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 31.4 days after submission; acceptance to publication is undertaken in 5.6 days (median values for papers published in this journal in the first half of 2024).
- 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:
2.3 (2023);
5-Year Impact Factor:
2.9 (2023)
Latest Articles
A Network Pharmacology and Molecular Docking Technology to Identify and Explore Mechanism of Bioactive Components of Fucus vesiculosus against Gut Disorders
Sci. Pharm. 2024, 92(3), 49; https://doi.org/10.3390/scipharm92030049 - 30 Aug 2024
Abstract
The gut is an intricate and diverse organ system for investigating visceral pattern generation. The gut made an early evolutionary breakthrough. There is evidence that the molecular mechanisms governing the development of gastrointestinal patterns are species-specific. Some have suggested using marine drugs to
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The gut is an intricate and diverse organ system for investigating visceral pattern generation. The gut made an early evolutionary breakthrough. There is evidence that the molecular mechanisms governing the development of gastrointestinal patterns are species-specific. Some have suggested using marine drugs to treat gastrointestinal disorders. The study, which used an integrated network pharmacology approach, aimed to find out how well fucoidan worked and what Fucus vesiculosus might be doing to help prevent digestive problems. Researchers gathered information on how potential bioactive components of brown seaweed and their associated targets interact with the disease gene targets of gastrointestinal disorders. We studied the signaling pathways linked to F. vesiculosus in the context of gut health treatments using a KEGG (Kyoto Encyclopedia of Genes and Genomes pathway) and GO (Gene ontology) enrichment analysis. We built and studied the protein–protein interaction (PPI) and compound-target networks using Cytoscape. PPI network analysis yielded a total of 44 important targets, including BCL2, ESR1, and STAT3. The KEGG enrichment analysis revealed a strong correlation between the signaling pathways used in the treatment and the prevention of gastrointestinal disorders. We docked significant genes with TNF, STAT3, BCL2, and ALB. Fucoxanthin and fucoidan possess beneficial properties for improving gut health by treating gastric-intestinal issues. This study showed that by controlling several targets and many pathways with multiple components, F. vesiculosus exhibited preventive effects against gastrointestinal disorders.
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Open AccessArticle
Phosal® Curcumin-Loaded Nanoemulsions: Effect of Surfactant Concentration on Critical Physicochemical Properties
by
Joanna Czerniel, Aleksandra Gostyńska, Tomasz Przybylski and Maciej Stawny
Sci. Pharm. 2024, 92(3), 48; https://doi.org/10.3390/scipharm92030048 - 30 Aug 2024
Abstract
Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject
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Curcumin is a well-known and widely used substance of natural origin. It has also been found to be helpful in the treatment of liver diseases. Unfortunately, curcumin has very low bioavailability and a sensitivity to external agents. Improving these parameters is the subject of many studies. One way to overcome these problems may be to use Phosal® Curcumin as a source of curcumin and encapsulate this dispersion into a nanoemulsion using different types and concentrations of surfactants and co-surfactants, thus manipulating the physicochemical parameters of the nanoemulsion. The present study aimed to develop curcumin-loaded nanoemulsions for intravenous administration and to investigate the effect of Kolliphor HS15 concentration on their critical quality attributes. Methods: Phosal® Curcumin-loaded nanoemulsions with different concentrations of Kolliphor HS15 were prepared by high-pressure homogenization. The effect of Kolliphor HS15 on emulsion physicochemical properties such as mean droplet diameter (MDD), polydispersity index (PDI), zeta potential (ZP), osmolality (OSM), and pH, as well as encapsulation efficiency (EE) and retention rate (RR) of curcumin, were determined. Mid-term stability studies and short-term stress tests were conducted to evaluate the impact of Kolliphor HS15 on the critical quality attributes of the curcumin-loaded nanoemulsions stored under various conditions. Results: Five nanoemulsions with increasing Kolliphor HS15 concentrations were developed. Their MDD ranged from 85.2 ± 2.0 to 154.5 ± 5.1 nm, with a PDI from 0.18 ± 0.04 to 0.10 ± 0.01 and ZP from −15.6 ± 0.7 to −27.6 ± 3.4 mV. Depending on the concentration of Kolliphor HS15, the EE ranged from 58.42 ± 1.27 to 44.98 ± 0.97%. Conclusions: The studied parameters of the developed nanoemulsions meet the requirements for formulations for intravenous administration. Using the appropriate concentration of Kolliphor HS15 allows for a formulation that presents a protective effect against both curcumin and emulsion degradation.
