibuprofen as ointments, creams and gels. They have been prepared by two methods; melting the components and then mixing (method 1) and in the unqutor (method 2). The preparations have been tested rheologically and determined for the consistency, pH and spreadability ex tempore and after 3 months of storage at 4° C. The studies showed that the consistency is stable during all the time of storage. The pH values were within the tolerance of the skin. The formulations prepared in the unquator have better consistency, spreadability and lower viscosity.

One of the newest substances, whose antidepressant activity was shown is traxoprodil, which is a selective antagonist of the NR2B subunit of the NMDA receptor. The main goal of the present study was to evaluate the effect of traxoprodil on animals’ behavior using the forced swim test (FST), as well as the effect of traxoprodil (10 mg/kg) on the activity of antidepressants, such as imipramine (15 mg/kg), fluoxetine (5 mg/kg), escitalopram (2 mg/kg) and reboxetine (2.5 mg/kg). Serotonergic lesion and experiment using the selective agonists of serotonin receptors 5-HT1A and 5-HT2 was conducted to evaluate the role of the serotonergic system in the antidepressant action of traxoprodil. Brain concentrations of tested agents were determined using HPLC. The results showed that traxoprodil at a dose of 20 and 40 mg/kg exhibited antidepressant activity in the FST and it was not related to changes in animals’ locomotor activity. Co-administration of traxoprodil with imipramine, fluoxetine or escitalopram, each in subtherapeutic doses, significantly affected the animals’ behavior in the FST and, what is important, these changes were not due to the severity of locomotor activity. The observed effect of traxoprodil is only partially associated with serotonergic system and is independent of the effect on the 5-HT1A and 5-HT2 serotonin receptors. The results of an attempt to assess the nature of the interaction between traxoprodil and the tested drugs show that in the case of joint administration of traxoprodil and fluoxetine, imipramine or escitalopram, there were interactions in the pharmacokinetic phase.

The purpose of this work was to investigate the influence of starch hydrolysates in the dissolution process of the substance practically insoluble in water. Progesterone and ibuprofen were chosen as model substances. The study was conducted with a constant amount of the drug (25 mg/mL) or constant amount of starch hydrolysate (50 mg/mL). Next, the influence of ethanolic solutions (10-30% v/v) on solubility of drug was tested. The results confirm the possibility of using starch hydrolysate as a cheap and safe addition to increase the solubility of practically insoluble drugs.

Purpose The study aims to assess the anticonvulsant effects offered by benzylamide nicotinic acid (Nic-BZA) in many animal models of chemically-induced seizures (i.e., pentylenetetrazole [PTZ], pilocarpine [PILO], bicuculline [BIC], α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid [AMPA], kainic acid [KA], and N -methyl- d -aspartic acid [NMDA]). Additionally, it analyses side effects of administering Nic-BZA in the form of loss of co-ordination and memory impairment as evaluated in the rotarod and passive avoidance tests, respectively. Results Antiseizure activity of Nic-BZA was reported in numerous models of chemically-induced seizures and its ED 50 value was 37.1 mg/kg for PTZ, 53.0 mg/kg for AMPA, 81.4 mg/kg for BIC, 86.3 mg/kg for KA, and 182.6 mg/kg for PILO. Moreover, Nic-BZA was totally ineffective (in dosages of up to 200 mg/kg) in mice challenged with NMDA-induced seizures. The evaluation of the side effects present shortly after dosing in the rotarod test has revealed neurotoxicity of Nic-BZA with experimentally determined TD 50 value of 188.5 mg/kg. Protective index (PI) assessment analysis for Nic-BZA has disclosed a substantial difference between the dosage resulting in acute impairment of co-ordination and the dosage resulting in anticonvulsant effect in various chemically evoked seizures, remaining practically ineffective (in dosages of up to 200 mg/kg) in mice subjected to the NMDA-induced seizure test. Additionally, Nic-BZA (in dosages of up to 100 mg/kg) did not impair long-term memory in mice. Conclusions Summing up, Nic-BZA has a wide anticonvulsant effect in different experimental epilepsy models.

Purpose The aim of this study was to evaluate the effects of 1-day, 7-day and 14-day administrations of cimetidine on the anticonvulsant activity of conventional antiepileptic drugs (AEDs; valproate, carbamazepine, phenytoin and phenobarbital) against maximal electroshock (MES)-induced convulsions in mice. Methods Electroconvulsions were evoked in Albino Swiss mice by a current delivered via ear-clip electrodes. In addition, the effects of cimetidine, AEDs alone and their combinations were studied on performance and long-term memory tests. Pharmacokinetic changes in plasma and brain concentrations of AEDs after cimetidine administration were evaluated with immunofluorescence. Results Cimetidine (up to 100 mg/kg) after 1-day administration did not affect the electroconvulsive threshold in animals. Moreover, in the 14-day treatment, cimetidine administered at a dose of 40 mg/kg did not significantly change the electroconvulsive threshold in the MES-test, cimetidine administered 14-day (at 20 mg/kg) significantly increased the anticonvulsant activity of carbamazepine, staying without effects after a 1-day and 7-day studies. In contrast, both the 7-day and 14-day administrations of cimetidine resulted in significant reductions of protective efficacy of the phenobarbital. Only valproate and phenytoin were not affected by cimetidine (20 mg/kg) in all experimental period. Cimetidine administered 1-day, did not alter total brain concentrations and free plasma levels of all AEDs tested, whilst the 14-day study elevated carbamazepine plasma and brain concentration and reduced phenobarbital brain concentration. Cimetidine co-applied with AEDs did not impair performance of mice evaluated in the chimney test however, it worsened long-term memory in animals. Conclusions Based on this preclinical study, a special caution is advised when treating epileptic patients with combinations of phenobarbital or carbamazepine with cimetidine.

Five nonisotonised emulsions with different degree of compaction containing 1% solution of phenobarbital in soybean oil, lecithin, human albumin and four concentrated emulsions with the same composition containing the addition of isotonic agents such as: glucose, sodium chloride, Ringer salt, glycerin were prepared. The release of phenobarbital was examined by dialysis through the semipermeable membrane using the modified Franz diffusion cell. The studies show that the release is a diffuse. Phenobarbital releases with a lag time and the process is biphasic; first faster, in the second stage slower. The release of phenobarbital depends on the amount of external phase (water) in nonisotonised emulsions and on the kind of using isotonic agent in concentrated emulsions.