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Keywords = naproxen sodium

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22 pages, 6643 KB  
Article
Analysis of the Effect of the Tablet Matrix on the Polymorphism of Ibuprofen, Naproxen, and Naproxen Sodium in Commercially Available Pharmaceutical Formulations
by Edyta Leyk, Marcin Środa, Gracjan Maślanka, Patrycja Nowaczyk, Amelia Orzołek, Hanna Grodzka, Aleksandra Kurek, Olaf Knut, Julia Michalak, Jonatan Płachciak and Alina Plenis
Methods Protoc. 2025, 8(5), 99; https://doi.org/10.3390/mps8050099 - 1 Sep 2025
Viewed by 2303
Abstract
Pharmaceutical formulations, in addition to the medicinal substance(s), contain added excipients that make it possible to create a pharmaceutical product that exhibits required properties in terms of mechanical, physical, chemical, and microbiological stability. Additionally, these substances can act as release modifiers or improve [...] Read more.
Pharmaceutical formulations, in addition to the medicinal substance(s), contain added excipients that make it possible to create a pharmaceutical product that exhibits required properties in terms of mechanical, physical, chemical, and microbiological stability. Additionally, these substances can act as release modifiers or improve bioavailability parameters. Literature data indicate that excipients, especially polymeric ones, can also affect the polymorphism of the active substance, resulting in drug bioavailability enhancement or reduction. This influence can be evaluated using thermal and spectroscopic methods. In the study, differential scanning calorimetry (DSC), vibrational spectroscopic studies (Fourier transform infrared spectroscopy, FTIR), Raman spectroscopy, and X-ray diffraction (XRD) assay of ibuprofen, naproxen, and naproxen sodium standards and pharmaceutical preparations containing these medicinal substances in their compositions were carried out. DSC results indicated that a sharp melting peak was observed on the DSC curves of the standards, confirming their crystalline form. DSC results obtained for pharmaceutical formulations also indicated that the enthalpy of melting is sometimes lower than calculated from the percentage of active ingredients in the formulations. In addition, the melting peak is often broadened and shifted toward lower temperatures, suggesting the influence of excipients on the polymorphism of drug substances. The FTIR and Raman spectra of pharmaceutical formulations contained all characteristics of the active substances. XRD analysis was also performed. Therefore, possible chemical interactions between the components of the preparations have been excluded. At the same time, FTIR and Raman spectroscopy results as well as XRD assay showed a reduction in the height of signals corresponding to the crystalline API form, confirming the possibility of reducing API crystallinity in pharmaceutical formulations. Full article
(This article belongs to the Special Issue Analytical Methods in Natural Sciences and Archaeometry)
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24 pages, 2229 KB  
Article
Effect of Mixing Technology on Homogeneity and Quality of Sodium Naproxen Tablets: Technological and Analytical Evaluation Using HPLC Method
by Mateusz Przywara, Regina Lech-Przywara, Patrycja Rupar and Wojciech Zapała
Molecules 2025, 30(15), 3119; https://doi.org/10.3390/molecules30153119 - 25 Jul 2025
Viewed by 1627
Abstract
The uniform distribution of APIs is essential in tablet formulations, particularly in direct compression, where powder blending is the only means of ensuring dose homogeneity. This study evaluated the influence of three mixing techniques—V-type mixer, planetary ball mill, and vibratory ball mill—on the [...] Read more.
