rss_2.0Sciendo RSS Feed for European Pharmaceutical Journalhttps://sciendo.com/journal/AFPUChttps://www.sciendo.comhttps://sciendo-parsed.s3.eu-central-1.amazonaws.com/6470850a71e4585e08a9f127/cover-image.jpghttps://sciendo.com/journal/AFPUC140216https://sciendo.com/article/10.2478/afpuc-2024-0010<abstract> <title style='display:none'>Abstract</title> <p>Luteolin, a flavonoid, has been reported to inhibit the enhanced endothelial permeability in vitro. The purpose of this study was to determine the mechanism of luteolin affected the in vitro suppression of elevated endothelial permeability involves protein kinase C activity and intracellular calcium concentration. The inducer bradykinin was tested using the in vitro vascular permeability assay in endothelial cells obtained from human umbilical vein endothelial cells (HUVECs). Protein kinase C assay test and the intracellular calcium concentration were also determined. Results revealed luteolin (5, 10, and 25 μM) significantly suppressed increased endothelial permeability (<italic>P</italic> &lt; 0.001). The increased activity of protein kinase C was significantly suppressed by luteolin at the dose of 5 μM (<italic>P</italic> &lt; 0.05), 10 μM (<italic>P</italic> &lt; 0.01), and 25 μM (<italic>P</italic> &lt; 0.01). The increased concentration of intracellular calcium was significantly suppressed by luteolin at the dose of 10 μM (<italic>P</italic> &lt; 0.01) and 25 μM (<italic>P</italic> &lt; 0.001). Collectively, these results showed luteolin suppressed the activity of protein kinase C and suppressed the increased concentration of intracellular calcium when HUVECs were induced by bradykinin, leading to the suppression of increased endothelial permeability as the nitric oxide-cyclic guanosine monophosphate (NO-cGMP ) pathway was being inactivated. This may explain the pharmacologic properties of luteolin, which is anti-inflammatory, antioxidant, and neuroprotective. These results also revealed the potential use of luteolin in treating many other diseases involve endothelial permeability.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00102024-09-26T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0009<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>In case of exocrine pancreatic insufficiency (EPI), the replacement of digestive enzymes with, for example porcine pancreatin or fungal rizoenzymes, is unavoidable under certain conditions. Current guidelines indicate that preparations from porcine pancreas have more advantageous physicochemical properties compared to those from fungi, especially at high bile salt concentrations, and that the latter can, therefore, only be used clinically to a limited extent. Since rizoenzymes are increasingly used in clinical practice, the present <italic>in vitro</italic> study investigated efficiency of enzymatic activity of rizoenzymes in comparison to pancreatin under various physiological and partly extreme environmental conditions.</p> </sec> <sec><title style='display:none'>Materials and Methods</title> <p>The lipolytic properties of two typical preparations containing digestive enzymes from porcine pancreatin and rizoenzymes were compared (same dosage of activity units) at different pH values (pH 3–9), with the addition of different bile salt concentrations (0–15 mmol/L sodium taurocholate). Lipolytic activity was measured by quantifying the fatty acids released from olive oil substrate by liquid chromatography–tandem mass spectrometry after enzymatic digestion.</p> </sec> <sec><title style='display:none'>Results</title> <p>For both enzyme preparations, the lipolytic activity maximum was reached at pH 7 with comparable fatty acid conversion rates (57% pancreatin, 58% rizoenzymes). However, in contrast to pancreatin, rizoenzymes were already active for certain fatty acids from pH 3 to 4. At a bile salt concentration up to 10 mmol/L taurocholate, there was an increase in activity of both enzyme preparations (rizoenzymes 69% vs. pancreatin 58% enzymatic conversion). Only at rather unphysiological concentration of 15 mmol/L during EPI, there was a slight decrease in activity (to 56%) for the rizoenzymes.</p> </sec> <sec><title style='display:none'>Conclusions</title> <p>Rizoenzymes are an alternative therapeutic option for EPI. Relevant differences between rizoenzymes and pancreatin with regard to lipolytic activity under different physicochemical conditions could not be demonstrated in this study, whereas a potential advantage in favor of rizoenzymes activity at already low pH values was observed.