Full article
(This article belongs to the Topic Complementary Strategies in Drug Delivery: From Particle Engineering to System Optimization)
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Open AccessArticle
Synthesis and Catalytic Activity of Novel Complexes Based on Cyano-Substituted Phthalocyanines as Promising Drug Conversion Agents
by
Dmitry Erzunov, Svetlana Tonkova, Ilya Sarvin and Arthur Vashurin
Sci. Pharm. 2024, 92(3), 47; https://doi.org/10.3390/scipharm92030047 - 28 Aug 2024
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This paper presents the results of obtaining new cobalt and zinc complexes based on dicyanophenoxy-substituted carboxypthalocyanine. The original method of synthesis and isolation of the compound is shown; its spectroscopic and photophysical characteristics are studied. Studies show the absence of aggregation processes in
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This paper presents the results of obtaining new cobalt and zinc complexes based on dicyanophenoxy-substituted carboxypthalocyanine. The original method of synthesis and isolation of the compound is shown; its spectroscopic and photophysical characteristics are studied. Studies show the absence of aggregation processes in organic media for solutions of complexes in working concentration ranges. This shows the possibility of the practical application of structures as catalysts. The high catalytic activity of cobalt complexes with dicyanophenoxy-substituted carboxyphthalocyanine ligand in the conversion reaction of sodium diethyldithiocarbamate to disulfiram, which is an active component of drugs for the treatment of alcohol dependence, is determined.
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Open AccessArticle
New Design and Characteristics of Probiotics Immobilized on a Clinoptilolite-Containing Tuff
by
Olga Ilinskaya, Antonina Galeeva, Michael Glukhov, William Kurdy, Pavel Zelinikhin, Alexey Kolpakov, Galina Yakovleva and Oleg Lopatin
Sci. Pharm. 2024, 92(3), 46; https://doi.org/10.3390/scipharm92030046 - 19 Aug 2024
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Increasing the biological effectiveness of probiotic preparations requires the development of new stable forms in the gastrointestinal tract. Live bacteria immobilized on a sorbent belong to the latest, fourth generation of probiotics, which ensures a prolonged effect. This study is devoted to developing
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Increasing the biological effectiveness of probiotic preparations requires the development of new stable forms in the gastrointestinal tract. Live bacteria immobilized on a sorbent belong to the latest, fourth generation of probiotics, which ensures a prolonged effect. This study is devoted to developing a new method of preparing active lactobacilli on a natural mineral carrier, a tuff containing zeolite of the clinoptilolite group, which is among the most common authigenic silicate minerals that occur in sedimentary rocks and is known as a safe ion-exchange and adsorbing detoxicant. Among the characterized lactobacilli, strains of L. plantarum, L. acidophilus, and L. crispatus possessed a high level of acid formation and stability in gastrointestinal fluids. The protective effect of the clinoptilolite-containing tuff was registered when the samples were incubated in gastric juice. The optimal technological conditions for immobilization and lyophilization were determined, and the preservation of the viability and probiotic properties of bacteria was confirmed during 8 months of storage. The release of bacteria from the carrier occurred gradually over 12 h. The data obtained show how promising the new preparation is, combining the ability to detoxify harmful intestinal metabolites and the prolonged release of probiotics.
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Open AccessArticle
Antioxidant Activity of the Medicinal Plant Urtica dioica L.: Extraction Optimization Using Response Surface Methodology and Protective Role in Red Blood Cells
by
Aleksja Suli and Eugenia Papadaki
Sci. Pharm. 2024, 92(3), 45; https://doi.org/10.3390/scipharm92030045 - 14 Aug 2024
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Free radicals are highly reactive compounds that lead to the onset of a variety of serious health conditions, known as “oxidative stress”. Antioxidants, on the other hand, act as defense mechanisms to fight the accumulation of free radicals and maintain cell homeostasis. Urtica
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Free radicals are highly reactive compounds that lead to the onset of a variety of serious health conditions, known as “oxidative stress”. Antioxidants, on the other hand, act as defense mechanisms to fight the accumulation of free radicals and maintain cell homeostasis. Urtica dioica L. is a medicinal plant with unique antioxidant properties, mainly attributable to the presence of polar phenolic compounds. This study aimed to optimize the combination of determinant factors toward the maximum extraction of antioxidants from U. dioica L. Furthermore, it investigated the protective role of the extract on red blood cells that were exposed to oxidative stress. The extraction optimization was performed using Response Surface Methodology and the in vitro antioxidant activity of the extract was determined with Folin–Ciocalteu, FRAP, and DPPH assays. Based on the results, the highest value of antioxidant activity and polar phenolic compounds was recorded using 34% (v/v) ethanol as a solvent in an ultrasonic process carried out at 42 °C for 87 min. In addition, UV–Vis spectrum of the extract revealed the presence of chlorophylls, carotenoids, and flavonoid glycosides. This study also provided insight into the in vitro protective effect of the plant extract on red blood cells morphology under oxidative stress conditions. The findings highlighted the good predictability of the extraction model and the potential role of the extract as an antioxidant product.