The uniform distribution of APIs is essential in tablet formulations, particularly in direct compression, where powder blending is the only means of ensuring dose homogeneity. This study evaluated the influence of three mixing techniques—V-type mixer, planetary ball mill, and vibratory ball mill—on the physical properties and content uniformity of naproxen sodium tablets. Blends consisting of naproxen sodium, cellulose, PVP, calcium carbonate, and magnesium stearate were prepared under varied mixing intensities and characterized in terms of flowability, compressibility, and particle size distribution. The resulting tablets were analyzed for weight, thickness, hardness, friability, and API content using a simplified bypass HPLC method. The V-type mixer yielded tablets with the most consistent weight and thickness, despite the poorest blend flow properties. Vibratory milling produced the hardest tablets and best API content uniformity, although high-energy processing introduced variability at longer mixing times. The analytical method proved fast and robust, allowing for reliable API quantification without full chromatographic separation. These findings underscore the need to balance mechanical blending energy with formulation properties and support the use of streamlined analytical strategies in pharmaceutical development. Full article
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17 pages, 2694 KB  
Article
Evaluation of Vibratory Ball Mill Mixing as an Alternative to Wet Granulation in the Manufacturing of Sodium Naproxen Tablets with Dolomite-Based Formulations
by Mateusz Przywara, Klaudia Jękot and Wiktoria Jednacz
Appl. Sci. 2025, 15(13), 6966; https://doi.org/10.3390/app15136966 - 20 Jun 2025
Cited by 1 | Viewed by 1430
Abstract
The development of robust and scalable tablet manufacturing methods remains a key objective in pharmaceutical technology, especially when dealing with active pharmaceutical ingredients (APIs) and excipients that exhibit suboptimal processing properties. This study evaluated two alternative manufacturing strategies for tablets containing sodium naproxen [...] Read more.
The development of robust and scalable tablet manufacturing methods remains a key objective in pharmaceutical technology, especially when dealing with active pharmaceutical ingredients (APIs) and excipients that exhibit suboptimal processing properties. This study evaluated two alternative manufacturing strategies for tablets containing sodium naproxen (20%, API), dolomite (65%, sustainable mineral filler), cellulose (7%), polyvinylpyrrolidone (5%, binder), and magnesium stearate (3%, lubricant). The direct compression method used a vibrating ball mill (SPEX SamplePrep 8000M), while the indirect method employed wet granulation using a pan granulator at different inclination angles. Physical properties of raw materials and granules were assessed, and final tablets were evaluated for mass, thickness, mechanical resistance, abrasiveness, and API content uniformity. Direct compression using vibratory mixing for 5–10 min (DT2, DT3) resulted in average tablet masses close to the target (0.260 g) and improved reproducibility compared to a reference V-type blender. Wet granulation produced tablets with the lowest abrasiveness (<1.0%) and minimal variability in dimensions and API content. The best uniformity (SD < 0.5%) was observed in batch IT2. Overall, vibratory mixing proved capable of achieving tablet quality comparable to that of wet granulation, while requiring fewer processing steps. This highlights its potential as an efficient and scalable alternative in solid dosage manufacturing. Full article
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14 pages, 1955 KB  
Article
A Novel Recyclable Strategy for Extraction of Naproxen Sodium from Environmental Water by Amino-Functionalized Immobilized Ionic Liquid Polymers
by Hongrui Yang, Ayiguli Maimaiti, Wei Liu, Wenye Deng, Xiaoping Fu and Jing Fan
Molecules 2025, 30(11), 2404; https://doi.org/10.3390/molecules30112404 - 30 May 2025
Cited by 1 | Viewed by 979
Abstract
Naproxen sodium is an emerging pollutant that may pose potential hazards to human health and the ecological environment. However, developing highly effective adsorbents for the extraction of naproxen sodium from aqueous environments is still a challenge. Herein, we have prepared a novel amino-functional [...] Read more.
Naproxen sodium is an emerging pollutant that may pose potential hazards to human health and the ecological environment. However, developing highly effective adsorbents for the extraction of naproxen sodium from aqueous environments is still a challenge. Herein, we have prepared a novel amino-functional ionic liquid polymer adsorbent (NH2-IL-PS) for the extraction of naproxen sodium (NPS) from aqueous environments. It was found that the NH2-IL-PS exhibits a high adsorption capacity of 456.6 mg/g for NPS and maintains high extraction efficiency over a wide pH range of 4 to 9 at room temperature. Notably, even when the concentration of NPS was lower than 5 ppb, the extraction efficiency still exceeded 90.0%, with the enrichment factor reaching up to 600.0. More importantly, the NH2-IL-PS adsorbent material can withstand at least 16 consecutive adsorption cycles while maintaining an extraction efficiency of over 90.0%. Finally, the NH2-IL-PS was successfully applied to extract and determine NPS in seven types of real water samples, with relative recoveries ranging from 90.9 to 96.2%. The study of the adsorption mechanism reveals that electrostatic interactions, ion exchange, π-π stacking, and hydrogen bonding are crucial in the extraction of NPS. This study provides a sustainable strategy for the efficient extraction of NPS. Full article
(This article belongs to the Topic Application of Nanomaterials in Environmental Analysis)
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23 pages, 17284 KB  
Article
Preparation and Study of Physicochemical and Adsorption Properties of Alginate Composites
by Małgorzata Wasilewska, Sylwia Gubernat and Paulina Gil-Kulik
Materials 2025, 18(3), 629; https://doi.org/10.3390/ma18030629 - 30 Jan 2025
Cited by 1 | Viewed by 1809
Abstract
This paper presents the preparation and study of the properties of alginate materials, which were obtained on the basis of sodium alginate, activated carbon, cellulose, and calcium chloride. Alginate–carbon (AlgCa + C) and alginate–cellulose (AlgCa + Cel) composites, as well as pure calcium [...] Read more.
