| 1. |
- Aziz, Anam, et al.
(författare)
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Preparation and Evaluation of a Self-Emulsifying Drug Delivery System for Improving the Solubility and Permeability of Ticagrelor
- 2024
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Ingår i: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 9:9, s. 10522-10538
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Tidskriftsartikel (refereegranskat)abstract
- Ticagrelor (TCG) is a BCS class IV antiplatelet drug used to prevent platelet aggregation in patients with acute coronary syndrome, having poor solubility and permeability. The goal of this study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) of TCG to improve its solubility and permeability. The excipients were selected based on the maximum solubility of TCG and observed by UV spectrophotometer. Different combinations of oil, surfactant, and co-surfactant (1:1, 2:1, and 3:1) were used to prepare TCG-SNEDDS formulations, and pseudo-ternary phase diagrams were plotted. The nanoemulsion region was observed. Clove oil (10–20%), Tween-80 (45–70%), and PEG-400 (20–45%) were used as an oil, surfactant, and co-surfactant, respectively. The selected formulations (F1, F2, F3, F4, F5, and F6) were analyzed for ζ potential, polydispersity index (PDI), ζ size, self-emulsification test, cloud point determination, thermodynamic studies, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM), in vitro dissolution, ex vivo permeation, and pharmacodynamic study. The TCG-SNEDDS formulations exhibited ζ potential from −9.92 to −6.23 mV, a ζ average of 11.85–260.4 nm, and good PDI. The in vitro drug release in phosphate buffer pH 6.8 from selected TCG-SNEDDS F4 was about 98.45%, and F6 was about 97.86%, displaying improved dissolution of TCG in 0.1 N HCl and phosphate buffer pH 6.8, in comparison to 28.05% of pure TCG suspension after 12 h. While the in vitro drug release in 0.1 N HCl from F4 was about 62.03%, F6 was about 73.57%, which is higher than 10.35% of the pure TCG suspension. In ex vivo permeability studies, F4 also exhibited an improved apparent permeability of 2.7 × 10–6 versus 0.6708 × 10–6 cm2/s of pure drug suspension. The pharmacodynamic study in rabbits demonstrated enhanced antiplatelet activity from TCG-SNEDDS F4 compared to that from pure TCG suspension. These outcomes imply that the TCG-SNEDDS may serve as an effective means of enhancing TCG’s antiplatelet activity by improving the solubility and permeability of TCG.
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| 2. |
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| 3. |
- Björk, Emma
(författare)
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Surface Area Determination of Particle-Based Mesoporous Films Using Krypton Physisorption
- 2024
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Ingår i: ACS Omega. - : AMER CHEMICAL SOC. - 2470-1343. ; 9:5, s. 5899-5902
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Tidskriftsartikel (refereegranskat)abstract
- One of the key characteristics of mesoporous films, making them attractive in many applications, is the surface enhancement gained by the porosity. Today, this attribute is rarely presented for particle-based mesoporous films. This work shows that krypton physisorption can be used to determine the available surface area of particle-based silica films synthesized by the direct growth (DiG) method. The surface area per substrate area of the films was measured to be 50-170 m(2)/m(2) and the surface area per film volume was 310-490 m(2)/cm(3) when the film thickness was varied between 100 and 520 nm. For comparison, a 105 nm thick film synthesized using dip-coating was used, as this technique renders more smooth films. The corresponding values for the dip-coated film was 90 m(2)/m(2) and 880 m(2)/cm(3), showing a higher surface area per film volume for the continuous film. The method is hence suitable for the characterization of mesoporous films synthesized with various techniques and can be used for the optimization of catalysts, drug delivery systems, and sensors.
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| 4. |
- Eriksson, Axl, et al.
(författare)
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Synthesis of Well-Ordered Functionalized Silicon Microwires Using Displacement Talbot Lithography for Photocatalysis
- 2024
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Ingår i: ACS Omega. - 2470-1343. ; 9:18, s. 20623-20628
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Tidskriftsartikel (refereegranskat)abstract
- Metal-assisted chemical etching (MACE) is a cheap and scalable method that is commonly used to obtain silicon nano- or microwires but lacks spatial control. Herein, we present a synthesis method for producing vertical and highly periodic silicon microwires, using displacement Talbot lithography before wet etching with MACE. The functionalized periodic silicon microwires show 65% higher PEC performance and 2.3 mA/cm2 higher net photocurrent at 0 V compared to functionalized, randomly distributed microwires obtained by conventional MACE at the same potentials.
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| 5. |
- Frasca, Serena, et al.
(författare)
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Toward Biomass-Based Organic Electronics : Continuous Flow Synthesis and Electropolymerization of N-Substituted Pyrroles
- 2024
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Ingår i: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 9:12, s. 13852-13859
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Tidskriftsartikel (refereegranskat)abstract
- Pyrroles are foundational building blocks in a wide array of disciplines, including chemistry, pharmaceuticals, and materials science. Currently sourced from nonrenewable fossil sources, there is a strive to explore alternative and sustainable synthetic pathways to pyrroles utilizing renewable feedstocks. The utilization of biomass resources presents a compelling solution, particularly given that several key bulk and fine chemicals already originate from biomass. For instance, 2,5-dimethoxytetrahydrofuran and aniline are promising candidates for biomass-based chemical production. In this study, we present an innovative approach for synthesizing N-substituted pyrroles by modifying the Clauson-Kaas protocol, starting from 2,5-dimethoxytetrahydrofuran as the precursor. The developed methodology offers the advantage of producing pyrroles under mild reaction conditions with the potential for catalyst-free reactions depending upon the structural features of the substrate. We devised protocols suitable for both continuous flow and batch reactions, enabling the conversion of a wide range of anilines and sulfonamides into their respective N-substituted pyrroles with good to excellent yields. Moreover, we demonstrate the feasibility of depositing thin films of the corresponding polymers onto electrodes through in situ electropolymerization. This innovative application showcases the potential for sustainable, biomass-based organic electronics, thus, paving the way for environmentally friendly advancements in this field.
