Journal Description
Scientia Pharmaceutica
Scientia Pharmaceutica
is an international, peer-reviewed, open access journal related to the pharmaceutical sciences. The journal is owned by the Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG) and is published quarterly online by MDPI and in print by the Austrian Pharmacists' Publishing House (Österreichischer Apothekerverlag).
- Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
- High Visibility: indexed within Scopus, ESCI (Web of Science), Embase, CAPlus / SciFinder, and other databases.
- Journal Rank: CiteScore - Q2 (Pharmaceutical Science)
- Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 22.7 days after submission; acceptance to publication is undertaken in 6.9 days (median values for papers published in this journal in the second half of 2023).
- Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
Impact Factor:
2.5 (2022);
5-Year Impact Factor:
3.5 (2022)
Latest Articles
Semaglutide as a Possible Calmodulin Binder: Ligand-Based Computational Analyses and Relevance to Its Associated Reward and Appetitive Behaviour Actions
Sci. Pharm. 2024, 92(2), 17; https://doi.org/10.3390/scipharm92020017 - 22 Mar 2024
Abstract
Semaglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, has gained considerable attention as a therapeutic agent for type 2 diabetes mellitus and obesity. Despite its clinical success, the precise mechanisms underlying its pharmacological effects remain incompletely understood. In this study, we employed ligand-based drug
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Semaglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, has gained considerable attention as a therapeutic agent for type 2 diabetes mellitus and obesity. Despite its clinical success, the precise mechanisms underlying its pharmacological effects remain incompletely understood. In this study, we employed ligand-based drug design strategies to investigate potential off-target interactions of semaglutide. Through a comprehensive in silico screening of semaglutide’s structural properties against a diverse panel of proteins, we have identified calmodulin (CaM) as a putative novel target of semaglutide. Molecular docking simulations revealed a strong interaction between semaglutide and CaM, characterized by favourable binding energies and a stable binding pose. Further molecular dynamics simulations confirmed the stability of the semaglutide–CaM complex, emphasizing the potential for a physiologically relevant interaction. In conclusion, our ligand-based drug design approach has uncovered calmodulin as a potential novel target of semaglutide. This discovery sheds light on the complex pharmacological profile of semaglutide and offers a promising direction for further research into the development of innovative therapeutic strategies for metabolic disorders. The CaM, and especially so the CaMKII, system is central in the experience of both drug- and natural-related reward. It is here hypothesized that, due to semaglutide binding, the reward pathway-based calmodulin system may be activated, and/or differently regulated. This may result in the positive semaglutide action on appetitive behaviour. Further studies are required to confirm these findings.
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(This article belongs to the Topic Bioinformatics in Drug Design and Discovery, 2nd Volume)
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Complementary Practices in Pharmacy and Their Relation to Glaucoma—Classification, Definitions, and Limitations
by
Tibor Rák and Adrienne Csutak
Sci. Pharm. 2024, 92(1), 16; https://doi.org/10.3390/scipharm92010016 - 14 Mar 2024
Abstract
Background: Traditional and evidence-based medicines, as seen depicted throughout human history, reportedly first begin with the application of medicinal plants, animal products, or inorganic minerals as a basic framework towards effectively engineering the prototypes generally aligned to pharmaceuticals and medical nutrition. The growing
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Background: Traditional and evidence-based medicines, as seen depicted throughout human history, reportedly first begin with the application of medicinal plants, animal products, or inorganic minerals as a basic framework towards effectively engineering the prototypes generally aligned to pharmaceuticals and medical nutrition. The growing global trend of complementary treatments for glaucoma can be explained by the intraocular pressure (IOP)-independent mechanisms of the disease and its interpretation as a progressive neurodegenerative disorder. Unfortunately, the categorical positions of the major fields of applied popular complementary therapies and their relation to glaucoma are consistently neglected. Methods: In consideration of bibliographic resources, the most well-known online scientific databases were searched. Conclusion: The rising popularity and the trends of products coming onto the market cannot escape the attention of pharmacists and ophthalmologists, as their patients suffering from eye diseases are also increasingly looking for such medicinal products. Most of them still lack knowledge of the appropriate evidence and side effect profiles. Our proposed systematic charts demonstrate the position of each mainstream complementary therapy throughout the applied medical sciences and are distinctively unique; we could not find any similar relevant illustration or resource among the published international literature.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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Pharmacokinetic Simulation Study: Exploring the Impact of Clinical Parameters on Lamotrigine for Different Patient Populations with Implications for Liver Function Assessment and Therapeutic Drug Monitoring
by
Bárbara Costa, Isabel Silva, José Carlos Oliveira, Henrique Reguengo and Nuno Vale