This paper presents the preparation and study of the properties of alginate materials, which were obtained on the basis of sodium alginate, activated carbon, cellulose, and calcium chloride. Alginate–carbon (AlgCa + C) and alginate–cellulose (AlgCa + Cel) composites, as well as pure calcium alginate (AlgCa) for comparative purposes, were obtained. Their textural (nitrogen adsorption/desorption isotherms), morphological (scanning electron microscopy), thermal (thermal analysis), and acid–base (pH drift method) properties, as well as the swelling index, were investigated. Additionally, to determine the adsorption properties, comprehensive equilibrium and kinetic studies of the adsorption of sodium salts of ibuprofen (IBP), diclofenac (D), and naproxen (NPX) from aqueous solutions on biocomposities were carried out. Adsorption isotherms were fitted using the Marczewski–Jaroniec isotherm equation (R2 = 0.941–0.988). Data on the adsorption rate were analyzed using simple kinetic equations, of which the best quality of fit was obtained using the multi-exponential equation (R2 − 1 = (3.9 × 10−4)–(6.9 × 10−4)). The highest obtained adsorption values were reached in systems with alginate–carbon composite and were 1.23 mmol/g for NPX, 0.81 mmol/g for D, and 0.43 mmol/g for IBP. The AlgCa + C material was characterized by a large specific surface area (1151 m2/g), a high degree of swelling (300%) and high resistance to high temperatures. Full article
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14 pages, 2556 KB  
Article
Electrical Conductivity as an Informative Factor of the Properties of Liposomal Systems with Naproxen Sodium for Transdermal Application
by Witold Musiał, Carla Caddeo, Alina Jankowska-Konsur, Giorgio Passiu, Tomasz Urbaniak, Maria Twarda and Adam Zalewski
Materials 2024, 17(22), 5666; https://doi.org/10.3390/ma17225666 - 20 Nov 2024
Cited by 2 | Viewed by 1835
Abstract
Liposomal preparations play an important role as formulations for transdermal drug delivery; however, the electrical conductivity of these systems is sparingly evaluated. The aim of the study was to outline the range of the values of electrical conductivity values that may be recorded [...] Read more.
Liposomal preparations play an important role as formulations for transdermal drug delivery; however, the electrical conductivity of these systems is sparingly evaluated. The aim of the study was to outline the range of the values of electrical conductivity values that may be recorded in the future pharmaceutical systems in the context of their viscosity. The electrical conductivity, measured by a conductivity probe of k = 1.0 cm−1, and the dynamic viscosity of liposomal and non-liposomal systems with naproxen sodium, embedded into a methylcellulose hydrophilic gel (0.25%), were compared with data from preparations without naproxen sodium in a range reflecting the naproxen sodium concentrations 0.1·10−2–9.5·10−2 mol/L. The specific conductivity covered a 1.5 μS·cm−1–5616.0 μS·cm−1 range, whereas the viscosity ranged from 0.9 to 9.4 mPa·s. The naproxen sodium highly influenced the electrical conductivity, whereas the dynamic viscosity was a moderate factor. The observed phenomena may be ascribed to the high mobility of sodium ions recruited from naproxen sodium and the relatively low concentrations of applied methylcellulose. The assembly of lecithin in liposomes may have lowered the specific conductivity of the systems with naproxen sodium. These measurements will be further developed for implementation as simple assays of the concentrations of active pharmaceutical ingredient in release experiments of preparations proposed for dermatological applications. Full article
(This article belongs to the Special Issue Functional Hydrogels: Design, Properties and Applications)
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15 pages, 1802 KB  
Article
Biopolymer-Based Hydrogel Incorporated with Naproxen Sodium and Lidocaine Hydrochloride for Controlled Drug Delivery
by Dorota Wójcik-Pastuszka, Karolina Stawicka and Witold Musiał
Polymers 2024, 16(10), 1353; https://doi.org/10.3390/polym16101353 - 10 May 2024
Cited by 5 | Viewed by 2525
Abstract
Sodium hyaluronate (HA) is a natural polysaccharide. This biopolymer occurs in many tissues of living organisms. The regenerating, nourishing, and moisturizing properties as well as the rheological properties of HA enable its application in the pharmaceutical industry as a carrier of medicinal substances. [...] Read more.
