Scientia Pharmaceutica

您所在的位置：网站首页 › pharmaceutic › Scientia Pharmaceutica

Scientia Pharmaceutica

2024-06-03 13:54:33| 来源: 网络整理| 查看: 265

Journals Active Journals Find a Journal Proceedings Series Topics Information For Authors For Reviewers For Editors For Librarians For Publishers For Societies For Conference Organizers Open Access Policy Institutional Open Access Program Special Issues Guidelines Editorial Process Research and Publication Ethics Article Processing Charges Awards Testimonials Author Services Initiatives Sciforum MDPI Books Preprints.org Scilit SciProfiles Encyclopedia JAMS Proceedings Series About Overview Contact Careers News Press Blog Sign In / Sign Up Notice clear Notice

You are accessing a machine-readable page. In order to be human-readable, please install an RSS reader.

Continue Cancel clear

All articles published by MDPI are made immediately available worldwide under an open access license. No special permission is required to reuse all or part of the article published by MDPI, including figures and tables. For articles published under an open access Creative Common CC BY license, any part of the article may be reused without permission provided that the original article is clearly cited. For more information, please refer to https://www.mdpi.com/openaccess.

Feature papers represent the most advanced research with significant potential for high impact in the field. A Feature Paper should be a substantial original Article that involves several techniques or approaches, provides an outlook for future research directions and describes possible research applications.

Feature papers are submitted upon individual invitation or recommendation by the scientific editors and must receive positive feedback from the reviewers.

Editor’s Choice articles are based on recommendations by the scientific editors of MDPI journals from around the world. Editors select a small number of articles recently published in the journal that they believe will be particularly interesting to readers, or important in the respective research area. The aim is to provide a snapshot of some of the most exciting work published in the various research areas of the journal.

Original Submission Date Received: .