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Graphical abstract
Open AccessArticle
Topical Application of Cha-Koji, Green Tea Leaves Fermented with Aspergillus Luchuensis var Kawachii Kitahara, Promotes Acute Cutaneous Wound Healing in Mice
by
Yasuhiro Katahira, Jukito Sonoda, Miu Yamagishi, Eri Horio, Natsuki Yamaguchi, Hideaki Hasegawa, Izuru Mizoguchi and Takayuki Yoshimoto
Sci. Pharm. 2024, 92(3), 44; https://doi.org/10.3390/scipharm92030044 - 12 Aug 2024
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“Koji” is one of the most well-known probiotic microorganisms in Japan that contribute to the maintenance of human health. Although the beneficial effects of some probiotics on ulcer healing have been demonstrated, there have been no reports on the wound healing effects of
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“Koji” is one of the most well-known probiotic microorganisms in Japan that contribute to the maintenance of human health. Although the beneficial effects of some probiotics on ulcer healing have been demonstrated, there have been no reports on the wound healing effects of koji to date. In the present study, we investigated the effects of “cha-koji”, green tea leaves fermented with Aspergillus luchuensis, on cutaneous wound healing, using a linear incision wound mouse model. Topical application of autoclave-sterilized cha-koji suspension on the dorsal incision wound area healed the wound significantly faster and, notably, with less scarring than did the green tea or the control distilled water treatment. Further in vitro experiments revealed that the accelerated effects of cha-koji could be attributed to its increased anti-bacterial activity, enhanced epidermal cell proliferation and migration, augmented expression of the anti-inflammatory cytokine transforming growth factor-β1, reduced expression of inflammatory cytokine interleukin-6 in macrophages, and decreased endoplasmic reticulum stress. In addition, we conducted a skin sensitizing potential test, which revealed that cha-koji had no adverse effects that posed a sensitizing risk. Thus, cha-koji may have a potent therapeutic effect on cutaneous wound healing, opening up a new avenue for its clinical application as a medical aid.
Full article
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Open AccessCommunication
Advances in the Production of PBCA Microparticles Using a Micromixer with HH-Geometry in a Microfluidic System
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Aline Rocha Vieira, Aline Furtado Oliveira, Fabiana Vieira Lima Solino Pessoa, Beatriz Nogueira Messias de Miranda and André Rolim Baby
Sci. Pharm. 2024, 92(3), 43; https://doi.org/10.3390/scipharm92030043 - 9 Aug 2024
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Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH
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Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH geometry and varying numbers of channels (4, 10, and 15), different synthesis formulations were investigated by varying monomer concentrations. PBCA microparticles synthesized with 19.2% (w/w) n-butyl cyanoacrylate (n-BCA) monomer, a residence time of 0.06 s, a flow rate of 78 mL·min−1, and a phase ratio of 45/55 (W/O), exhibited an average diameter of 642.2 nm as determined by dynamic light scattering (DLS) analysis. In contrast, PBCA microparticles synthesized with 5.0% (w/w) n-BCA monomer, the same residence time of 0.06 s, a flow rate of 39 mL·min−1, and a phase ratio of 20/80 (W/O), exhibited an average diameter of 74.73 µm according to laser diffraction particle size analysis. Polymer formation was confirmed by Fourier-transform infrared (FTIR) spectroscopy in both formulation and process conditions. These results indicate that the parameters for the production of microparticles with different monomer concentrations in the microfluidic system with HH geometry and 15 channels can be optimized for potential applications in cosmetics and pharmaceutical ingredients.
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Open AccessArticle
Phytochemical Profiling and Biological Activities of Two Helianthemum Species Growing in Greece
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Evgenia Panou, Konstantia Graikou, Nikolaos Tsafantakis, Fanourios-Nikolaos Sakellarakis and Ioanna Chinou
Sci. Pharm. 2024, 92(3), 42; https://doi.org/10.3390/scipharm92030042 - 8 Aug 2024
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Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted
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Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted in the identification of 15 compounds in each species, mainly terpene and fatty acid derivatives, through GC–MS. The methanolic extract analysis, conducted through UHPLC–MS/MS, led to the identification of 39 metabolites in HN and 29 in HO, respectively, the majority of which were phenolics. Among the identified compounds, several have also been isolated and structurally determined (from HN: rutin, linoleic acid, gallic acid, and isoquercetin, and from HO: quercetin-3-O-(2″-O-galloyl)-galactopyranoside, methyl gallate, catechin-3-O-glucopyranoside, and astragalin, while hyperoside, and cis- and trans-tiliroside have been determined in both species). Furthermore, the methanolic extracts of HN and HO displayed a high total phenolic content (177.2 mg GA/g extract and 150.6 mg GA/g extract, respectively) and considerable free-radical scavenging activity against the DPPH radical (94.6% and 94.0% DPPH inhibition, respectively). Antimicrobial testing showed stronger inhibition of HN against Gram (+) bacterial strains (MIC values 0.07–0.15 mg/mL), while both extracts exhibited low tyrosinase-inhibitory activity. Considering the lack of studies conducted on the chemistry and biological activities of the genus Helianthemum, the chemical characterization of extracts could contribute to new sources of bioactive metabolites to be explored and exploited for further potential applications such as food and/ or the cosmetic industry.