Sci. Pharm. 2024, 92(1), 15; https://doi.org/10.3390/scipharm92010015 - 28 Feb 2024
Abstract
Lamotrigine, widely used for managing epilepsy and bipolar disorder, carries potential side effects, including severe anticonvulsant hypersensitivity syndrome (AHS) or drug rash with eosinophilia and systemic symptoms (DRESS), which may lead to hepatotoxicity. Patients with Type 2 Diabetes (TD2) and Non-Alcoholic Fatty Liver
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Lamotrigine, widely used for managing epilepsy and bipolar disorder, carries potential side effects, including severe anticonvulsant hypersensitivity syndrome (AHS) or drug rash with eosinophilia and systemic symptoms (DRESS), which may lead to hepatotoxicity. Patients with Type 2 Diabetes (TD2) and Non-Alcoholic Fatty Liver Disease (NAFLD) are identified as more susceptible to these adverse reactions. This exploratory analysis aims to identify clinical parameters influencing lamotrigine pharmacokinetics across diverse populations, shedding light on toxicity and therapeutic drug monitoring (TDM) considerations. Starting with a retrospective analysis of 41 lamotrigine-treated patients at Hospital Santo António reveals changes or deviations from normal levels in various blood parameters and significant correlations between these parameters. Serum level changes, including creatinine, albumin, gamma-glutamyl transferase, total bilirubin, and Vitamin B12, are observed, with strong negative correlations between Vitamin B12 and creatinine. Then, we used GastroPlus and DILIsym to explore the impact of clinical parameters on lamotrigine for different patient populations. We constructed a Physiologically Based Pharmacokinetic (PBPK) model for lamotrigine in GastroPlus, based on ADMET predictions and data from the literature, to simulate the pharmacokinetic variability of lamotrigine in different populations, and we visualized the impact of increasing lamotrigine dose on its plasma concentration–time profiles (200 mg, 400 mg, 600 mg, 1200 mg) and reduced bioavailability. At higher doses, it is possible that the saturation of metabolic pathways leads to the formation of toxic metabolites or intermediates. These metabolites may exert inhibitory effects on drug-metabolizing enzymes or disrupt normal physiological processes, thereby impeding the drug’s clearance and potentially lowering its bioavailability. In DILIsym, we investigated lamotrigine’s DILI potential for individuals with diabetes and NAFLD. The results demonstrated an increased risk, emphasizing the need for careful monitoring. This study underscores the importance of understanding lamotrigine’s pharmacokinetics for tailored treatment decisions, improved outcomes, and minimized adverse reactions.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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New Carriers for Bioadhesive Gastroretentive Drug Delivery Systems Based on Eudragit® EPO/Eudragit® L100 Interpolyelectrolyte Complexes
by
Daria S. Gordeeva, Aleksandra V. Sitenkova (Bukhovets) and Rouslan I. Moustafine
Sci. Pharm. 2024, 92(1), 14; https://doi.org/10.3390/scipharm92010014 - 22 Feb 2024
Abstract
The aim of this study was the analysis of interpolyelectrolyte complexes (IPECs) based on Eudragit® EPO and Eudragit® L100 as prospective carriers for gastroretentive drug delivery systems (GRDDS) using two model drugs: metronidazole (MZ) and acyclovir (ACR). Eudragit® EPO/L100 IPECs
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The aim of this study was the analysis of interpolyelectrolyte complexes (IPECs) based on Eudragit® EPO and Eudragit® L100 as prospective carriers for gastroretentive drug delivery systems (GRDDS) using two model drugs: metronidazole (MZ) and acyclovir (ACR). Eudragit® EPO/L100 IPECs with different pH concentrations were characterized by different degrees of swelling in mimicking fasted stomach medium (0.1 M HCl) and saved their shape for 6 h. The microenvironmental changes in IPEC structures in acidic medium were investigated using FT-IR spectroscopy, thermal and elemental analysis. IPEC samples showed bioadhesive properties that were not significantly different from the positive control (Carbopol) in the test with the mucin compacts. The release rate of metronidazole (class I BCS) from IPEC matrices increased with the increasing degree of swelling. IPEC 1 provided 49.62 ± 6.20% and IPEC 2 reached 87.69 ± 5.15% of metronidazole release after 6 h in mimicking fasted stomach medium (0.1 M HCl). The total amount of released acyclovir (class III BCS) from IPEC 1 was 25.76 ± 5.67% and from IPEC 2 was 21.48 ± 5.00%. Release of both drugs was controlled by relaxation of polymeric chains in matrices according to the Peppas–Sahlin model. According to the received results, investigated interpolymer complexes are prospects for further evaluation as carriers for gastroretentive bioadhesive systems.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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Protective Effect of Panicum dichotomiflorum in a Rodent Model of Testosterone-Induced Benign Prostatic Hyperplasia
by
Eun Bok Baek, Eun-Ju Hong, Jung-Hee Kim, Min Kim, Jongmin Ahn and Hyo-Jung Kwun
Sci. Pharm. 2024, 92(1), 13; https://doi.org/10.3390/scipharm92010013 - 19 Feb 2024
Abstract
Benign prostatic hyperplasia (BPH) is a common disease in aging men. Panicum dichotomiflorum (PD) is an annual grass species of Poaceae that is distributed worldwide. The present study examined whether PD has a protective effect against BPH. BPH was generated in rats by