6.4

2.5 Journals Sci. Pharm. 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) subject Imprint Information get_app Journal Flyer Open Access ISSN: 2218-0532 Latest Articles 16 pages, 1485 KiB Open AccessArticle Effect of Edge Activator Combinations in Transethosomal Formulations for Skin Delivery of Thymoquinone via Langmuir Technique by Hana Mohd, Katarzyna Dopierała, Anze Zidar, Amitkumar Virani and Bozena Michniak-Kohn Sci. Pharm. 2024, 92(2), 29; https://doi.org/10.3390/scipharm92020029 - 27 May 2024 Abstract Abstract: Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an [...] Read more. Abstract: Thymoquinone (TQ), a bioactive compound found in Nigella sativa seeds, possesses diverse therapeutic properties for skin conditions. However, formulating TQ presents challenges due to its hydrophobic nature and chemical instability, which hinder its skin penetration. Transethosomes, as a formulation, offer an environment conducive to enhancing TQ’s solubility, stability, and skin permeation. To optimize TQ transethosomal formulations, we introduced a combination of ionic and nonionic surfactants, namely Tween 20 and sodium lauryl sulfate (SLS) or sodium lauroyl glutamate (SLG). Surfactants play a crucial role in stabilizing the formulation, reducing aggregation, improving biocompatibility, and minimizing potential toxicity. We fine-tuned the formulation composition and gained insights into its interfacial behavior using the Langmuir monolayer technique. This method elucidated the interfacial properties and behavior of phospholipids in ethosome and transethosome formulations. Our findings suggest that monolayer studies can serve as the initial step in selecting surfactants for nanocarrier formulations based on their interfacial dilational rheology studies. It was found that the addition of surfactant to the formulation increased the elasticity considering the capability of transethosomes to significantly decrease their radius when permeating the skin barrier. The results of the dilational rheology experiments were most relevant to drug permeation through the skin for the largest amplitude of deformation. The combination of Tween 20 and SLS efficiently modified the rheological behavior of lipids, increasing their elasticity. This conclusion was supported by in vitro studies, where formulation F2 composed of Tween 20 and SLS demonstrated the highest permeation after 24 h (300.23 µg/cm2). Furthermore, the F2 formulation showed the highest encapsulation efficiency (EE) of 94%, surpassing those of the control and ethosomal formulations. Additionally, this transethosomal formulation exhibited antimicrobial activity against S. aureus, with a zone of inhibition of 26.4 ± 0.3 mm. Importantly, we assessed the cytotoxicity of both ethosomes and transethosomes at concentrations ranging from 3.5 µM to 50 µM on HaCaT cell lines and found no cytotoxic effects compared to TQ hydroethanolic solution. These results suggest the potential safety and efficacy of TQ transethosomal formulations. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) 35 pages, 5088 KiB Open AccessReview Drug Delivery Nano-Platforms for Advanced Cancer Therapy by Ekaterina Naumenko, Ivan Guryanov and Marina Gomzikova Sci. Pharm. 2024, 92(2), 28; https://doi.org/10.3390/scipharm92020028 - 22 May 2024 Abstract The incidence of cancer is growing every year and covers all age groups, including the working population, which makes cancer socially significant. Existing methods of treatment, despite the effectiveness of individual compounds in relation to cancer cells, are not perfect due to a [...] Read more. The incidence of cancer is growing every year and covers all age groups, including the working population, which makes cancer socially significant. Existing methods of treatment, despite the effectiveness of individual compounds in relation to cancer cells, are not perfect due to a number of side effects associated with high doses that physicians are forced to administer when using treatment protocols. A particularly difficult issue is the creation of effective functional containers that would have the properties of targeting certain types of cells. The solution of this problem is currently relevant, which is reflected in the growth of publications on this subject in recent years. The most promising is the use of nanotechnology in the development of bioengineered therapeutics and containers for chemotherapeutic agents. In this review, we tried to assess the trends that exist in this area of research, as well as show the wide using of some commercially available formulations based on the nano-sized vehicles. Full article attachment Supplementary material: Supplementary File 1 (ZIP, 192 KiB) 16 pages, 763 KiB Open AccessArticle Bioactive Components Analysis and Pharmacological Properties of Extracts and Metabolites of Lichen Umbilicaria crustulosa by Jovica Tomović, Aleksandar Kočović, Marijana Anđić, Jovana Bradić, Nevena Zubić, Vladimir Jakovljević, Miroslav Sovrlić, Perica Vasiljević and Nedeljko Manojlović Sci. Pharm. 2024, 92(2), 27; https://doi.org/10.3390/scipharm92020027 - 20 May 2024 Abstract Lichens, a diverse group of organisms, have a unique structure consisting of fungal filaments and photosynthetic partner cells. This research conducted a comprehensive chemical analysis and evaluation of the anti-inflammatory and antioxidant properties of methanolic and acetone extracts from Umbilicaria crustulosa lichen, along [...] Read more. Lichens, a diverse group of organisms, have a unique structure consisting of fungal filaments and photosynthetic partner cells. This research conducted a comprehensive chemical analysis and evaluation of the anti-inflammatory and antioxidant properties of methanolic and acetone extracts from Umbilicaria crustulosa lichen, along with its isolated metabolites. The process involved separating atranorin and chloratranorin fractions, physodic acid, and gyrophoric acid. Secondary metabolites were identified using chromatographic and spectroscopic data. The total polyphenols content was determined spectrophotometrically. This study examined the antioxidant activity of extracts of the lichen U. crustulosa and the isolated fractions using three methods: DPPH scavenging activity, ABTS scavenging activity, and reducing power. This study also evaluated the acute oral toxicity and the anti-inflammatory activity of the extracts in Wistar albino rats. A higher content of the total phenolic compounds was found in the acetone extract, but antioxidant and anti-inflammatory activities were more prominent in the methanolic extract. The isolated atranorin and chloratranorin fractions and compound physodic acid showed the highest antioxidant activity. No toxic effects were noted in the acute oral toxicity study. This study highlights the potential of the investigated lichen as a valuable source of novel biological agents. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Figure 1