Sodium hyaluronate (HA) is a natural polysaccharide. This biopolymer occurs in many tissues of living organisms. The regenerating, nourishing, and moisturizing properties as well as the rheological properties of HA enable its application in the pharmaceutical industry as a carrier of medicinal substances. The aim of this work was to assess the release of naproxen sodium (Nap) in the presence of lidocaine hydrochloride (Lid) from the biopolymer-based hydrogels and to determine the respective kinetic parameters of this process. The possible interaction between the HA polysaccharide carrier and the selected drugs was also investigated. Three hydrogels containing Nap and Lid with different concentrations of the biopolymer were prepared. The release of Nap was studied by employing USP apparatus 5. The infrared study and differential scanning calorimetry analysis of physical mixtures and dried formulations were performed. The highest amount of Nap was released from the formulation with the lowest concentration of the biopolymer. The most representative kinetic model that described the dissolution of Nap was obtained through the Korsmeyer–Peppas equation. The release rate constants were in the range of 1.0 ± 0.1 × 10−2 min−n–1.7 ± 0.1 × 10−2 min−n. Lid did not influence the dissolution of Nap from the formulations tested; however, in the desiccated samples of assessed formulations, the interaction between the polysaccharide and both drugs was observed. Full article
(This article belongs to the Section Biobased and Biodegradable Polymers)
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19 pages, 4295 KB  
Article
Activated Carbons as Effective Adsorbents of Non-Steroidal Anti-Inflammatory Drugs
by Małgorzata Wasilewska and Elżbieta Grządka
Appl. Sci. 2024, 14(2), 743; https://doi.org/10.3390/app14020743 - 15 Jan 2024
Cited by 4 | Viewed by 2737
Abstract
In this study, the adsorption of naproxen sodium, ibuprofen sodium, and diclofenac sodium on activated carbon is investigated. Comprehensive studies of adsorption equilibrium and kinetics were performed using UV-Vis spectrophotometry. Thermal analysis and zeta potential measurements were also performed for pure activated carbon [...] Read more.
In this study, the adsorption of naproxen sodium, ibuprofen sodium, and diclofenac sodium on activated carbon is investigated. Comprehensive studies of adsorption equilibrium and kinetics were performed using UV-Vis spectrophotometry. Thermal analysis and zeta potential measurements were also performed for pure activated carbon and hybrid materials (activated carbon–drug) obtained after adsorption of naproxen sodium, ibuprofen sodium, and diclofenac sodium. The largest amount and rate of adsorption was demonstrated for naproxen sodium. A significant impact of temperature on the adsorption of the tested salts of non-steroidal anti-inflammatory drugs was also indicated. Faster kinetics and larger amounts of adsorption were recorded at higher temperatures. Thermodynamic parameters were also determined, based on which it was indicated that adsorption in the tested experimental systems is an endothermic, spontaneous, and thermodynamically privileged process of a physical nature. The generalized Langmuir isotherm was used to study the equilibrium data. The adsorption rate data were analyzed using numerous adsorption kinetics equations, including FOE, SOE, MOE, f-FOE-, f-SOE, f-MOE, and m-exp. Full article
(This article belongs to the Special Issue Advanced Research in Activated Carbon Adsorption)
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25 pages, 12356 KB  
Article
Application of TGA/c-DTA for Distinguishing between Two Forms of Naproxen in Pharmaceutical Preparations
by Paweł Ramos, Barbara Klaudia Raczak, Daniele Silvestri and Stanisław Wacławek
Pharmaceutics 2023, 15(6), 1689; https://doi.org/10.3390/pharmaceutics15061689 - 8 Jun 2023
Cited by 10 | Viewed by 4750
Abstract
Naproxen is one of the most used non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat pain of various origins, inflammation and fever. Pharmaceutical preparations containing naproxen are available with prescription and over-the-counter (OTC). Naproxen in pharmaceutical preparations is used in the form [...] Read more.