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Benign prostatic hyperplasia (BPH) is a common disease in aging men. Panicum dichotomiflorum (PD) is an annual grass species of Poaceae that is distributed worldwide. The present study examined whether PD has a protective effect against BPH. BPH was generated in rats by daily subcutaneous administration of testosterone for four weeks. During this period, the rats were also given daily oral gavages of an extract of PD (150 mg/kg). After the final treatment, all animals were euthanized and their prostates were collected and weighed. In BPH model rats, the prostate weight and levels of dihydrotestosterone (DHT) and 5α-reductase expression were inhibited following treatment with PD extract. Testosterone-induced increases in prostate gland epithelial thickness and expression of cyclin D1 and proliferating cell nuclear antigen (PCNA) were markedly suppressed in PD-treated rats, whereas cleaved caspase-3 levels were increased. PD administration also decreased the expression of transforming growth factor (TGF)-β and vascular endothelial growth factor (VEGF), the phosphorylation of Akt, and inflammatory cytokines levels. Taken together, these results show that PD extract protects against testosterone-induced BPH progression by alleviating prostate cell growth and reducing levels of growth factors and inflammatory cytokines, indicating that PD extract may have potential in protecting against BPH.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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Attenuation of Pulmonary Damage Associated with COPD in a Cadmium-Exposed Model Due to the Administration of a siRNA Targeting PAD4
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Sergio Adrian Ocampo-Ortega, Sandra Edith Cabrera-Becerra, Vivany Maydel Sierra-Sanchez, Vanessa Giselle García-Rubio, Citlali Margarita Blancas-Napoles, Rodrigo Romero-Nava, Fengyang Huang, Enrique Hong, Asdrúbal Aguilera-Méndez and Santiago Villafaña
Sci. Pharm. 2024, 92(1), 12; https://doi.org/10.3390/scipharm92010012 - 04 Feb 2024
Abstract
Chronic obstructive pulmonary disease (COPD), characterised by persistent airflow limitation during breathing, is considered to be the third leading cause of death worldwide. Among the mechanisms involved in this pathology is the excessive generation of neutrophil extracellular traps (NETs), which can induce an
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Chronic obstructive pulmonary disease (COPD), characterised by persistent airflow limitation during breathing, is considered to be the third leading cause of death worldwide. Among the mechanisms involved in this pathology is the excessive generation of neutrophil extracellular traps (NETs), which can induce an unwanted inflammatory response. These traps have been reported to be generated by the enzyme peptidyl arginine deiminase 4 (PAD4). The aim of this work is therefore to evaluate the effect of the administration of a siRNA targeting PAD4 on lung damage in a COPD animal model. Wistar rats weighing 300–350 g were administered cadmium chloride (5 mg/kg i.p.) every 24 h. Then, following one week of the administration of cadmium chloride, the PAD4-targeted siRNA was administered, and at the second week, lung function was measured, as were lung and heart weights, as well as PAD4 expression by RT-PCR. Our results showed that cadmium administration generated a COPD model, which increased PAD4 expression and decreased lung and heart weights and respiratory function. SiRNA administration partially reversed the changes associated with the COPD model. In conclusion, our results suggest that administration of an siRNA targeting PAD4 could improve respiratory function by decreasing lung and heart damage.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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The Potential of Incorporating a Pharmacist-Only Medicine Category in Poland
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Tomasz Zaprutko, Józefina Sprawka, Barbara Maciuszek-Bartkowska, Piotr Ratajczak, Dorota Kopciuch, Anna Paczkowska and Krzysztof Kus
Sci. Pharm. 2024, 92(1), 11; https://doi.org/10.3390/scipharm92010011 - 04 Feb 2024
Abstract
Pharmacists play an important role, being increasingly focused on patient care and pharmaceutical services. This trend is also noticeable in Poland. Thus, we aimed to study the opinions of Polish pharmacists to determine the potential for introducing a new category of pharmacist-only medicines
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Pharmacists play an important role, being increasingly focused on patient care and pharmaceutical services. This trend is also noticeable in Poland. Thus, we aimed to study the opinions of Polish pharmacists to determine the potential for introducing a new category of pharmacist-only medicines (POMs). This study was conducted during the COVID-19 pandemic. Hence, the survey (anonymous questionnaire consisting of 10 questions addressed to pharmacists) was only available in electronic form. A total of 500 correctly completed surveys were collected and subjected to further analysis. The vast majority of pharmacists (91.8%) revealed a willingness to expand their professional rights and 88% stated that the POMs implementation would be important. As a substance that should function as a POM instead of an OTC medicine, respondents most often indicated ketoprofen, sildenafil, and mometasone, accounting for 26.2%, 24.8%, and 24.4% of responses, respectively. In terms of funding pharmaceutical services, 54.2% of respondents indicated that costs should be covered partially by the patient and the payer. There is a clear need for the incorporation of the POM category in Poland. Polish pharmacists are anticipating the development of pharmaceutical services which should be partly covered by patients and payers.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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Mucoadhesive Vaginal Tablets Containing Metronidazole: Screening of Optimal Natural Polymer in the Composition
by
Kamila Bartoníková, Miroslava Špaglová, Martina Papadakos, Michal Hanko and Oliver Macho