11 pages, 1857 KiB Open AccessArticle Advancing Transdermal Delivery by Zn/Ag-Electrode-Printed Iontophoretic Patch with Self-Generating Microcurrents by Cheng-Liang Peng, Pei-Chi Lee, Hsin-Tung Liu and Ping-Shan Lai Sci. Pharm. 2024, 92(2), 26; https://doi.org/10.3390/scipharm92020026 - 14 May 2024 Abstract This study aimed to evaluate Zn/Ag-electrode-printed patches for the transdermal delivery of small molecules through iontophoresis. The Zn/Ag-electrode-printed patches interact with biological liquid electrolytes and generate suitable microcurrents for the iontophoretic delivery of small molecules across the skin. In fluorescein permeation studies, Zn/Ag-electrode-printed [...] Read more. This study aimed to evaluate Zn/Ag-electrode-printed patches for the transdermal delivery of small molecules through iontophoresis. The Zn/Ag-electrode-printed patches interact with biological liquid electrolytes and generate suitable microcurrents for the iontophoretic delivery of small molecules across the skin. In fluorescein permeation studies, Zn/Ag-electrode-printed patches increased the transdermal depth of fluorescein into the dermis, while the permeation of fluorescein was limited when Zn/C-electrode-printed patches were tested. Further permeation experiments were conducted with 3D skin models, which showed a similar trend to the above, indicating that Zn/Ag-electrode-printed patches had a higher penetration rate compared to the blank. Studies using acetyl hexapeptide-8 as a peptide drug model and sodium ascorbyl phosphate (SAP) as a hydrophilic derivative of ascorbic acid showed that the iontophoretic patch with Zn/Ag electrodes promoted more penetration of drugs than unprinted patches. The permeation of SAP exhibited a two-phase profile with a relatively rapid permeation followed by a sustained, slower permeation. The permeation of acetyl hexapeptide-8 was slower due to its higher molecular weight, but the iontophoretic patch increased the permeation up to 1.5 times more than the unprinted patch. The microcurrent generated by the patch drives the transport of small molecule components through the skin, for the controlled and efficient delivery of therapeutic agents. The flexible design, efficient microcurrent generation, and stable electrodes make the Zn/Ag-electrode-printed patch a promising tool for transdermal drug delivery. Full article ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 372 KiB) 14 pages, 1859 KiB Open AccessArticle Breast Cancer Prevention by Dietary Polyphenols: Microemulsion Formulation and In Vitro Studies by Ghea Putri Cristy, Desy Liana, Jaruwan Chatwichien, Chanat Aonbangkhen, Chantragan Srisomsap and Anuchit Phanumartwiwath Sci. Pharm. 2024, 92(2), 25; https://doi.org/10.3390/scipharm92020025 - 13 May 2024 Abstract Concerns surrounding breast cancer have been increasing, as it leads to the current global cancer incidence and causes a high mortality rate in women. This study investigated the physiological effects of common dietary polyphenols that might prevent breast cancer progression. Quercetin, kaempferol, and [...] Read more. Concerns surrounding breast cancer have been increasing, as it leads to the current global cancer incidence and causes a high mortality rate in women. This study investigated the physiological effects of common dietary polyphenols that might prevent breast cancer progression. Quercetin, kaempferol, and rosmarinic acid were selected to explore their potential bioactivities. Each polyphenol was formulated into a microemulsion to improve its bioactivity and bioavailability. In vitro antioxidant and cytotoxicity activities of the selected polyphenols and their microemulsion forms were further investigated. The optimized microemulsion carrier with 1% oleic acid, 3% ethanol, 10% polysorbate 20, and 86% ultrapure water achieved more than 90% polyphenol encapsulation efficiency. The microemulsion was stable for more than 30 days when encapsulating polyphenol in the fluctuating temperature treatment. In vitro studies suggested that rosmarinic acid-loaded microemulsion had the best antioxidant activity compared with other polyphenol-loaded microemulsions (PL-MEs). Blank microemulsion and all PL-MEs significantly inhibited the proliferation of both hormone-dependent (T47D) and hormone-independent (MDA-MB-231) breast cancer cells. More studies are warranted to confirm the contribution of the microemulsion carrier components to the polyphenols’ improved antioxidant activity and high toxicity of PL-MEs on breast cancer cells. Full article ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 530 KiB) 13 pages, 1643 KiB Open AccessArticle Quantitative 1H NMR Spectroscopy Method for Determination of Anthraquinone Derivatives in Extracts from Rubia tinctorum L. Roots and Rhizomes by Vasilii Vasil’ev, Anzhelika Sheremeta, Vasilii Ivlev, Sergey Goriainov, Fadi Hajjar, Cesar Esparza, Evgeniy Platonov, Arkadiy Khromov, Alexandr Kolesnov, Victoria Romashchenko and Gennady Kalabin Sci. Pharm. 2024, 92(2), 24; https://doi.org/10.3390/scipharm92020024 - 4 May 2024 Abstract The roots and rhizomes of Rubia tinctorum L. have been widely used both for industrial and medicinal purposes for centuries. The primary biologically active substances from Rubia tinctorum L. roots and rhizomes are anthraquinone derivatives such as ruberythric acid and lucidin-3-primeveroside. Their identification [...] Read more. The roots and rhizomes of Rubia tinctorum L. have been widely used both for industrial and medicinal purposes for centuries. The primary biologically active substances from Rubia tinctorum L. roots and rhizomes are anthraquinone derivatives such as ruberythric acid and lucidin-3-primeveroside. Their identification and quantification are carried out by various analytical methods, requiring a complicated sample preparation as well as special reagents and reference samples. However, NMR spectroscopy has no limitations of this kind. In this work, we have developed and validated a new express and standard-free method for the qualitative and quantitative analysis of ruberythric acid and lucidin-3-primeveroside by 1H NMR spectroscopy in the extracts from the roots and rhizomes of Rubia tinctorum L. In this work, we have optimized the conditions of the sample preparation and registration of 1H NMR spectra, determined the optimal solvent and reference compound and confirmed the obtained results by HPLC-UV-MS. Full article (This article belongs to the Topic Natural Products and Drug Discovery) ►▼ Show Figures

