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
Identification of Potential Trypanosoma cruzi Trans-Sialidase Inhibitors by Computational Drug Repositioning Approaches
Sci. Pharm. 2024, 92(3), 40; https://doi.org/10.3390/scipharm92030040 (registering DOI) - 27 Jul 2024
Abstract
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
by
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
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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
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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
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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
by
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
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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
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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
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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.)
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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
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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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Open AccessArticle
Effect of Edge Activator Combinations in Transethosomal Formulations for Skin Delivery of Thymoquinone via Langmuir Technique
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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
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
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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.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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Open AccessReview
Drug Delivery Nano-Platforms for Advanced Cancer Therapy
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Ekaterina Naumenko, Ivan Guryanov and Marina Gomzikova
Sci. Pharm. 2024, 92(2), 28; https://doi.org/10.3390/scipharm92020028 - 22 May 2024
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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
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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.
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Open AccessArticle
Bioactive Components Analysis and Pharmacological Properties of Extracts and Metabolites of Lichen Umbilicaria crustulosa
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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
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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.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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Open AccessArticle
Advancing Transdermal Delivery by Zn/Ag-Electrode-Printed Iontophoretic Patch with Self-Generating Microcurrents
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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
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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
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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.
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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
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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
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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.
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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
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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.
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(This article belongs to the Topic Natural Products and Drug Discovery)
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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
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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.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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
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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.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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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
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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.
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(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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