Sci. Pharm. 2024, 92(1), 10; https://doi.org/10.3390/scipharm92010010 - 26 Jan 2024
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(1) Background: The study aimed to compare the impact of various natural polymers–sodium alginate, acacia gum, carrageenan, guar gum, xanthan gum, and tragacanth on the formulation and the physical properties of mucoadhesive vaginal tablets containing metronidazole (167 mg/g). (2) Methods: The quality of
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(1) Background: The study aimed to compare the impact of various natural polymers–sodium alginate, acacia gum, carrageenan, guar gum, xanthan gum, and tragacanth on the formulation and the physical properties of mucoadhesive vaginal tablets containing metronidazole (167 mg/g). (2) Methods: The quality of the tablets prepared by direct compression was evaluated by pharmacopoeia tests (uniformity of mass, resistance to crushing, friability). Mucoadhesion of the tablets was characterized by swelling capacity and mucoadhesive strength, i.e., the force required to detach the tablet from the rabbit mucosa. In vitro drug release was performed by a modified dissolution method in paddle apparatus containing the simulated vaginal fluid (pH 4.5). Scanning electron microscopy observed morphological changes on the swollen tablets’ surface. (3) Results: Pharmacopoeia tests have shown that all prepared tablets met the requirements on quality. The highest mucoadhesive strength was noted in tablets containing guar and xanthan gum. The highest swelling capacity was possessed by tablets containing carrageenan. (4) Conclusions: Summarizing all tests’ results, sodium alginate can be considered the most suitable natural polymer in tablet formulation. The combination of polymers providing higher mucoadhesiveness and at the same time a prolonged release, e.g., xanthan or guar, together with sodium alginate, could also be of interest.
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Effect of Zoapatle (Montanoa tomentosa) on Inflammatory Markers in a Murine Model of Ventricular Hypertrophy
by
Carlos Enrique López-Luna, Cruz Vargas-De-León, Rocio Alejandra Gutiérrez-Rojas, Karla Aidee Aguayo-Cerón, Claudia Camelia Calzada-Mendoza, Fengyang Huang, Rodrigo Romero-Nava and Maria Esther Ocharan-Hernandez
Sci. Pharm. 2024, 92(1), 9; https://doi.org/10.3390/scipharm92010009 - 24 Jan 2024
Abstract
Zoapatle, a native plant utilized for centuries in traditional Mexican medicine, is abundantly found in Mesoamerica and northern South America. Pleiotropic effects of this genus have been recognized, primarily inducing alterations in smooth muscle contractility in animal models. The aim of this study
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Zoapatle, a native plant utilized for centuries in traditional Mexican medicine, is abundantly found in Mesoamerica and northern South America. Pleiotropic effects of this genus have been recognized, primarily inducing alterations in smooth muscle contractility in animal models. The aim of this study was to evaluate the effect of Zoapatle on the hypertrophy index and the gene expression of TNF-α, IL-1β, NF-κB, STAT5, and the PRLR in the brain, left ventricle, and renal cortex of rats with isoproterenol-induced cardiac hypertrophy. Three groups were studied, the control group (n = 4), hypertrophy group (n = 4) and hypertrophy group treated with Zoapatle (n = 4). A ventricular hypertrophy model was developed with 150 mg/kg/day of isoproterenol intraperitoneally administered over two days with a 24 h interval between applications. Zoapatle was administered for 28 consecutive days (25 mg/kg). Gene expression was determined with RT-qPCR. Subsequently, a principal component analysis (PCA) was performed using the RNA expression variables. A notably reduced left ventricle mass index was observed in the Zoapatle group. Additionally, Zoapatle administration in cardiac hypertrophy demonstrated a significant decrease in the gene expression of TNF-α, IL-1B, STAT 5, and the PRLR. TNF-α and the transcription factor STAT5 exhibited a similar trend in both the left ventricle and renal cortex, suggesting a correlation with the inflammatory state in these tissues due to ventricular hypertrophy. The findings suggest that Zoapatle reverses the hypertrophy index in a hypertrophy model, concurrently reducing several proinflammatory mediators associated with the hypertrophy index.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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A Thermal-Analysis-Technique-Based Mechanistic Approach toward the Release of Omeprazole from Solid Dosage Forms
by
Georgios Agapakis, Angeliki Siamidi, Stefanos Kikionis, Marilena Vlachou and Natassa Pippa
Sci. Pharm. 2024, 92(1), 8; https://doi.org/10.3390/scipharm92010008 - 16 Jan 2024
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The design, development, and release kinetics of omeprazole (OME) from solid dosage forms have been investigated. These formulations were examined for their resilience in pH = 4.5 buffer solutions and their rate of disintegration in a small-intestine-like environment (pH = 6.8). The results
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The design, development, and release kinetics of omeprazole (OME) from solid dosage forms have been investigated. These formulations were examined for their resilience in pH = 4.5 buffer solutions and their rate of disintegration in a small-intestine-like environment (pH = 6.8). The results were compared with those of the well-known brand product Losec®, where its use is accompanied by numerous benefits but drawbacks as well. Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) tests were conducted in order to examine the release kinetics of the various dosage forms and provide explanations based on the interactions between the excipients and the active substance.