Naproxen is one of the most used non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat pain of various origins, inflammation and fever. Pharmaceutical preparations containing naproxen are available with prescription and over-the-counter (OTC). Naproxen in pharmaceutical preparations is used in the form of acid and sodium salt. From the point of view of pharmaceutical analysis, it is crucial to distinguish between these two forms of drugs. There are many costly and laborious methods to do this. Therefore, new, faster, cheaper and, at the same time, simple-to-perform identification methods are sought. In the conducted studies, thermal methods such as thermogravimetry (TGA) supported by calculated differential thermal analysis (c-DTA) were proposed to identify the type of naproxen in commercially available pharmaceutical preparations. In addition, the thermal methods used were compared with pharmacopoeial methods for the identification of compounds, such as high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FTIR), UV-Vis spectrophotometry, and a simple colorimetric analyses. In addition, using nabumetone, a close structural analog of naproxen, the specificity of the TGA and c-DTA methods was assessed. Studies have shown that the thermal analyses used are effective and selective in distinguishing the form of naproxen in pharmaceutical preparations. This indicates the potential possibility of using TGA supported by c-DTA as an alternative method. Full article
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22 pages, 3077 KB  
Article
Influence of HA on Release Process of Anionic and Cationic API Incorporated into Hydrophilic Gel
by Dorota Wójcik-Pastuszka, Karolina Stawicka, Andrzej Dryś and Witold Musiał
Int. J. Mol. Sci. 2023, 24(6), 5606; https://doi.org/10.3390/ijms24065606 - 15 Mar 2023
Cited by 12 | Viewed by 2961
Abstract
The properties of sodium hyaluronate (HA), such as hygroscopicity, flexibility, the ability to form hydrogels, as well as biocompatibility and biodegradability, are beneficial for the applications in pharmaceutical technology, cosmetics industry, and aesthetic medicine. The aim of this study was to prepare HA-based [...] Read more.
The properties of sodium hyaluronate (HA), such as hygroscopicity, flexibility, the ability to form hydrogels, as well as biocompatibility and biodegradability, are beneficial for the applications in pharmaceutical technology, cosmetics industry, and aesthetic medicine. The aim of this study was to prepare HA-based hydrogels doped with active pharmaceutical ingredient (API): a cationic drug—lidocaine hydrochloride or anionic drug—sodium. The interaction between the carrier and the implemented active pharmaceutical substances was evaluated in prepared systems by applying viscometric measurements, performing release tests of the drug from the obtained formulations, and carrying out FTIR and DSC. The data from release studies were analyzed using the zero-, first-, and second-order kinetics and Higuchi, Korsmeyer-Peppas, and Hixon-Crowell models. The respective kinetic parameters: the release rate constants, the half-release time and, in the case of the Korsmeyer-Peppas equation, the n parameter were calculated. The variability between the obtained release profiles was studied by calculating the difference (f1) and the similarity factor (f2) as well as employing statistical methods. It was revealed that the incorporation of the drugs resulted in an increase in the viscosity of the hydrogels in comparison to the respective drug-free preparations. The dissolution study showed that not entire amount of the added drug was released from the formulation, suggesting an interaction between the carrier and the drug. The FTIR and DSC studies confirmed the bond formation between HA and both medicinal substances. Full article
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22 pages, 1169 KB  
Article
Removal of Contaminants of Emerging Concern from Wastewater Using an Integrated Column System Containing Zero Valent Iron Nanoparticles
by Evridiki Barka, Constantinos Noutsopoulos, Andriani Galani, Iliana Panagou, Maria Kalli, Elena Koumaki, Simos Malamis and Daniel Mamais
Water 2023, 15(3), 598; https://doi.org/10.3390/w15030598 - 3 Feb 2023
Cited by 15 | Viewed by 5496
Abstract
Non-steroidal anti-inflammatory drugs (NSAIDs) and endocrine disruptors (EDCs) are among the most important categories of contaminants of emerging concern (CECs), and many advanced technologies have been developed for their elimination from water and wastewater, including nano-zero valent iron (nZVI). This study investigates the [...] Read more.