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Open AccessArticle
Antibacterial and Wound Healing Activity In Vitro of Individual and Combined Extracts of Tagetes nelsonii Greenm, Agave americana and Aloe vera
by
Karen Alejandra Olán-Jiménez, Rosa Isela Cruz-Rodríguez, Beatriz del Carmen Couder-García, Nadia Jacobo-Herrera, Nancy Ruiz-Lau, Maritza del Carmen Hernández-Cruz and Víctor Manuel Ruíz-Valdiviezo
Sci. Pharm. 2024, 92(3), 41; https://doi.org/10.3390/scipharm92030041 - 31 Jul 2024
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Currently, there are various physical and mechanical agents that can cause skin wounds, which are still traditionally treated with plant extracts. It has been reported that the genus Tagetes has a wide range of biological properties, including antibacterial and wound healing activity. Likewise,
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Currently, there are various physical and mechanical agents that can cause skin wounds, which are still traditionally treated with plant extracts. It has been reported that the genus Tagetes has a wide range of biological properties, including antibacterial and wound healing activity. Likewise, Agave americana extract and Aloe vera gel have shown potential in the treatment of burn wounds and other skin conditions both in vitro and in vivo. In this study, the antibacterial and wound healing activities of each of these plants were investigated, as well as the possibility of enhancing these activities by combining them. First, the secondary metabolites of the extracts were quantified, the antibacterial activity was evaluated using the Kirby-Bauer method, and their cytotoxicity was measured in 3T3 and HaCaT cells using the sulforhodamine B assay. The results revealed that Tagetes nelsonii extract had a higher amount of secondary metabolites, which is why it exhibited antibacterial activity. Finally, the scratch assay showed that the individual extracts of T. nelsonii and A. americana demonstrated greater cell migration and proliferation starting from 12 h, as well as when using the combination of A. americana extract and A. vera gel, which almost completely closed the wound compared to the control.
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Graphical abstract
Open AccessArticle
Identification of Potential Trypanosoma cruzi Trans-Sialidase Inhibitors by Computational Drug Repositioning Approaches
by
Miguel A. Uc-Chuc, Nohemi Cigarroa-Toledo, Karla Y. Acosta-Viana, José I. Chan-Pérez, Juan C. Pineda-Cortes and Hernán de J. Villanueva-Alonzo
Sci. Pharm. 2024, 92(3), 40; https://doi.org/10.3390/scipharm92030040 - 27 Jul 2024
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Chagas disease, caused by the parasitic protozoan Trypanosoma cruzi (T. cruzi), represents a worldwide public health issue. To date, there is no efficient treatment to combat this pathology, and the only drugs available are usually toxic to the patient. Through the
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Chagas disease, caused by the parasitic protozoan Trypanosoma cruzi (T. cruzi), represents a worldwide public health issue. To date, there is no efficient treatment to combat this pathology, and the only drugs available are usually toxic to the patient. Through the enzyme trans-salidase, the parasite invades, infects, and multiplies intracellularly in the host cell. This protein has been considered an attractive target for developing or searching for compounds with potential trypanocidal activity. In this study, an in silico analysis was performed using a Food and Drug Administration-approved computational drug repositioning approach to identify compounds with anti-Chagas potential against two trans-sialidase proteins. Those compounds with potential inhibition were analyzed and selected through a molecular docking-based virtual screening. Forty-nine compounds were identified, of which forty-five are available on the market, and the rest were evaluated in silico. Our predicted results follow that these compounds are safe for human use and could be potential anti-trans-sialidase agents.
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Open AccessCommunication
Implementation of an Antimicrobial Stewardship Program at the Hospital and ICU Level of a Clinic in Sincelejo-Sucre
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Erick Diaz-Morales, Ana Paola Pacheco-Hermosilla, Daniel Esteban Castro-Mangonez and Nerlis Pajaro-Castro
Sci. Pharm. 2024, 92(3), 39; https://doi.org/10.3390/scipharm92030039 - 17 Jul 2024
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Objectives: In this retrospective observational study, the aim is to establish how the implementation of the use of antimicrobial stewardship programs at the hospital and intensive care unit level in a Sucre Clinic in Sincelejo has had a significant impact on the improvement
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Objectives: In this retrospective observational study, the aim is to establish how the implementation of the use of antimicrobial stewardship programs at the hospital and intensive care unit level in a Sucre Clinic in Sincelejo has had a significant impact on the improvement of the rational use of antibiotics, due to the alarming situation of increasing antibiotic resistance. Materials and methods: The methodology used was to analyze the Excel database of the Clinic in such a way as to compare the data from 2017, the period prior to the implementation of the antimicrobial stewardship program (ASP), with the subsequent evolution between the years 2018 and 2022, in relation to the institutional records of four antibiotics—ceftriaxone3, ciprofloxacin4, meropenem5, and vancomycin6, measured in defined daily dose (DDD). Results: According to the defined daily dose values obtained for the four antibiotics, a reduction in the defined daily dose was identified in the post-implementation period. On the other hand, considering the DDD reported by the World Health Organization for each of the antibiotics, significant differences were verified in comparison with those obtained in the clinic in the hospitalization and intensive care unit services. Conclusions: In conclusion, in the clinic, a reduction in the defined daily dose was verified in the period after the implementation of the antimicrobial stewardship program compared to the previous period, both in the hospitalization and intensive care unit, as well as having a mild-to-large effect with Cohen’s D.