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00092024-08-10T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0008<abstract> <title style='display:none'>Abstract</title> <p>While many types of diabetes medications are currently available, orally administered formulations of glucagon-like peptide-1 (GLP-1) receptor agonists have recently been launched. Therefore, gastrointestinal epithelial cells will be increasingly exposed to GLP-1 receptor agonists; however, their effects on these cells remain unclear. The present study attempted to clarify the effects of GLP-1 receptor agonists on intestinal epithelial barrier functions. Semaglutide (5, 50, and 500 ng/mL) and dulaglutide (15, 150, and 1500 ng/mL) were selected as GLP-1 receptor agonists and applied to the Caco-2 cell line. Changes in mRNA and protein expression levels of epithelial cell barrier regulators due to exposure to GLP-1 receptor agonists were examined by real-time RT-PCR and Western blotting. Neither semaglutide nor dulaglutide changed the growth rate or ratio of Caco-2 cells. Furthermore, they did not significantly affect the mRNA expression levels of membrane proteins involved in epithelial cell barrier functions. However, dulaglutide increased the protein expression levels of these membrane proteins in a concentration-dependent manner, whereas semaglutide did not. Only dulaglutide enhanced epithelial cell barrier functions. Since various gastrointestinal symptoms develop in patients with diabetes and epithelial cell barrier functions may be compromised, medicines that promote barrier function, such as dulaglutide, may effectively attenuate these changes. However, their mechanisms of action remain unknown; therefore, further studies are warranted.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00082024-08-07T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0007<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Background</title> <p>White-water yam (<italic>Dioscorea alata L</italic>.) is one of the potential sources of starch; however, it is not yet available for commercial purposes. Besides, native white-water yam starch (WS) presents limited functionality due to poor flowability, mechanical properties and instability at high temperature and acidic conditions. Therefore, this study aims to modify the starch to improve its characteristics and make it useful as an excipient for the preparation of the tablets.</p> </sec> <sec><title style='display:none'>Materials and methods</title> <p>The modification of WS was achieved by physical and chemical treatments, specifically pre-gelatinization and phosphorylation, respectively. Pre-gelatinization WS involves heating, meanwhile phosphorylation WS is obtained by treating WS with sodium tripolyphosphate.</p> </sec> <sec><title style='display:none'>Results</title> <p>The results showed that the powder of the modified WS has good characteristics which improved the flowability of the powder mixture as a granule based on density, porosity, compressibility index and swelling power determination. The WS granules were found to display the oval or irregular (polygonal) shape with the amylose content 11.92±0.61% for unmodified WS, 10.41±0.90% for pre-gelatinized WS and 12.61±1.75% for phosphorylated WS. Furthermore, the granule was formulated as an excipient in tablet preparations, and the formulas were compressed after wet granulation. The mechanical properties of the tablets were assessed using uniformity of mass and size, hardness, friability and disintegration time. WS modification affects the hardness of tablets when used as a binder. Phosphorylated WS is recommended to be used as a binder in wet granulation formulations because it produces tablets with a longer disintegration time, which means better binding ability. However, the utilization of modified WS with both pre-gelatinization and phosphorylation leads to tablets with low brittleness compared to others with unmodified binder with the disintegration time still met the requirement of fast disintegrating tablet (&lt;15 minutes).</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>All the physical properties studied indicated that the modified WS is a promising pharmaceutical excipient in tablets.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00072024-06-08T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0005<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Objective</title> <p>The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets.</p> </sec> <sec><title style='display:none'>Materials and methods</title> <p>To increase the solubility and bioavailability of valsartan, a low-soluble antihypertensive drug, immediate release dosage forms were formulated by a direct compression method using a solid dispersion technique with three different carriers (β-cyclodextrin, polyvinyl pyrrolidone K30 and poloxamer 188) at three different ratios (1:3, 1:4 and 1:5). Nine physical mixtures (PM1–PM9) were prepared and various physical parameters were characterised in <italic>in vitro</italic> release studies.</p> </sec> <sec><title style='display:none'>Results</title> <p>Out of the prepared physical mixtures, PM8 showed the best results, with 94.2% of the drug dissolving within 30 min. Formulation PM8 solid dispersion further used for the preparation of valsartan immediate release tablets by using sodium starch glycolate superdisintegrant, at different concentrations (3%, 4% and 5%; i.e., IF1, IF2 and IF3 formulations, respectively). The optimised formulation showed friability and disintegration values of 0.456±0.9 and 6.2±0.4 min. Among the three immediate release formulations, IF2, which contains 4% sodium starch glycolate, demonstrated an 84.46% drug release in 30 min and a 99.69% drug release in 1 hr, indicating increased drug solubility. When compared with a valsartan pure drug, the solubility of the solid dispersion increased by 135.06-fold.</p> </sec> <sec><title style='display:none'>Discussion and conclusion</title> <p>The results show that the optimised IF2 formulation demonstrated enhanced drug solubility by 135.06-fold, using a solid dispersion technique with poloxamer 188. This can be explained by the conversion of crystalline to an amorphous form of drug, leading to a reduction in the contact angle between the drug and the gastric medium. It can be concluded that poloxamer 188 is a suitable carrier and that use of a physical mixture technique is an applicable method to improve the solubility of valsartan.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00052024-06-07T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0006<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>To determine the content of phenolcarboxylic acids using gas chromatography–mass spectrometer (GC–MS) in the obtained extract, conduct a study of the antimicrobial, antifungal, and antioxidant activities of <italic>Rubus idaeus</italic> shoot lipophilic extract.</p> </sec> <sec><title style='display:none'>Material/methods</title> <p>The quantification of phenolcarboxylic was accomplished through GC–MS, antioxidant activity was assessed by potentiometric method, antimicrobial and antifungal activities were determined by well method.</p> </sec> <sec><title style='display:none'>Results</title> <p>The 8 compounds were identified by the GC–MS method. The vanillic acid (2.59 ± 0.08 mg/100 g), benzoic acid (1.51±0.08 mg/100 g), and ferulic acid (0.79±0.04 mg/100 g) dominated in the obtained lipophilic <italic>R. idaeus</italic> shoot extract. <italic>Bacillus subtilis</italic> (17.00 ± 0.50 mm) was the most sensitive to lipophilic extract, whereas <italic>Proteus vulgaris</italic> was the most resistant to the lipophilic extract. Moreover, <italic>Candida albicans</italic> was medium sensitive to lipophilic extract (13.50 ± 0.50 mm). The antioxidant activity was 1.00 mmol-equiv./m_{dry res}; according to Maslov's antioxidant level classification it has low level.</p> </sec> <sec><title style='display:none'>Conclusions</title> <p>The lipophilic extract from <italic>R. idaeus</italic> shoots contains various phenolcarboxylic acids, including vanillic acid, benzoic acid, ferulic acid, <italic>p</italic>-hydroxybenzoic acid, syringic acid, gentisic acid, salicylic acid, and phenylacetic acid, with the highest concentrations observed for vanillic, benzoic, and ferulic acids. This study highlights the antimicrobial and antifungal properties of the <italic>R. idaeus</italic> shoot lipophilic extract. However, the obtained lipophilic extract showed a relatively low level of antioxidant activity. Consequently, the derivatives of phenolcarboxylic acids play a substantial role in the antimicrobial and antifungal effects, whereas their contribution to antioxidant activity appears to be limited.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00062024-06-07T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0004<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of olanzapine (OLZ) loaded solid lipid nanoparticles (SLNs) for sustained release.