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Open AccessReview
The Risks of “Getting High” on Over-the-Counter Drugs during Pregnancy
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Bianca-Eugenia Ősz, Ruxandra Ștefănescu, Andreea Sălcudean, George Jîtcă and Camil-Eugen Vari
Sci. Pharm. 2024, 92(1), 7; https://doi.org/10.3390/scipharm92010007 - 09 Jan 2024
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Easy access to over-the-counter (OTC) drugs makes it possible to procure active substances that normally used in therapeutic doses do not raise health problems. The use of high doses of OTC drugs containing codeine, loperamide, pseudoephedrine, diphenhydramine or dimenhydrinate, as well as the
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Easy access to over-the-counter (OTC) drugs makes it possible to procure active substances that normally used in therapeutic doses do not raise health problems. The use of high doses of OTC drugs containing codeine, loperamide, pseudoephedrine, diphenhydramine or dimenhydrinate, as well as the use of benzidamine systemically raises concerns regarding the increase in units sold. These drugs are used for recreational or euphorizing purposes, including by young women of childbearing age, psychoactive substance users representing a risk group in terms of the possibility of an unplanned pregnancy. Abusive consumption of OTC products during pregnancy is harmful, with consequences for both fetal and late development that can occur in the infant. This literature review presents the risks (teratogenicity, fetal toxicity, neonatal abstinence syndrome, etc.) associated with the use of potentially psychoactive OTC drugs to emphasize the importance of re-evaluating OTC classification and dispensing.
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The Extraction of Bioactive Agents from Calophyllum inophyllum L., and Their Pharmacological Properties
by
Sahena Ferdosh
Sci. Pharm. 2024, 92(1), 6; https://doi.org/10.3390/scipharm92010006 - 09 Jan 2024
Abstract
Calophyllum inophyllum L. has been used for many generations by Pacific Islanders because of its numerous health and aesthetic advantages. The leaves, stems, roots, fruits, flowers, and seeds of this plant contain significant phytochemicals, including flavonoids, coumarins, fatty acids, and xanthones, which have
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Calophyllum inophyllum L. has been used for many generations by Pacific Islanders because of its numerous health and aesthetic advantages. The leaves, stems, roots, fruits, flowers, and seeds of this plant contain significant phytochemicals, including flavonoids, coumarins, fatty acids, and xanthones, which have been shown to have wound healing, analgesic, anti-inflammatory, antiaging, anti-arthritic, anti-cancer, anti-proliferative, anti-diabetic, anti-microbial, and anti-HIV effects. The chemical profiles and bioactive potential may vary due to different extraction techniques, plant parts, and geographical origins. Extraction is the essential first step in the analysis of bioactive compounds that leads to further separation, identification, and characterization. Conventional methods like maceration, Soxhlet, and percolation are often used to extract bioactive compounds from C. inophyllum. However, little study has been carried out on non-conventional methods such as pressured liquid extraction, supercritical fluid extraction (SFE), and ultrasound-assisted extraction. The SFE method can be used to extract bioactive compounds from C. inophyllum to retain their pharmacological properties for application in pharmaceutical and cosmetic products.
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Diastereomers of Spheroidal Form and Commercially Available Taxifolin Samples
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Roman P. Terekhov, Evgeny S. Melnikov, Ilya D. Nikitin, Margarita A. Tokareva, Tatyana A. Rodina, Anastasiya D. Savina, Denis I. Pankov, Anastasiya K. Zhevlakova, Vladimir L. Beloborodov and Irina A. Selivanova
Sci. Pharm. 2024, 92(1), 5; https://doi.org/10.3390/scipharm92010005 - 03 Jan 2024
Abstract
Taxifolin is a natural polyphenol belonging to the class of flavonoids. The structure of this compound is characterized by the presence of two chiral centers. The spheroidal form of taxifolin (TAXs) has emerged as a promising modification due to enhanced solubility, higher safety
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Taxifolin is a natural polyphenol belonging to the class of flavonoids. The structure of this compound is characterized by the presence of two chiral centers. The spheroidal form of taxifolin (TAXs) has emerged as a promising modification due to enhanced solubility, higher safety profile, and long-term release from solid dosage forms. The study’s objective was to assess the diastereomeric content in TAXs and industrially produced samples of taxifolin. Considering the difference in the physico-chemical properties of diastereomers and based on the literature data, we developed a qualitative HPLC method. The chromatograms were recorded using a diode array detector at 290 nm and a mass spectrometer operated in negative ionization mode. Our data suggest that a biphenyl column and gradient elution using 0.1% formic acid in water and 0.2% formic acid in methanol, with the organic phase gradient from 7% to 21% and a flow rate of 0.65 mL/min for 15 min at 60 °C, provides the best conditions for the separation of taxifolin diastereomers. This method was validated for quantitative analysis. We discovered that the cis-isomer was present in all the analyzed samples, with its quantity ranging from 0.8% to 9.5%. TAXs can be considered a sample enriched with diastereomers.