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Open AccessArticle
Combined Effect of Sertraline and Capecitabine on Breast Cancer Cell Lines In Vitro and In Silico Evidence for Synergistic Interaction
by
Serap Ozkaya Gul, Alaaddin Korkut and Esra Aydemir
Sci. Pharm. 2024, 92(3), 38; https://doi.org/10.3390/scipharm92030038 - 15 Jul 2024
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Background: Depression is a common mood disorder that manifests itself simultaneously with chronic diseases. It is especially common in patients diagnosed with cancer, and when neglected, it reduces the success of cancer treatment. The fact that breast cancer is the most common type
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Background: Depression is a common mood disorder that manifests itself simultaneously with chronic diseases. It is especially common in patients diagnosed with cancer, and when neglected, it reduces the success of cancer treatment. The fact that breast cancer is the most common type of cancer in women shows that the treatment of depression in women with cancer is very important. As a result, cancer patients undergoing chemotherapy in oncology units also use antidepressants simultaneously. It is critical to correctly understand the interactions between drugs used in combination. Method: In this study, doses were prepared for MCF7 and MDAMB-231 cell lines by serial dilution from 1000 ng/mL to 1.95 ng/mL. Cell viability was calculated with the WST-1 kit by applying the prepared doses of capecitabine and sertraline alone. In the sertraline/capecitabine combination study, cell viability was examined in MDAMB-231 and MCF-7 cells by applying doses of 300, 100, 50, 25, 10 ng/mL. Combinations that showed selective cytotoxicity after the combination were analyzed with the CompuSyn program and the combination index (CI<1 = synergism) was calculated. Studies on caspase 3-8-9, DNA fragmentation and mTOR were continued using a combination that showed a synergistic effect. Result: It was determined that compared to drug use alone, the sertraline/capecitabine combination decreased cell viability. There is no significant difference in caspase-3,-8,-9 and DNA fragmentation in cancer cells, but there is a reduction in the level of mTOR. This suggests that the death mechanism may be autophagy. Docking studies with autophagy pathway-related proteins further support our results. It is noteworthy that the AKT1-sertraline complex had the best binding affinity among the target proteins (−9.1 kcal/mol).
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Open AccessReview
Intravenous Lipid Emulsions in Anticonvulsants’ Toxicity
by
Simeonka Dimitrova, Stela Dragomanova and Gabriela Kehayova
Sci. Pharm. 2024, 92(3), 37; https://doi.org/10.3390/scipharm92030037 - 4 Jul 2024
Abstract
In recent years, an innovative approach has emerged in the field of toxicology for managing acute intoxications caused by lipophilic substances: intravenous lipid emulsions (ILEs). Through numerous experiments and case reports, the efficacy of lipid emulsions in counteracting toxicities induced by lipophilic agents,
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In recent years, an innovative approach has emerged in the field of toxicology for managing acute intoxications caused by lipophilic substances: intravenous lipid emulsions (ILEs). Through numerous experiments and case reports, the efficacy of lipid emulsions in counteracting toxicities induced by lipophilic agents, including a significant number of antiepileptic (AE) drugs, have become increasingly evident. Data spanning a 10-year period (2010–2020) were analyzed by searching through multiple scientific publication platforms like PubMed, Science Direct, Research Gate, and Springer Link. This study focused on reviewing relevant case reports detailing successful intravenous lipid emulsion (ILE) administration in patients with acute intoxications with antiepileptics, specifically examining the impact of fat emulsions on neurological status, Glasgow Coma Scale (GCS) scores, and corrected QT interval concerning hemodynamic instability. The typical symptoms of antiepileptic toxicity include central nervous system depression, ataxia, and nystagmus. Intravenous lipid emulsion application resulted in an increase in Glasgow Coma Scale scores and enhanced recovery from drug intoxication. This study provides a comprehensive overview of the potential utility of ILE as a component to antidote therapy in cases of acute AE poisoning involving neurotropic drugs. The process involves the engagement of various mechanisms of antitoxic activity.