</p> </sec> <sec><title style='display:none'>Materials/methods</title> <p>OLZ SLNs were prepared by hot melt emulsification and ultrasonication using Precirol ATO 5 (PRE) as a solid lipid, combination of Kolliphor ELP (KELP) and Tween 80 (T80) as surfactants, after optimising formulation and process variables. The SLN system was subjected to evaluation of particle size, zeta potential, entrapment efficiency (EE), <italic>in-vitro</italic> drug release and <italic>ex-vivo</italic> intestinal permeability studies using the chicken intestinal segments (jejunum). Further, these SLNs were converted into stable DANs by adsorbing onto a Neusilin US2 (NUS2) and Avicel CL 611 (ACL) carriers using the granulation-evaporative drying method. The DANs were characterised for redispersion properties, <italic>in-vitro</italic> drug release, thermal behaviour, crystallinity, and morphology.</p> </sec> <sec><title style='display:none'>Results</title> <p>The SLN and DAN had a particle size of 238.0 nm [0.274 polydispersity index (PdI)] and 302.4 [0.494 PdI] respectively. The zeta potentials of SLN and DAN were found to be −29.3 mV and −26.3 mV, respectively. The SLN had 67% EE, and showed a sustained drug release in various media. The highest permeability of SLNs was observed in <italic>ex-vivo</italic> permeation model compared to the OLZ suspension, indicating that SLNs have the potential to bypass hepatic metabolism. The adsorption of SLNs onto carriers was confirmed by surface morphology. The DAN had good flow properties and sustained drug release similar to that of SLNs. The X-ray diffraction (XRD) patterns and endothermic peaks confirmed the complete encapsulation of actives in lipid matrices.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The encapsulating of OLZ in SLNs and converting it into DAN showed a sustained release and adsorption technique that can be used for improving the stability of NLC dispersion. The DANs can be offered in dosage forms such as filling into sachets, capsules and compressed into tablets.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00042024-04-20T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0003<abstract> <title style='display:none'>Abstract</title> <p>Metal complexes, which, under physiologic conditions, show redox properties and are able to bind to DNA, are great tools to cleave the DNA chain. This aspect is of great importance for their use as antineoplastic drugs. We synthesized ligands derived from short-chain amino acids and from salicylaldehyde. The prepared ligands of the type of reduced Schiff bases were subsequently used for the preparation of copper(II) complexes. The aim of the study was in vitro testing of copper(II) complexes, where it was confirmed that they are capable of cleaving DNA. Their cytotoxic activity was also confirmed by the resazurin redox method on Saccharomyces cerevisiae based on preserved healthy mitochondrial function.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00032024-03-28T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0001<abstract> <title style='display:none'>Abstract</title> <p>Mushrooms from the genus <italic>Cordyceps</italic> are characterized by a wide range of biological effects due to the diverse amount of substances contained in them and are an important source of bioactive compounds. In China, mushrooms of the genus <italic>Cordyceps</italic> have been used as a medicinal preparation of traditional Chinese medicine for centuries. So far, a considerable number of studies have been conducted that focused on analyzing the effects of <italic>Cordyceps</italic>, which include their antioxidant, antibacterial, immunomodulatory, antidiabetic, antitumor, and many other effects. The ability of fungi to form complexes with various metals is also interesting. It is believed that polysaccharides are the main component of the extracts involved in the complexation with metals, after which their biological effects are improved and deepened. The work deals with the comparison of the antioxidant and antibacterial effects of <italic>Cordyceps</italic> extracts with extracts of this mushroom enriched with silver ions. Based on scientific studies, it is assumed that there is a complexation between the chemical compounds of the extracts and silver.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00012024-03-18T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2024-0002<abstract> <title style='display:none'>Abstract</title> <p>Aminopeptidase N (APN) is a broad specificity zinc metallopeptidase with many functions that do not always depend on its enzymatic activity. Among others, it is involved in tumor angiogenesis and metastasizing and also serves as a cellular receptor of some coronaviruses. Some APN inhibitors, such as bestatin or tosedostat, were used or tested as anticancer drugs in the past. Within the past two decades, we have prepared several series of potential APN inhibitors. Some of them reached interesting values of inhibitory activity and were also successfully tested for antiproliferation activity in cancer cell lines. We also performed some QSAR studies with APN inhibitors prepared by us and other authors.