Figure 1

16 pages, 336 KiB Open AccessReview Wide Use of Hyaluronic Acid in the Process of Wound Healing—A Rapid Review by Magdalena Antoszewska, Ewa Maria Sokolewicz and Wioletta Barańska-Rybak Sci. Pharm. 2024, 92(2), 23; https://doi.org/10.3390/scipharm92020023 - 25 Apr 2024 Abstract Hyaluronic acid (HA), as one of the main components of the extracellular matrix (ECM), plays an important role in the process of wound-healing and tissue-repair processes due to its unique properties and different physiological functions. HA has an ability to maintain a moist [...] Read more. Hyaluronic acid (HA), as one of the main components of the extracellular matrix (ECM), plays an important role in the process of wound-healing and tissue-repair processes due to its unique properties and different physiological functions. HA has an ability to maintain a moist environment that promotes healing, the stimulation of growth factors and cellular constituents, and the migration of various cells essential for healing. This paper offers a review of HA use in the process of wound healing, with emphasis on hard-to-heal wounds, and examines its various applications in ophthalmology and otorhinolaryngology. It proves HA to be a versatile agent which finds its use in various fields of medicine for its antioxidant, anti-inflammatory, antibacterial properties and accelerated wound healing. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) attachment Supplementary material: Supplementary File 1 (ZIP, 586 KiB) 22 pages, 6185 KiB Open AccessArticle Stability-Indicating UPLC-PDA-QDa Methodology for Carvedilol and Felodipine in Fixed-Dose Combinations Using AQbD Principles by Jesús Alberto Afonso Urich, Viktoria Marko, Katharina Boehm, Raymar Andreina Lara Garcia, Anna Fedorko, Sharareh Salar-Behzadi and Dalibor Jeremic Sci. Pharm. 2024, 92(2), 22; https://doi.org/10.3390/scipharm92020022 - 25 Apr 2024 Abstract The development of analytical procedures, in line with the recent regulatory requirements ICH Q2 (R2) and ICH Q14, is progressing, and it must be able to manage the entire life cycle of the methodology. This is also applicable to and especially challenging for [...] Read more. The development of analytical procedures, in line with the recent regulatory requirements ICH Q2 (R2) and ICH Q14, is progressing, and it must be able to manage the entire life cycle of the methodology. This is also applicable to and especially challenging for combinations of drug substances and dosage form. A reliable and efficient, stability-indicating, MS-compatible, reverse-phase ultra-performance liquid chromatographic (UPLC®) method was developed for the determination of carvedilol and felodipine in a combination oral dosage form. The development of the method, performed using analytical quality by design (AQbD) principles, was in line with the future regulatory requirements. Furthermore, the fixed-dose combination dosage forms are a clear solution to the polypharmacy phenomenon in the elderly population. The main factors evaluated were the mobile phase buffer, organic modifier, column, flow, and column temperature. The optimum conditions were achieved with a Waters Acquity HSS T3 (100 × 2.1 mm i.d., 1.8 µm) column at 38 °C, using ammonium acetate buffer (5 mM, pH 4.5) (Solution A) and MeOH (Solution B) as mobile phases in gradient elution (t = 0 min, 10% B; t = 1.5 min, 10% B; t = 12.0 min, 90% B; t = 13.0 min, 10% B; t = 15.5 min, 10% B) at a flow rate of 0.2 mL/min and UV Detection of 240 and 362 nm for carvedilol (CAV) and felodipine (FLP), respectively. The linearity was demonstrated over concentration ranges of 30–650 µg/mL (R2 = 0.9984) (CAV) and 32–260 µg/mL (R2 = 0.9996) (FLP). Forced degradation studies were performed by subjecting the samples to hydrolytic (acid and base), oxidative, and thermal stress conditions. Standard solution stability was also performed. The proposed validated method was successfully used for the quantitative analysis of bulk, stability, and fixed-dose combination dosage form samples of the desired drug product. Using the AQbD principles, it is possible to generate methodologies with improved knowledge, leading to high-quality data, lower operation costs, and minimum regulatory risk. Furthermore, this work paves the way for providing a platform of robust analytical methods for the simultaneous quantification of innovative on-demand new dose combinations. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Graphical abstract