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Assessing the Influence of a Rotating Magnetic Field on Ibuprofen Permeability from Diverse Pharmaceutical Formulations
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Anna Nowak, Paula Ossowicz-Rupniewska, Maciej Konopacki, Anna Muzykiewicz-Szymańska, Łukasz Kucharski and Rafał Rakoczy
Sci. Pharm. 2024, 92(1), 4; https://doi.org/10.3390/scipharm92010004 - 29 Dec 2023
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This study introduces a novel approach for enhancing the transdermal permeability of ibuprofen through the skin by utilising a rotating magnetic field (RMF). The core objective is to systematically evaluate the influence of a 50 Hz RMF on ibuprofen’s skin permeability across various
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This study introduces a novel approach for enhancing the transdermal permeability of ibuprofen through the skin by utilising a rotating magnetic field (RMF). The core objective is to systematically evaluate the influence of a 50 Hz RMF on ibuprofen’s skin permeability across various formulation types, each employing distinct physical forms and excipients. The experimental setup involved Franz cells with skin as the membrane, exposed to a 50 Hz RMF in conjunction with specific formulations. Subsequent comprehensive analysis revealed a notable increase in the transdermal transport of ibuprofen, irrespective of the formulation employed. Notably, the differences in the initial 30 min of permeation were particularly pronounced. Crucially, this investigation establishes that the application of a 50 Hz RMF resulted in a remarkable over-sevenfold increase in ibuprofen permeability compared to the control group without RMF exposure. It is noteworthy that in all semi-solid pharmaceutical formulations tested, RMF effectively reduced the delay time to zero, underscoring the efficiency of RMF in overcoming barriers to transdermal drug delivery. This research positions the application of RMF as a highly promising and innovative technology, significantly enhancing the transdermal penetration of anti-inflammatory and analgesic drugs through the skin. The demonstrated effectiveness of RMF across diverse formulations suggests its potential in transdermal drug delivery, offering a novel and efficient strategy for improving therapeutic outcomes in the administration of ibuprofen and potentially other pharmaceutical agents.
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Inhibitory Effect of Mistletoe Ointment on DNCB-Induced Atopic Dermatitis in BALB/c Mice
by
Chang-Eui Hong and Su-Yun Lyu
Sci. Pharm. 2024, 92(1), 3; https://doi.org/10.3390/scipharm92010003 - 29 Dec 2023
Abstract
Atopic dermatitis (AD) is increasingly prevalent globally. However, the frequent and prolonged use of corticosteroids, which are commonly employed for AD treatment, carries potential side effects. Korean mistletoe (Viscum album L. var. coloratum), a perennial parasitic plant, has demonstrated various biological
[...] Read more.
Atopic dermatitis (AD) is increasingly prevalent globally. However, the frequent and prolonged use of corticosteroids, which are commonly employed for AD treatment, carries potential side effects. Korean mistletoe (Viscum album L. var. coloratum), a perennial parasitic plant, has demonstrated various biological effects. In this study, we conducted in vivo investigations to determine whether Korean mistletoe possesses anti-inflammatory effects that play pivotal roles in regulating the pathological mechanisms of AD. BALB/c mice with AD-like skin lesions induced by 2,4-dinitrochlorobenzene (DNCB) were utilized to explore the therapeutic effects of 1% and 2% Korean mistletoe extract (KME) ointments. The KME ointment was topically applied to the dorsal surface of the BALB/c mice, and they were categorized into four distinct groups: normal, DNCB-induced, DNCB-induced with 1% KME ointment, and DNCB-induced with 2% KME ointment. Each assessment parameter employed to evaluate the curative impact of the KME ointment displayed improvement with the application of the 1% KME ointment. While the effects observed were less pronounced than those of the 1% KME ointment, the overall therapeutic outcomes were also evident with the utilization of the 2% KME ointment. The results suggest the potential of Korean mistletoe as a viable therapeutic agent for AD. Further investigations are warranted to elucidate the underlying mechanisms of action.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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Polymorphisms in Drug Transporter and Metabolism Genes Associated with Resistance to Imatinib in Chronic Myeloid Leukemia: A Systematic Review and Meta-Analysis
by
Ana Marcela Arrieta Gómez, María Antonia Díaz-Mendoza, Yesit Bello Lemus, Grethel León-Mejía and Martha Lucia Ruiz Benitez
Sci. Pharm. 2024, 92(1), 2; https://doi.org/10.3390/scipharm92010002 - 25 Dec 2023
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The aim of this study was to establish the relationship between different polymorphisms in drug transporter and metabolizer genes and resistance to imatinib in chronic myeloid leukemia (CML). For this purpose, an exhaustive search was carried out in the Scopus, Web of Science,
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The aim of this study was to establish the relationship between different polymorphisms in drug transporter and metabolizer genes and resistance to imatinib in chronic myeloid leukemia (CML). For this purpose, an exhaustive search was carried out in the Scopus, Web of Science, and PubMed databases using different combinations of keywords with different inclusion and exclusion criteria. The meta-analysis included nine studies that met the established criteria. The results of the study showed that the polymorphic variants AG and GG of CYP3A5*3 are associated with response to treatment, presenting a significantly lower risk with resistance to imatinib. Likewise, the variants T1236C and G2677T/A of the ABCB1 gene show a significant association with treatment efficacy. In addition, the genetic polymorphism 1236T, homozygous CC of the MDR1 gene, significantly influences the increased risk of cytogenetic relapse and the polymorphic variant 361G>A GA of the SLCO1A2 gene significantly affects the complete molecular response.