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2024-00022024-03-18T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0023ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00232024-02-18T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0022ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00222024-02-18T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0006<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Background</title> <p>Mints (<italic>Mentha</italic> L., Lamiaceae) are medicinal plants frequently used in pharmacy, cosmetics, and food industry. Among the secondary metabolites found in mint, rosmarinic acid is one of the most abundant in the whole plant. Rosmarinic acid is known as a powerful antioxidant and anti-inflammatory agent.</p> </sec> <sec><title style='display:none'>Aim</title> <p>There is much information about the use and profile of secondary metabolites of mint's aerial parts. On the contrary, less is known about the secondary metabolites in the rhizomes. So, this research intended to determine the content of rosmarinic acid in the underground parts of 10 species of the genus <italic>Mentha</italic>, section <italic>Mentha</italic>.</p> </sec> <sec><title style='display:none'>Method</title> <p>High-performance liquid chromatography with diode array detection (HPLC-DAD) was used to identify and determine rosmarinic acid.</p> </sec> <sec><title style='display:none'>Results</title> <p>Rosmarinic acid was detected in all 10 species. The highest amount was found in <italic>Mentha × piperita</italic> L. “BULHARSKA 1” and <italic>Mentha rotundifolia</italic> (L.) Huds. The lowest content of rosmarinic acid was found in <italic>Mentha arvensis</italic> L., and a slightly higher content was measured in <italic>Mentha × piperita</italic> L.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The underground parts of mints seem to be an interesting source of natural antioxidants such as rosmarinic acid.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00062023-08-31T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0021ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00212023-11-28T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0010<abstract> <title style='display:none'>Abstract</title> <p>Taurine (2-aminoethanesulfonic acid) is a free sulfur-containing β-amino acid widely distributed in many mammalians. Owing to the energizing effects, it is mostly used in soft drinks and supplements for athletes. Regular intake of soft drinks may lead to an overdose of caffeine, taurine, and guarana and loss of bone mass, overweight, hypertension, and in older age, osteoporosis and cardiovascular diseases. Therefore, it is essential to control the maximum amount of taurine consumed by humans in the food and beverages. Here, a fast, simple, accurate, and robust method based on ultrahigh-performance liquid chromatography hyphenated with mass spectrometry (UHPLC-MS) was successfully applied for the determination of taurine in selected soft drinks sold in Slovakia. The method was characterized by coefficient of determination higher than 0.99, and the predicted value of the limit of detection was 4.29 μmol/L. The analyzed levels of taurine in selected commercial drinks ranged from 2.8 to 3.78 mg/mL. The concentration in one brand of the investigated drinks was found to be extremely low (about 70%) compared to the declared content by the manufacturer.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00102023-08-31T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0019<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>Vildagliptin/metformin 50 mg/1000 mg film coated tablets (Sensityn^®) is being developed for the treatment of type 2 diabetes mellitus. An open label, crossover, bioequivalence study (phase I) was conducted to assess the bioequivalence between Sensityn^® Film Coated Tablets (Test Product/Alpha Pharma Industries, a subsidiary of Cigalah Healthcare LLC, KAEC, Saudi Arabia) and Galvusmet^® Film Coated Tablets (Reference product/Novartis Pharma, Switzerland), in healthy adults under fed conditions. Safety and tolerance were evaluated as secondary endpoints.