Non-steroidal anti-inflammatory drugs (NSAIDs) and endocrine disruptors (EDCs) are among the most important categories of contaminants of emerging concern (CECs), and many advanced technologies have been developed for their elimination from water and wastewater, including nano-zero valent iron (nZVI). This study investigates the performance of nZVI synthesized from green tea extracts and incorporated into a cationic resin (R-nFe) in the removal of four selected NSAIDs, namely ibuprofen (IBU), naproxen (NPX), diclofenac (DCF), and ketoprofen (KFN), and an EDC, namely bisphenol A (BPA). Column experiments were conducted to evaluate the effect of various operating parameters, including initial CECs concentration, contact time, pH, addition, and dose of sodium persulfate (PS). To the authors’ knowledge, this is the first time that environmentally friendly produced nZVI has been combined with PS in column experiments for the removal of CECs from wastewater. With a contact time of 2.2 min, PS = 1 mM, and influent pH = 3.5, 27–72% of IBU, 70–99% of NPX, 70–95% of DCF, 28–50% of KFN, and 61–91% of BPA were removed during a 12-day operation of the system, while the initial concentration of each substance was 5 μg/L. Therefore, it is anticipated that the proposed system could be a promising post-treatment technology for the removal of CECs from wastewater. Full article
(This article belongs to the Section Wastewater Treatment and Reuse)
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16 pages, 2979 KB  
Article
Simultaneous Voltammetric Determination of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Using a Modified Carbon Paste Electrode and Chemometrics
by Guadalupe Yoselin Aguilar-Lira, Jesús Eduardo López-Barriguete, Prisciliano Hernandez, Giaan Arturo Álvarez-Romero and Juan Manuel Gutiérrez
Sensors 2023, 23(1), 421; https://doi.org/10.3390/s23010421 - 30 Dec 2022
Cited by 13 | Viewed by 4309
Abstract
This work presents the simultaneous quantification of four non-steroidal anti-inflammatory drugs (NSAIDs), paracetamol, diclofenac, naproxen, and aspirin, in mixture solutions, by a laboratory-made working electrode based on carbon paste modified with multi-wall carbon nanotubes (MWCNT-CPE) and Differential Pulse Voltammetry (DPV). Preliminary electrochemical analysis [...] Read more.
This work presents the simultaneous quantification of four non-steroidal anti-inflammatory drugs (NSAIDs), paracetamol, diclofenac, naproxen, and aspirin, in mixture solutions, by a laboratory-made working electrode based on carbon paste modified with multi-wall carbon nanotubes (MWCNT-CPE) and Differential Pulse Voltammetry (DPV). Preliminary electrochemical analysis was performed using cyclic voltammetry, and the sensor morphology was studied by scanning electronic microscopy and electrochemical impedance spectroscopy. The sample set ranging from 0.5 to 80 µmol L−1 was prepared using a complete factorial design (34) and considering some interferent species such as ascorbic acid, glucose, and sodium dodecyl sulfate to build the response model and an external randomly subset of samples within the experimental domain. A data compression strategy based on discrete wavelet transform was applied to handle voltammograms’ complexity and high dimensionality. Afterward, Partial Least Square Regression (PLS) and Artificial Neural Networks (ANN) predicted the drug concentrations in the mixtures. PLS-adjusted models (n = 12) successfully predicted the concentration of paracetamol and diclofenac, achieving correlation values of R ≥ 0.9 (testing set). Meanwhile, the ANN model (four layers) obtained good prediction results, exhibiting R ≥ 0.968 for the four analyzed drugs (testing stage). Thus, an MWCNT-CPE electrode can be successfully used as a potential sensor for voltammetric determination and NSAID analysis. Full article
(This article belongs to the Section Chemical Sensors)
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25 pages, 5435 KB  
Article
Adsorption and Release Properties of Drug Delivery System Naproxen-SBA-15: Effect of Surface Polarity, Sodium/Acid Drug Form and pH
by Ľuboš Zauška, Eva Beňová, Martina Urbanová, Jiří Brus, Vladimír Zeleňák, Virginie Hornebecq and Miroslav Almáši
J. Funct. Biomater. 2022, 13(4), 275; https://doi.org/10.3390/jfb13040275 - 5 Dec 2022
Cited by 39 | Viewed by 4296
Abstract
Mesoporous silica SBA-15 was prepared via sol-gel synthesis and functionalized with different types of organosilanes containing various organic functional groups: (3-aminopropyl)triethoxysilane (SBA-15-NH2), (3-mercaptopropyl)triethoxysilane (SBA-15-SH), triethoxymethylsilane (SBA-15-CH3), triethoxyphenylsilane (SBA-15-Ph), and (3-isocynatopropyl)triethoxysilane (SBA-15-NCO). The prepared materials were investigated as drug delivery [...] Read more.