attachment Supplementary material: Supplementary File 1 (ZIP, 533 KiB) 16 pages, 5997 KiB Open AccessArticle Design, Synthesis and Antimicrobial Potential of Conjugated Metallopeptides Targeting DNA by Maria Camila Moreno-Ramirez, Adriana Stefania Arias-Bravo, Alberto Aragón-Muriel, César Alonso Godoy, Yamil Liscano, Jose Oñate Garzón and Dorian Polo-Cerón Sci. Pharm. 2024, 92(2), 21; https://doi.org/10.3390/scipharm92020021 - 17 Apr 2024 Abstract Antimicrobial resistance threatens the effective prevention and treatment of an increasingly broad spectrum of infections caused by pathogenic microorganisms. This pressing challenge has intensified the search for alternative antibiotics with new pharmacological properties. Due to the chemical synergy between the biological activity of [...] Read more. Antimicrobial resistance threatens the effective prevention and treatment of an increasingly broad spectrum of infections caused by pathogenic microorganisms. This pressing challenge has intensified the search for alternative antibiotics with new pharmacological properties. Due to the chemical synergy between the biological activity of antimicrobial peptides (AMPs) and the different modes of action, catalytic properties, and redox chemistry of metal complexes, metallopeptides have emerged in recent years as an alternative to conventional antibiotics. In the present investigation, peptide ligands conjugated with 5-carboxy-1,10-phenanthroline (Phen) were prepared by solid-phase peptide synthesis (SPPS), and the corresponding copper(II) metallopeptides, Cu-PhenKG and Cu-PhenRG (where K = lysine, R = arginine, and G = glycine), were synthesized and characterized. The antimicrobial activities of these compounds toward Gram-positive and Gram-negative bacteria, evaluated by the broth microdilution technique, indicate that the metal center in the metallopeptides increases the antimicrobial activity of the complexes against the conjugated peptide ligands. Minimum inhibitory concentration (MIC) values of 0.5 μg/mL for S. aureus with the Cu-PhenKG complex and 0.63 μg/mL for S. typhimurium with the Cu-PhenRG complex were obtained. The MIC values found for the conjugated peptides in all microorganisms tested were greater than 1.5 μg/mL. The interactions of the conjugated peptides and their metallopeptides with plasmid DNA were evaluated by agarose gel electrophoresis. Alterations on the replication machinery were also studied by polymerase chain reaction (PCR). The results indicate that the complexes interact efficiently with pBR322 DNA from E. coli, delaying the band shift. Furthermore, the resulting DNA–metallopeptide complex is not a useful template DNA because it inhibits PCR, since no PCR product was detected. Finally, molecular dynamics and molecular docking simulations were performed to better understand the interactions of the obtained compounds with DNA. The Cu-PhenRG complex shows a significantly higher number of polar interactions with DNA, suggesting a higher binding affinity with the biopolymer. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 385 KiB) 8 pages, 1434 KiB Open AccessCommunication Nanosized Particles of Synthetic Silicon Dioxide Delay the Regeneration of Gastric Ulcers Created by N-Methyl-N′-Nitro-N-Nitrosoguanidine and Induce Hyper-Trophic Gastritis-like Symptoms by Ayaka Iwasaki, Yuichi Kawai and Akira Onodera Sci. Pharm. 2024, 92(2), 20; https://doi.org/10.3390/scipharm92020020 - 11 Apr 2024 Abstract Synthetically produced silicon dioxide used as a food additive exhibits nanoparticle size and shape during the early stages of manufacturing. Even when processed into food products, these nanoparticles are detected. Although processing food ingredients into nanoparticles can improve absorption rates or enhance texture, [...] Read more. Synthetically produced silicon dioxide used as a food additive exhibits nanoparticle size and shape during the early stages of manufacturing. Even when processed into food products, these nanoparticles are detected. Although processing food ingredients into nanoparticles can improve absorption rates or enhance texture, there are concerns about the specific biological effects of nanoparticles. In this study, three types of silica particles, including nanosized particles, were repetitively administered to the stomach using a gastric tube or exposed to a single injection into the submucosal layer of the stomach. Macroscopic and microscopic examinations did not reveal acute toxicity. However, when silica particles were administered to the stomach during the healing and regeneration process of gastric ulcers (induced by injecting the alkylating agent of N-Methyl-N′-Nitro-N-Nitrosoguanidine into the submucosal layer), silica particles with a diameter of 70 nm (SiNPs-70) delayed regeneration more strongly than microsized silica particles with diameters of 300 nm or 1000 nm (SiMPs-300, -1000). Furthermore, fibrosis for tissue regeneration spread throughout the entire mucosa of the stomach, resulting in hypertrophic gastritis-like symptoms. The frequency of this symptom was over 50% with SiNPs-70, 20% with SiMPs-300, and 0% with SiMPs-1000. Although the silica particles used in this study differ from actual samples found in food, the impact of particle size, particularly the effects unique to nanosize, was identified as toxicity in the stomach healing process. Full article ►▼ Show Figures