</p> </sec> <sec><title style='display:none'>Materials and methods</title> <p>A randomized study with two treatments, two periods, crossover, open-label, laboratory-blind, single dose, with a washout period of seven days under fed conditions in 36 healthy male subjects. These were administered medicinal drug product (Sensityn^®) or the reference medicinal product (Galvusmet^®); both as a single 50 mg/1000 mg oral dose, under fed conditions. Blood samples were collected for pharmacokinetic analysis before treatment and until 24.00h post-dosing in each study period. ANOVA analysis (test sequence, subjects’ nested within sequence, product and period effect) was performed using a 5% significance level for logarithmic and untransformed data for C_max AUC_0-t and AUC_0-∞ and for untransformed data for T_max, K_elimination (λz) and half-life.</p> </sec> <sec><title style='display:none'>Results</title> <p>The results showed that C_max, AUC_0-t, and AUC_0-∞ have passed the 90% CI acceptance limits of 80.00%–125.00% for vildagliptin and metformin. Consequently, the bioequivalence of Sensityn^® and Galvusmet^® film coated tablets was demonstrated under fed conditions. Treatment emergent adverse events were reported by 3 subjects and 1 subject following the administration of Sensityn^® and the Galvusmet^®, respectively.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The present findings confirmed that Sensityn^®, the test medicinal product is bioequivalent to Galvusmet^®, the reference medicinal product, in the rate and extent of absorption. Also, it has comparable safety profile. These findings support the continued development of vildagliptin/metformin 50 mg/1000 mg film coated tablets (Sensityn^®) for use in patients with type 2 diabetes mellitus.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00192023-10-20T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0018<abstract> <title style='display:none'>Abstract</title> <p>A revolutionary concept for achieving long-term medication release is the gastroretentive <italic>in situ</italic> gelling system. The goal of this research was to formulate and test a gastroretentive <italic>in situ</italic> gel for ketoprofen delivery to targeted site to increase the residence and delivery time. Ketoprofen gastroretentive <italic>in situ</italic> gels were synthesized using a cation-driven gelation approach using various combinations and concentrations of polymers such as gellan gum, sodium alginate, and hydroxypropyl methylcellulose (HPMC) K100M. Visual appearance, pH, viscosity, <italic>in vitro</italic> gelation, <italic>in vitro</italic> buoyancy, drug content, density measurement, gel strength measurement, water uptake, and <italic>in vitro</italic> drug release were all evaluated. The total floating time was more than 12 h, with a floating lag time of less than 2 min. The formulations showed pH ranging from 6.89 to 7.61 and drug content ranging from 82.01% to 95.53%. For 11 h, the percent cumulative drug release of formulations F5 and F14, which contained a greater concentration of polymer sodium alginate (1.5%) and a combination of gellan gum and HPMC K100M (0.175% and 0.2%), was 84.10% and 85.49%, respectively. <italic>In vitro</italic> dissolution experiments and stability investigations both revealed no significant changes in drug content. The findings revealed that the formulated <italic>in situ</italic> gels aided in extending gastric residence duration, allowing the drug to be released in the stomach.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00182023-10-07T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0003<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Objective</title> <p>Due to the severe side effects of long-term treatment using hormone replacement therapy, Raloxifene (RLX) is introduced with beneficial effects on rheumatoid arthritis (RA) for postmenopausal women. This review was conducted to collect data from the available literature on RLX for the management of postmenopausal women suffering from RA.</p> </sec> <sec><title style='display:none'>Method</title> <p>All studies published up to 2019 were searched in four databases, including Google Scholar, PubMed, Scopus, and Medline. All articles were searched using several keywords, including “Raloxifene” or “Evista” in combination with “Rheumatoid Arthritis” or “Autoimmunity”. Finally, six studies were selected for the review analysis of this study. In all studies, 60 mg/day RLX was administered for postmenopausal subjects. The majority of the studies showed that the use of RLX was effective in postmenopausal women who underwent corticosteroid therapy. No severe complications were reported after RLX therapy in patients with RA.