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Open AccessArticle
Formulation and Physicochemical Characterization of Terpenocannabinoid-Functionalized Hemp Oil Emulsifier: Assessment of Topical Anti-Inflammatory, Antinociceptive, Wound Healing Activity and Cutaneous Toxicity Effects
by
Amira Metouekel, Hind Zejli, Mohamed Chebaibi, Youssra Lefrioui, Dalila Bousta, Hamid El Amri, Elmostafa El Fahime, Saïd El Kazzouli and Nabil El Brahmi
Sci. Pharm. 2024, 92(3), 36; https://doi.org/10.3390/scipharm92030036 - 21 Jun 2024
Abstract
This article presents a comprehensive study on the formulation and physicochemical characterization of a novel terpenocannabinoid-functionalized hemp oil emulsifier (AMCana-Oil) for potential applications in topical anti-inflammatory, antinociceptive, and wound healing treatments. The emulsifier exhibits interesting properties, meets international acidity index requirements, and has
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This article presents a comprehensive study on the formulation and physicochemical characterization of a novel terpenocannabinoid-functionalized hemp oil emulsifier (AMCana-Oil) for potential applications in topical anti-inflammatory, antinociceptive, and wound healing treatments. The emulsifier exhibits interesting properties, meets international acidity index requirements, and has a room temperature density comparable to liquid oils. The prepared emulsifier (AMCana-Oil), AMCana-Oil (10% TC) and AMCana-Oil (20% TC), contains a diverse array of cannabinoids, including cannabidiol (CBD) and delta-9-tetrahydrocannabinol (THC), alongside bioactive compounds such as benzenepropanoic acid and oleamide. Physicochemical properties of AMCana-Oil and MCana-Oil (20% TC) were found, respectively, as follows: density value of 0.9872 ± 0.001 mg/mL: g/cm³ and 0.9882 ± 0.002 mg/mL: g/cm³; an acidity index of 1.599 ± 0.002 mgKOH/g and 1.605 ± 0.001 mgKOH/g; an average peroxide value encompassing a range from 12.982 ± 0.351 to 23.320 ± 0.681 (mEq O2/kg), and a K of 1.575 ± 0.004 and 1.535 ± 0.0039, which underscore the fluidity, stability, and quality of emulsifiers studied. Preliminary pharmacological examinations reveal significant antioxidant, anti-inflammatory, antinociceptive, and wound healing potentials. Moreover, in silico predictions confirm the safety profile of the prepared emulsifiers. These findings emphasize the multifaceted nature of the terpenocannabinoid-functionalized emulsifier, paving the way for its potential applications in topical formulations.
Full article
(This article belongs to the Topic Cannabis, Cannabinoids and Its Derivatives)
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Open AccessArticle
Fluid Dynamics Optimization of Microfluidic Diffusion Systems for Assessment of Transdermal Drug Delivery: An Experimental and Simulation Study
by
Dorottya Kocsis, Shanmugam Dhinakaran, Divyam Pandey, András József Laki, Mária Laki, Dániel Sztankovics, Miléna Lengyel, Judit Vrábel, Márton Bese Naszlady, Anna Sebestyén, Jeyaraj Ponmozhi, István Antal and Franciska Erdő
Sci. Pharm. 2024, 92(2), 35; https://doi.org/10.3390/scipharm92020035 - 20 Jun 2024
Abstract
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Organ-on-a-chip technologies show exponential growth driven by the need to reduce the number of experimental animals and develop physiologically relevant human models for testing drugs. In vitro, microfluidic devices should be carefully designed and fabricated to provide reliable tools for modeling physiological or
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Organ-on-a-chip technologies show exponential growth driven by the need to reduce the number of experimental animals and develop physiologically relevant human models for testing drugs. In vitro, microfluidic devices should be carefully designed and fabricated to provide reliable tools for modeling physiological or pathological conditions and assessing, for example, drug delivery through biological barriers. The aim of the current study was to optimize the utilization of three existing skin-on-a-chip microfluidic diffusion chambers with various designs. For this, different perfusion flow rates were compared using cellulose acetate membrane, polyester membrane, excised rat skin, and acellular alginate scaffold in the chips. These diffusion platforms were integrated into a single-channel microfluidic diffusion chamber, a multi-channel chamber, and the LiveBox2 system. The experimental results revealed that the 40 µL/min flow rate resulted in the highest diffusion of the hydrophilic model formulation (2% caffeine cream) in each system. The single-channel setup was used for further analysis by computational fluid dynamics simulation. The visualization of shear stress and fluid velocity within the microchannel and the presentation of caffeine progression with the perfusion fluid were consistent with the measured data. These findings contribute to the development and effective application of microfluidic systems for penetration testing.