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Open AccessArticle
In Silico Activity Prediction and Docking Studies of the Binding Mechanisms of Levofloxacin Structure Derivatives to Active Receptor Sites of Bacterial Type IIA Topoisomerases
by
Elena V. Uspenskaya, Vasilisa A. Sukhanova, Ekaterina S. Kuzmina, Tatyana V. Pleteneva, Olga V. Levitskaya, Timur M. Garaev and Anton V. Syroeshkin
Sci. Pharm. 2024, 92(1), 1; https://doi.org/10.3390/scipharm92010001 - 20 Dec 2023
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The need for new antimicrobial agents (AntAg) is driven by the persistent antibiotic resistance in microorganisms, as well as the increasing frequency of pandemics. Due to the deficiency of AntAg, research aimed at developing speedy approaches to find new drug candidates is relevant.
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The need for new antimicrobial agents (AntAg) is driven by the persistent antibiotic resistance in microorganisms, as well as the increasing frequency of pandemics. Due to the deficiency of AntAg, research aimed at developing speedy approaches to find new drug candidates is relevant. This study aims to conduct an in silico study of the biological activity spectrum as well as the molecular binding mechanisms of four structurally different forms of levofloxacin (Lvf) with bacterial topoisomerases targets of type IIA (DNA gyrase and topoisomerase IV) to enable the development of drugs with an improved characterization of the safety profile. To achieve this goal, a number of software products were used, such as ChemicPen v. 2.6, PyMol 2.5, Avogadro 1.2.0, PASS, AutoDockTools 1.5.7 with the new generation software Autodock Vina. These software products are the first to be made available for visualization of clusters with determination of ligand-receptor pair binding affinity, as well as clustering coordinates and proposed mechanisms of action. One of the real structures of Lvf, a decarboxylated derivative, was obtained with tribochemical (TrbCh) exposure. The action spectrum of molecular ligands is described based on a Bayesian probability activity prediction model (PASS software Version 2.0). Predicted and real (PMS and RMS) molecular structures of Lvf, with decreasing levels of structural complexity, were translated into descriptors via Wiener (W), Balaban (Vs), Detour (Ip), and Electropy € indices. The 2D «structure-activity» diagrams were used to differentiate closely related structures of levofloxacin. PMS and RMS were visualized as 3D models of the ligand-receptor complexes. The contact regions of RMS and PMS with key amino acid residues—SER-79, DT-15, DG-1, DA-1—were demonstrated. The intra- and inter-molecular binding sites, data on free energy (affinity values, kcal/mol), the binding constant Kb (M−1), and the number of clusters are presented. The research results obtained from the presented in silico approach to explore the spectrum of action find quantitative “structure-activity” correlations, and predict molecular mechanisms may be of applied interest for directed drug discovery.
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Open AccessArticle
STAT3 Inhibitory Activities of Lignans Isolated from the Stems of Lindera obtusiloba Blume
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Eun-Jae Park, Hee Ju Lim, Hyung Jin Lim, Bong-Sik Yun, Soyoung Lee, Seung-Jae Lee and Seung Woong Lee
Sci. Pharm. 2023, 91(4), 56; https://doi.org/10.3390/scipharm91040056 - 08 Dec 2023
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Lindera obtusiloba Blume has several activities, such as anti-inflammatory, anti-allergic, anti-tumor, anti-wrinkle, and antioxidant activities. Interleukin-6 (IL-6) is a classic pro-inflammatory cytokine that is associated with various functions, such as proliferation, invasion, inflammatory responses and functions within antioxidant defense systems. In this study,
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Lindera obtusiloba Blume has several activities, such as anti-inflammatory, anti-allergic, anti-tumor, anti-wrinkle, and antioxidant activities. Interleukin-6 (IL-6) is a classic pro-inflammatory cytokine that is associated with various functions, such as proliferation, invasion, inflammatory responses and functions within antioxidant defense systems. In this study, we investigated IL-6-induced STAT3 activation of lignan compounds isolated from L. obtusiloba. The structures of the isolated compounds were elucidated via spectroscopic nuclear magnetic resonance (NMR) and electrospray ionization mass spectrometry (ESI-MS). As a result, seven lignans were identified from L. obtusiloba. All the isolated compounds (1–7) were evaluated for their IL-6-induced STAT3 inhibitory effects in Hep3B cells using a luciferase reporter assay. Of the isolates, compounds 1 and 5 showed inhibitory effects against IL-6-stimulated STAT3 activation. Furthermore, the mRNA expression levels of inflammation-related genes such as CRP, IL-1b, and SOCS3 were significantly reduced by exposure to compounds 1 and 5. The protein levels of p-STAT3 and p-JAK2 in IL-6-induced U266 cells were regulated in the presence of lignans derived from Lindera obtusiloba by Western blot assay. Based on the results, this study of L. obtusiloba demonstrates that the species has promise as a bioactive candidate for the treatment of IL-6-induced STAT3-related disease.