</p> </sec> <sec><title style='display:none'>Result</title> <p>Based on the obtained results, RLX is a selective estrogen receptor modulator that its short-term anti-arthritic effects are proven in the treatment of postmenopausal osteoporosis. It was well tolerated without serious adverse events.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>It seems that RLX is a promising treatment candidate in postmenopausal RA due to its anti-arthritic and anti-osteoporotic effects and based on the outcomes of experimental postmenopausal arthritis in animal and human studies.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00032023-09-30T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0016<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Background</title> <p>The family of calcium-activated chloride channels, TMEM16, plays a significant role in contributing to the pathogenesis of airway inflammatory diseases. Targeting these ion channels and aiming to modulate them may provide an interesting new approach to the therapy of these potentially fatal diseases.</p> </sec> <sec><title style='display:none'>Methods</title> <p>We tested this hypothesis in both healthy and ovalbumin (OVA)-sensitized male Dunkin-Hartley guinea pigs. The ion channel activity was modulated by TMEM16A-nonselective (benzbromarone) and TMEM16A-selective blockers (CaCCinh-A01). <italic>In vivo</italic> airway reactivity, induced by histamine and methacholine, was expressed as specific airway resistance (sRaw) values. The number of citric acid-induced coughs was counted using a double-chambered body plethysmograph, and the frequency of ciliary beating (CBF) was assessed <italic>in vitro</italic> by brushing method. For comparison, salbutamol and codeine were tested under the same conditions.</p> </sec> <sec><title style='display:none'>Results</title> <p>The results showed significant differences in the responses of unsensitized and sensitized airways to both TMEM16 blockers administered. CaCCinh-A01 and benzbromarone significantly reduced the number of cough efforts in the group of OVA-sensitized guinea pigs. Significant improvement in sRaw values could be observed in OVA-sensitized TMEM16 blocker–treated animals compared to salbutamol when challenged with inhalational histamine, and the outcome was similar to salbutamol when challenged with methacholine. CBF was significantly inhibited in animals sensitized to OVA treated with selective inhibition of TMEM16A.</p> </sec> <sec><title style='display:none'>Conclusions</title> <p>The results demonstrated that treatment with blockers of TMEM16 can reduce both cough effort and sRaw, and the difference between TMEM16A-selective and TMEM16A-nonselective blocking is only negligibly in favor of CaCCinh-A01. It is also worthwhile to note the impairment of CBF in OVA-sensitized animals treated with CaCCinh-A01.</p> </sec> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00162023-09-30T00:00:00.000+00:00https://sciendo.com/article/10.2478/afpuc-2023-0020<abstract> <title style='display:none'>Abstract</title> <p>There are several approaches for the formulation of abuse-deterrent, tamper-resistant, or alcohol-resistant dosage forms. This work is specifically focused on the formulation of microforms and multiple unit dosage forms with the mentioned resistant features. We prepared microcapsules based on sodium alginate by Ca²⁺-induced gelation, containing caffeine as a model drug. The prepared microcapsules were dried either by hot air or freeze-dried and the resistance in an alcoholic environment and the resistance against mechanical stress were observed. Subsequently, swelling studies were conducted to predict the behavior of prepared microcapsules during dissolution testing. Differences in the behavior of microcapsules during dissolution testing were strongly related to the different abilities of Ca²⁺-alginate microcapsules to swell in an acidic and alkaline environment. Alginate microcapsules exhibited gastro-resistant properties due to excellent swelling in an alkaline environment and poor swelling in a gastric environment. The addition of ethanol did not influence the swelling behavior of alginate microcapsules in the gastric fluid; rather, it showed the opposite effect, where swelling was slightly suppressed. Therefore, we conclude that alginate microcapsules are alcohol resistant. Also, they showed high mechanical strength, and therefore, grinding the microcapsules into a powder was impossible.</p> </abstract>ARTICLEtruehttps://sciendo.com/article/10.2478/afpuc-2023-00202023-09-15T00:00:00.000+00:00en-us-1