Mesoporous silica SBA-15 was prepared via sol-gel synthesis and functionalized with different types of organosilanes containing various organic functional groups: (3-aminopropyl)triethoxysilane (SBA-15-NH2), (3-mercaptopropyl)triethoxysilane (SBA-15-SH), triethoxymethylsilane (SBA-15-CH3), triethoxyphenylsilane (SBA-15-Ph), and (3-isocynatopropyl)triethoxysilane (SBA-15-NCO). The prepared materials were investigated as drug delivery systems for naproxen. As model drugs, naproxen acid (HNAP) and its sodium salt (NaNAP) were used. Mentioned medicaments belong to the group of non-steroidal anti-inflammatory drugs (NSAIDs). The prepared materials were characterized by different analytical methods such as transmission electron microscopy (TEM), infrared spectroscopy (IR), nitrogen adsorption/desorption analysis (N2), thermogravimetric analysis (TG), 1H, 13C and 23Na solid-state nuclear magnetic resonance spectroscopy (1H, 13C and 23Na ss-NMR). The abovementioned analytical techniques confirmed the successful grafting of functional groups to the SBA-15 surface and the adsorption of drugs after the impregnation process. The BET area values decreased from 927 m2 g−1 for SBA-15 to 408 m2 g−1 for SBA-15-NCO. After drug encapsulation, a more significant decrease in surface area was observed due to the filling of pores with drug molecules, while the most significant decrease was observed for the SBA-15-NH2 material (115 m2 g−1 for NaNAP and 101 m2 g−1 for HNAP). By combining TG and nitrogen adsorption results, the occurrence of functional groups and the affinity of drugs to the carriers’ surface were calculated. The dominant factor was the volume of functional groups and intermolecular interactions. The highest drug affinity values were observed for phenyl and amine-modified materials (SBA-15-Ph = 1.379 μmol m−2 mmol−1 for NaNAP, 1.761 μmol m−2 mmol−1 for HNAP and SBA-15-NH2 = 1.343 μmol m−2 mmol−1 for NaNAP, 1.302 μmol m−2 mmol−1 for HNAP) due to the formation of hydrogen bonds and π-π interactions, respectively. Drug release properties and kinetic studies were performed at t = 37 °C (normal human body temperature) in different media with pH = 2 as simulated human gastric fluid and pH = 7.4, which simulated a physiological environment. Determination of drug release quantity was performed with UV-VIS spectroscopy. The surface polarity, pH and naproxen form influenced the total released amount of drug. In general, naproxen sodium salt has a higher solubility than its acid form, thus significantly affecting drug release from surface-modified SBA-15 materials. Different pH conditions involved surface protonation and formation/disruption of intermolecular interactions, influencing both the release rate and the total released amount of naproxen. Different kinetic models, zero-order, first-order, Higuchi and Hixson–Crowell models, were used to fit the drug release data. According to the obtained experimental results, the drug release rates and mechanisms were determined. Full article
(This article belongs to the Special Issue Biomedical Applications of Mixed-Charge Nanomaterials)
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15 pages, 3558 KB  
Article
Constructing an Intelligent Model Based on Support Vector Regression to Simulate the Solubility of Drugs in Polymeric Media
by Sait Senceroglu, Mohamed Arselene Ayari, Tahereh Rezaei, Fardad Faress, Amith Khandakar, Muhammad E. H. Chowdhury and Zanko Hassan Jawhar
Pharmaceuticals 2022, 15(11), 1405; https://doi.org/10.3390/ph15111405 - 14 Nov 2022
Cited by 9 | Viewed by 2681 | Correction
Abstract
This study constructs a machine learning method to simultaneously analyze the thermodynamic behavior of many polymer–drug systems. The solubility temperature of Acetaminophen, Celecoxib, Chloramphenicol, D-Mannitol, Felodipine, Ibuprofen, Ibuprofen Sodium, Indomethacin, Itraconazole, Naproxen, Nifedipine, Paracetamol, Sulfadiazine, Sulfadimidine, Sulfamerazine, and Sulfathiazole in 1,3-bis[2-pyrrolidone-1-yl] butane, Polyvinyl [...] Read more.