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Open AccessArticle
Fact-Finding Survey and Exploration of Preventive Drugs for Antineoplastic Drug-Induced Oral Mucositis Using the Japanese Adverse Drug Event Report Database
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Hajime Matsuo, Kiri Endo, Hiroyuki Tanaka, Toshihisa Onoda and Toshihiro Ishii
Sci. Pharm. 2024, 92(2), 34; https://doi.org/10.3390/scipharm92020034 - 20 Jun 2024
Abstract
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Oral mucositis (OM) is one of the most common adverse events associated with antineoplastic drug treatment. Studies on the risk of antineoplastic drug-induced OM and its prevention are limited. We, therefore, conducted a disproportionality analysis of antineoplastic drug-induced OM and explored candidate preventive
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Oral mucositis (OM) is one of the most common adverse events associated with antineoplastic drug treatment. Studies on the risk of antineoplastic drug-induced OM and its prevention are limited. We, therefore, conducted a disproportionality analysis of antineoplastic drug-induced OM and explored candidate preventive drugs for OM using the Japanese Adverse Drug Event Report (JADER) database. The JADER database showed that between April 2004 and March 2022, antineoplastic drug-related adverse events were reported in 210,822 cases, of which 2922 were OM. Forty-two drugs appeared to be associated with OM. The weibull distribution showed different patterns of time-to-onset depending on the type of antineoplastic drug administered. Cluster analyses classified antineoplastic drugs according to the typical symptoms of OM. These findings suggest that antineoplastic drug-induced OM should be monitored based on expression patterns of symptoms. Upon analyzing the inverse association, several concomitant drugs, including lenalidomide hydrate and febuxostat, were expected to be candidate preventive drugs for antineoplastic drug-induced OM. Concomitant drugs that showed an inverse association with antineoplastic drug-induced OM differed within the Anatomical Therapeutic Chemical classification. These findings could serve as a reference when considering drugs that should be prioritized to validate their prophylactic effect against antineoplastic-induced OM in the future.
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Open AccessReview
Non-Analog Compounds to Sialic Acid as Inhibitors of Influenza Virus Neuraminidase: An Underexplored Approach for Novel Antivirals―Systematic Review
by
Luis Márquez-Domínguez, Carolina Jasso-Miranda, Virginia Sedeño-Monge and Gerardo Santos-López
Sci. Pharm. 2024, 92(2), 33; https://doi.org/10.3390/scipharm92020033 - 19 Jun 2024
Abstract
Influenza poses a significant threat to public health worldwide, particularly among vulnerable populations such as children, the elderly, immunocompromised individuals, and those with chronic diseases. It is associated with high mortality and morbidity rates. Neuraminidase inhibitors play a crucial role in influenza treatment
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Influenza poses a significant threat to public health worldwide, particularly among vulnerable populations such as children, the elderly, immunocompromised individuals, and those with chronic diseases. It is associated with high mortality and morbidity rates. Neuraminidase inhibitors play a crucial role in influenza treatment by mitigating the risk of complications and death. However, the genetic variability of the influenza virus enables the emergence of drug-resistant mutations. This review focuses on the search for new compounds that are not analogous to sialic acid, aiming to inhibit the activity of viral neuraminidase in vitro, viral replication in cell cultures, or animal models. Influenza virus strains that have been reported in the literature present specific mutations that generate resistance to neuraminidase inhibitors. Since these inhibitors bear structural resemblance to sialic acid, the predominant location for these mutations is the enzyme’s active site. Consequently, exploring alternative compound classes becomes imperative to circumvent this interaction pattern. These compounds will introduce diverse molecular frameworks, serving as foundational structures for further development through rational drug design, thereby engendering novel antiviral agents targeting influenza. The potential prospects for developing novel influenza antivirals based on these findings are discussed.
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(This article belongs to the Topic Challenges and Opportunities in Drug Delivery Research)
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Open AccessArticle
Evidence of Hyperglycemic Levels Improving the Binding Capacity between Human Serum Albumin and the Antihypertensive Drug Hydrochlorothiazide
by
Marilia Amável Gomes Soares, Franklin Souza-Silva, Carlos Roberto Alves, Leonardo Vazquez, Talita Stelling de Araujo, Carlos Serpa and Otávio Augusto Chaves
Sci. Pharm. 2024, 92(2), 32; https://doi.org/10.3390/scipharm92020032 - 7 Jun 2024
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Cardiovascular diseases (CVDs), especially arterial hypertension, stand as prominent contributors to global mortality. Regrettably, individuals with diabetes encounter a two-fold increase in the risk of mortality associated with CVDs. Hydrochlorothiazide (HCTZ) represents a primary intervention for hypertension, particularly in diabetic patients. Nevertheless, there
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Cardiovascular diseases (CVDs), especially arterial hypertension, stand as prominent contributors to global mortality. Regrettably, individuals with diabetes encounter a two-fold increase in the risk of mortality associated with CVDs. Hydrochlorothiazide (HCTZ) represents a primary intervention for hypertension, particularly in diabetic patients. Nevertheless, there has not yet been a comprehensive assessment of the biophysical characteristics regarding the impact of glucose levels on its binding affinity with human serum albumin (HSA). Thus, the present work reports the interactive profile of HSA/HCTZ in nonglycemic, normoglycemic (80 mg/dL), and hyperglycemic (320 mg/dL) conditions by time-resolved fluorescence, saturation transfer difference–nuclear magnetic resonance (STD-NMR), and surface plasmon resonance (SPR). There was a moderate ground state association of HSA/HCTZ with subdomain IIA that was affected in the presence of different glucose levels. The hyperglycemic condition decreased the binding affinity of HCTZ to subdomain IIA and increased the possibility of subdomain IB also being considered as a secondary binding site due to cooperativity and/or alterations in the protein’s structure. Overall, the glucose level under hyperglycemic conditions led to the cavities being more likely to receive more ligands, offering insights into the necessity of glucose control in the human bloodstream to not impact the residence time (pharmacokinetic profile) and pharmacotherapeutic potential of HCTZ.