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Open AccessArticle
Analysis of Beneficial Effects of Flavonoids in Patients with Atherosclerosis Risk on Blood Pressure or Cholesterol during Random Controlled Trials: A Systematic Review and Meta-Analysis
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Rosa Edith Grijalva-Guiza, Thais Lucía Grijalva-Montano, Mariana Cuautle, Enrique Quiroga-González, Luis Ricardo Hernández, Alicia Ortega Aguilar and Aura Matilde Jiménez-Garduño
Sci. Pharm. 2023, 91(4), 55; https://doi.org/10.3390/scipharm91040055 - 22 Nov 2023
Abstract
Flavonoids are plant-secondary metabolites with cardiovascular protective properties. Few studies have examined specific flavonoid classes or pure flavonoids concerning some common cardiovascular risks. To obtain information in a systematic review to analyze in a meta-analysis, data were recovered regarding flavonoid intake in random
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Flavonoids are plant-secondary metabolites with cardiovascular protective properties. Few studies have examined specific flavonoid classes or pure flavonoids concerning some common cardiovascular risks. To obtain information in a systematic review to analyze in a meta-analysis, data were recovered regarding flavonoid intake in random controlled trials and atherosclerosis disease, related to risk factors such as blood pressure, total cholesterol (TC), and low-density lipoprotein cholesterol (LDLc). Our aim was to conduct a meta-analysis using the Scopus and PubMed databases without restrictions on the year of publication, extracting articles over the period 1–15 April 2023, searching for randomized controlled trials (RCTs) that investigated different types of flavonoids, measuring blood pressure and low-density cholesterol plasmatic concentration. This paper’s Prospero registration is CRD 42023414153. There were 19 RCTs: twelve RCTs were considered for blood pressure data analysis and fifteen RCTs for total cholesterol and LDL cholesterol data analysis. The meta-analysis showed no significant differences between placebo treatments and treatments with different flavonoids on blood pressure. However, there was a significant difference found in quantitative analysis for TC and LDLc. In conclusion, flavonoid consumption can be associated with a lower risk of LDLc and TC, and more RCTs are needed to specify the effect of more types of pure flavonoids in atherosclerotic patients.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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Open AccessArticle
Monitoring Cutaneous Leishmaniasis Lesions in Mice Undergoing Topical Miltefosine Treatment
by
Laura Fernanda Neira, Julio Cesar Mantilla and Patricia Escobar
Sci. Pharm. 2023, 91(4), 54; https://doi.org/10.3390/scipharm91040054 - 09 Nov 2023
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A study was conducted on BALB/c mice infected with Leishmania (Leishmania) amazonensis to analyse the effects of 0.5% miltefosine (MTF) hydrogel treatment on cutaneous leishmaniasis (CL) lesions. The mice were treated for 25 days topically, and lesion sizes, parasite loads, histopathology, ultrastructure, cytokines
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A study was conducted on BALB/c mice infected with Leishmania (Leishmania) amazonensis to analyse the effects of 0.5% miltefosine (MTF) hydrogel treatment on cutaneous leishmaniasis (CL) lesions. The mice were treated for 25 days topically, and lesion sizes, parasite loads, histopathology, ultrastructure, cytokines including interleukin 4 (IL-4), tumour necrosis factor alfa (TNFα), interferon gamma (IFNγ), IL-10, and vascular endothelial growth factor (VEGF) profiles were evaluated on days 0, 12, 25, and 85. After 12 days of treatment, the lesion sizes and parasite numbers decreased. By day 60 post treatment, there were no lesions and only a few parasites. At day 25, there was a temporary papillomatosis reaction, an increase in mast cells, a few giant cells, and granulomas, and a decrease in diffuse inflammatory infiltrate and parasites. Transmission electron microscopy (TEM) examination showed early ultrastructural changes, including macrophages without parasites and vacuoles containing electrodense material. At the different evaluated times, the cytokine regulation indexes (ICRs) decreased for IL-4, TNFα, and VEGF. According to the study, the 0.5% MTF hydrogel was effective and showed positive results from the early stages of usage. The MTF directly targeted parasites, downregulated the release of IL-4, TNFα, and VEGF, increased mast cell production, and induced granuloma reaction during evaluation periods.
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