This study constructs a machine learning method to simultaneously analyze the thermodynamic behavior of many polymer–drug systems. The solubility temperature of Acetaminophen, Celecoxib, Chloramphenicol, D-Mannitol, Felodipine, Ibuprofen, Ibuprofen Sodium, Indomethacin, Itraconazole, Naproxen, Nifedipine, Paracetamol, Sulfadiazine, Sulfadimidine, Sulfamerazine, and Sulfathiazole in 1,3-bis[2-pyrrolidone-1-yl] butane, Polyvinyl Acetate, Polyvinylpyrrolidone (PVP), PVP K12, PVP K15, PVP K17, PVP K25, PVP/VA, PVP/VA 335, PVP/VA 535, PVP/VA 635, PVP/VA 735, Soluplus analyzes from a modeling perspective. The least-squares support vector regression (LS-SVR) designs to approximate the solubility temperature of drugs in polymers from polymer and drug types and drug loading in polymers. The structure of this machine learning model is well-tuned by conducting trial and error on the kernel type (i.e., Gaussian, polynomial, and linear) and methods used for adjusting the LS-SVR coefficients (i.e., leave-one-out and 10-fold cross-validation scenarios). Results of the sensitivity analysis showed that the Gaussian kernel and 10-fold cross-validation is the best candidate for developing an LS-SVR for the given task. The built model yielded results consistent with 278 experimental samples reported in the literature. Indeed, the mean absolute relative deviation percent of 8.35 and 7.25 is achieved in the training and testing stages, respectively. The performance on the largest available dataset confirms its applicability. Such a reliable tool is essential for monitoring polymer–drug systems’ stability and deliverability, especially for poorly soluble drugs in polymers, which can be further validated by adopting it to an actual implementation in the future. Full article
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Case Report
Efficacy of Naproxen/Fexofenadine (SJP-003) in the Prevention of Side Effects of Influenza Vaccination: Four Case Studies
by Pantea Kiani, Thomas A. Dahl, Jacqueline M. Iversen, Andrew Scholey and Joris C. Verster
Clin. Pract. 2022, 12(5), 734-737; https://doi.org/10.3390/clinpract12050076 - 9 Sep 2022
Cited by 1 | Viewed by 3642
Abstract
The influenza virus is associated with sickness, and in particular among vulnerable populations such as elderly and those with underlying disease with hospitalization and increased mortality rates. Vaccination is an effective way to prevent infection with influenza. However, undesirable side effects of the [...] Read more.
The influenza virus is associated with sickness, and in particular among vulnerable populations such as elderly and those with underlying disease with hospitalization and increased mortality rates. Vaccination is an effective way to prevent infection with influenza. However, undesirable side effects of the vaccination are commonly experienced, and comprise one of the primary reasons for a substantial group of individuals to refrain from vaccination. An effective treatment against vaccination side effects could increase the overall willingness to vaccinate against influenza. Here, four cases are presented that self-administered SJP-003 (a combination of 220 mg naproxen sodium, directly followed by a single oral dose of 60 mg fexofenadine HCL), 2 h before and 10 h after influenza vaccination. No flu-like symptoms and pain at the injection site were reported. These observations warrant further investigation of SJP-003 in double-blind, placebo-controlled clinical trials. Full article
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