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Open AccessReview
Medicinal Use of Chicory (Cichorium intybus L.)
by
Łukasz Duda, Karol Kamil Kłosiński, Grażyna Budryn, Andrzej Jaśkiewicz, Damian Kołat, Żaneta Kałuzińska-Kołat and Zbigniew Włodzimierz Pasieka
Sci. Pharm. 2024, 92(2), 31; https://doi.org/10.3390/scipharm92020031 - 5 Jun 2024
Abstract
The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions.
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The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions. A comprehensive search of articles in Polish and English from 1986–2022 years was carried out in PubMed, Google Scholar and ScienceDirect using the keywords chicory, Cichorium intybus L., sesquiterpene lactones and their synonyms. Articles were checked for titles, abstracts, and full-text reviews. The first part of the review article discusses chicory, the countries in which it is found, its life cycle or modern cultivation methods, as well as its many uses, which will be discussed in more detail later in the article. The increased interest in plants as medicines or supplements is also briefly mentioned, as well as some limits that are associated with the medical use of plants. In the Results and Discussion section, there is a discussion of the numerous health-promoting properties of Cichorium intybus L. as a whole plant, with its collection of all the components, and we then examine the structure and the individual constituents of Cichorium intybus L. Among these, this article discusses those that can be utilized for causal applications in medicine, including sesquiterpene lactones and polyphenols, mainly known for their anti-cancer properties, although, in this article, their other health-promoting properties are also discussed. The article also examines inulin, a major component of Cichorium intybus L. The Discussion and the Conclusions sections propose directions for more detailed research and the range of factors that may affect specific results, which may have safety implications when used as supplements or medications.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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Open AccessArticle
Exposure to Benzo(a)pyrene Enhances Acetaminophen-Induced Liver Injury in Mice at Non-Hepatotoxic Doses
by
Yina Montero-Pérez and Jesus Olivero-Verbel
Sci. Pharm. 2024, 92(2), 30; https://doi.org/10.3390/scipharm92020030 - 3 Jun 2024
Abstract
Acetaminophen (APAP) is a widely used analgesic, especially for children. Its primary mechanism involves inhibiting cyclooxygenase enzymes and activating the endocannabinoid and TRPV1 systems. Though its toxicity is low, it can harm the liver in a dose-dependent manner. Low APAP doses can also
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Acetaminophen (APAP) is a widely used analgesic, especially for children. Its primary mechanism involves inhibiting cyclooxygenase enzymes and activating the endocannabinoid and TRPV1 systems. Though its toxicity is low, it can harm the liver in a dose-dependent manner. Low APAP doses can also increase pollutant-induced liver damage. Little is known about interactions between APAP and benzo[a]pyrene (B[a]P). This study aimed to assess if co-exposure to non-hepatotoxic doses of B[a]P and APAP causes liver injury in mice, exploring the underlying mechanisms. Female ICR mice received 50 mg/kg B[a]P or a vehicle for three days, followed by 200 mg/kg APAP or a vehicle. Liver injury was assessed through histopathological examination, serum transaminase activity, and gene expression analysis. In the B[a]P/APAP group, several histology changes were observed, including ballooning injury, steatosis, necrosis, inflammation, and apoptosis. Transaminase levels correlated with histopathological scores, and there was an increase in hepatic cytochrome P450 family 1 subfamily a member 1 (Cyp1a1) mRNA levels and a decrease in aryl hydrocarbon receptor (Ahr), cytochrome P450 family 2 subfamily e polypeptide 1 (Cyp2e1), superoxide dismutase 1 (Sod1), peroxisome proliferator activated receptor gamma (Ppar-γ), and caspase 3 (Casp3). This suggests that prior exposure to B[a]P makes mice more susceptible to APAP-induced liver injury, involving changes in gene expression related to metabolism, redox balance, and cell proliferation. Therefore, using therapeutic APAP doses after exposure to B[a]P could lead to liver injury.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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