Graphical abstract

15 pages, 3098 KiB Open AccessArticle β-Sitosterol Mediates Gastrointestinal Smooth Muscle Relaxation Induced by Coccoloba uvifera via Muscarinic Acetylcholine Receptor Subtype 3 by Francisco J. Aguirre-Crespo, José L. Aragón-Gastélum, Eduardo J. Gutiérrez-Alcántara, Pedro Zamora-Crescencio, Diana L. Gómez-Galicia, Diego R. Alatriste-Kurzel, Guzman Alvarez and Emanuel Hernández-Núñez Sci. Pharm. 2024, 92(2), 19; https://doi.org/10.3390/scipharm92020019 - 5 Apr 2024 Abstract Coccoloba uvifera is a Mayan medicinal plant, and these leaves are used as antidiarrheal and diuretic agents. In the present work, we develop in-vitro, ex-vivo, in-vivo, and in-silico strategies to evaluate several aqueous extracts of C. uvifera leaves. In vitro tests showed that [...] Read more. Coccoloba uvifera is a Mayan medicinal plant, and these leaves are used as antidiarrheal and diuretic agents. In the present work, we develop in-vitro, ex-vivo, in-vivo, and in-silico strategies to evaluate several aqueous extracts of C. uvifera leaves. In vitro tests showed that decoction extract (CuDe) presented the best yield and chlorophyll, phenol, and flavonoid content; however, CuDe showed low antioxidant activity (DPPH model). All aqueous extracts exert spasmolytic and vasorelaxant activity in a concentration-dependent manner (ex vivo), and in vivo tests showed that CuDe exerts the best antiperistaltic and diuretic effects. The in-silico analysis suggests that C. uvifera triterpenes act as a ligand of GPCR, and β-sitosterol could act as an antagonist of muscarinic acetylcholine receptor subtype 3 (m3AChR). In the context of aqueous extracts of C. uvifera, β-sitosterol and their heterosides were identified by FTIR and 1H-NMR spectroscopy. The concerted binding of β-sitosterol and other triterpenes within the m3AChR binding site may be relevant for the induction of relaxant effects at the gastrointestinal smooth muscle level. In this context, C. uvifera is a high-value plant species that requires analytical and pharmacological studies to confirm traditional medicinal use. Full article (This article belongs to the Topic Natural Products and Drug Discovery) ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 1853 KiB) 20 pages, 6519 KiB Open AccessArticle Synthesis, Biological Evaluation, Molecular Docking and ADME Studies of Novel Pyrrole-Based Schiff Bases as Dual Acting MAO/AChE Inhibitors by Emilio Mateev, Magdalena Kondeva-Burdina, Maya Georgieva, Alexandrina Mateeva, Iva Valkova, Virginia Tzankova and Alexander Zlatkov Sci. Pharm. 2024, 92(2), 18; https://doi.org/10.3390/scipharm92020018 - 29 Mar 2024 Abstract Considering the complex pathogenesis of Alzheimer’s disease (AD), the multitarget ligand strategy is expected to provide superior effects for the treatment of the neurological disease compared to the classic single target approach. Thus, a series of 13 novel (5e-q) pyrrole-based Schiff [...] Read more. Considering the complex pathogenesis of Alzheimer’s disease (AD), the multitarget ligand strategy is expected to provide superior effects for the treatment of the neurological disease compared to the classic single target approach. Thus, a series of 13 novel (5e-q) pyrrole-based Schiff bases were synthesized by conventional and microwave-assisted condensations, and the compounds were evaluated for MAO-A, MAO-B and AChE inhibitory activities. The chemical structures of the newly formed molecules were elucidated by a combination of spectral methods. The obtained results confirmed the theoretical data. The majority of the title Schiff bases demonstrated good potential towards AChE at 10 μM concentrations, with the most promising compound 5m (58%) exerting a comparative effect to that of the applied standard—Donepezil. 5j and 5o selectively inhibited MAO-B by 26% and 21% (at 1 μM concentration), respectively. The compound condensed with 5-nitro-2-furaldehyde (5j) achieved the best dual MAO-B and AChE inhibitory capacities. In addition to the in vitro analysis, docking simulations targeting the active sites of AChE (PDB ID: 4EY6) and MAO-B (PDB: 2V5Z) were employed to explore the possible interactions of the most prominent dual inhibitor (5j) with the enzymes. Furthermore, in silico ADME and PAMPA-blood–brain barrier (BBB) studies were conducted. Full article ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 283 KiB) 13 pages, 2456 KiB Open AccessArticle Semaglutide as a Possible Calmodulin Binder: Ligand-Based Computational Analyses and Relevance to Its Associated Reward and Appetitive Behaviour Actions by Giuseppe Floresta, Davide Arillotta, Valeria Catalani, Gabriele Duccio Papanti Pelletier, John Martin Corkery, Amira Guirguis and Fabrizio Schifano 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 [...] Read more. 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. Full article (This article belongs to the Topic Bioinformatics in Drug Design and Discovery, 2nd Volume) ►▼ Show Figures

Figure 1

17 pages, 1730 KiB Open AccessReview 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 [...] Read more. 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. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Graphical abstract

attachment Supplementary material: Supplementary File 1 (ZIP, 198 KiB) 23 pages, 2298 KiB Open AccessArticle 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 [...] Read more. 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. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 276 KiB) 16 pages, 4225 KiB Open AccessArticle 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 [...] Read more. 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. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Graphical abstract

14 pages, 3928 KiB Open AccessArticle 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 [...] Read more. 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. Full article (This article belongs to the Topic Natural Products and Drug Discovery) ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 429 KiB) 11 pages, 2743 KiB Open AccessArticle Attenuation of Pulmonary Damage Associated with COPD in a Cadmium-Exposed Model Due to the Administration of a siRNA Targeting PAD4 by 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 - 4 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 [...] Read more. 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. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Figure 1

attachment Supplementary material: Supplementary File 1 (ZIP, 192 KiB) 8 pages, 903 KiB Open AccessArticle The Potential of Incorporating a Pharmacist-Only Medicine Category in Poland by 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 - 4 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 [...] Read more. 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. Full article (This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica) ►▼ Show Figures

Figure 1

18 pages, 2869 KiB Open AccessArticle 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 Abstract (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 [...] Read more. (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. Full article ►▼ Show Figures