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| 6. |
- Hakim, M. Waqas, et al.
(författare)
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Enhanced Electrochemical Performance of MWCNT-Assisted Molybdenum-Titanium Carbide MXene as a Potential Electrode Material for Energy Storage Application
- 2024
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Ingår i: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 9:8, s. 8763-8772
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Tidskriftsartikel (refereegranskat)abstract
- Two-dimensional (2D) materials such as MXenes have attracted considerable attention owing to their enormous potential for structural flexibility. Here, we prepared a Mo2TiC2Tx-layered structure from parent Mo2TiAlC2Tx MAX by chemically selective etching of the aluminum layer. The prepared MXene was employed in composite formation with CTAB-grafted multiwalled carbon nanotubes (MWCNTs) to have a structure with improved electrochemical performance. The samples were characterized to analyze the structure, morphology, elemental detection, vibrational modes, and surface chemistry, followed by an electrochemical performance of the Mo2TiC2Tx MXene and MWCNTs@Mo2TiC2Tx composite using the GAMRAY Potentiostat under a 1 M KOH electrolyte. The specific capacitance of pristine Mo2TiC2Tx was 425 F g–1, which was enhanced to 1740 F g–1 (almost 4 times) at 5 mV s–1 due to the increase in active surface area and conductive paths between the MXene sheets. The charge storage mechanism was studied by further resolving the cyclic voltammograms. MWCNTs@Mo2TiC2Tx showed much improved electrochemical performance and reaction kinetics, making it an ideal material candidate for supercapacitor applications.
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| 7. |
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| 8. |
- Iversen, Alexandra, 1997-, et al.
(författare)
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Enzymatically Triggered Peptide–Lipid Conjugation of Designed Membrane Active Peptides for Controlled Liposomal Release
- 2024
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Ingår i: ACS Omega. - : American Chemical Society. - 2470-1343. ; 9:17, s. 19613-19619
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Tidskriftsartikel (refereegranskat)abstract
- Possibilities for controlling the release of pharmaceuticals from liposomal drug delivery systems can enhance their efficacy and reduce their side effects. Membrane-active peptides (MAPs) can be tailored to promote liposomal release when conjugated to lipid head groups using thiol-maleimide chemistry. However, the rapid oxidation of thiols hampers the optimization of such conjugation-dependent release strategies. Here, we demonstrate a de novo designed MAP modified with an enzyme-labile Cys-protection group (phenylacetamidomethyl (Phacm)) that prevents oxidation and facilitates in situ peptide lipidation. Before deprotection, the peptide lacks a defined secondary structure and does not interact with maleimide-functionalized vesicles. After deprotection of Cys using penicillin G acylase (PGA), the peptide adopts an α-helical conformation and triggers rapid release of vesicle content. Both the peptide and PGA concentrations significantly influence the conjugation process and, consequently, the release kinetics. At a PGA concentration of 5 μM the conjugation and release kinetics closely mirror those of fully reduced, unprotected peptides. We anticipate that these findings will enable further refinement of MAP conjugation and release processes, facilitating the development of sophisticated bioresponsive MAP-based liposomal drug delivery systems.
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| 9. |
- Kanellopoulos, Panagiotis, et al.
(författare)
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Two Novel [68Ga]Ga-Labeled Radiotracers Based on Metabolically Stable [Sar11]RM26 Antagonistic Peptide for Diagnostic Positron Emission Tomography Imaging of GRPR-Positive Prostate Cancer
- 2024
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Ingår i: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 9:16, s. 18608-18616
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Tidskriftsartikel (refereegranskat)abstract
- Gastrin releasing peptide receptor (GRPR) is overexpressed in prostate cancer (PC-3) and can be used for diagnostic purposes. We herein present the design and preclinical evaluation of two novel NOTA/NODAGA-containing peptides suitable for labeling with the positron emission tomography (PET) radionuclide Ga-68. These analogs are based on the previously reported GRPR-antagonist DOTAGA-PEG2-[Sar11]RM26, developed for targeted radiotheraostic applications. Both NOTA-PEG2-[Sar11]RM26 and NODAGA-PEG2-[Sar11]RM26 were successfully labeled with Ga-68 and evaluated in vitro and in vivo using PC-3 cell models. Both, [68Ga]Ga-NOTA-PEG2-[Sar11]RM26 and [68Ga]Ga-NODAGA-PEG2-[Sar11]RM26 displayed high metal-chelate stability in phosphate buffered saline and against the EDTA-challenge. The two [68Ga]Ga-labeled conjugates demonstrated highly GRPR-mediated uptake in vitro and in vivo and exhibited a slow internalization over time, typical for radioantagonistis. The [natGa]Ga-loaded peptides displayed affinity in the low nanomole range for GRPR in competition binding experiments. The new radiotracers demonstrated biodistribution profiles suitable for diagnostic imaging shortly after administration with fast background clearance. Their high tumor uptake (13 ± 1 and 15 ± 3% IA/g for NOTA and NODAGA conjugates, respectively) and high tumor-to-blood ratios (60 ± 10 and 220 ± 70, respectively) 3 h pi renders them promising PET tracers for use in patients. Tumor-to-normal organ ratios were higher for [68Ga]Ga-NODAGA-PEG2-[Sar11]RM26 than for the NOTA-containing counterpart. The performance of the two radiopeptides was further supported with the PET/CT images. In conclusion, [68Ga]Ga-NODAGA-PEG2-[Sar11]RM26 is a promising PET imaging tracer for visualization of GRPR-expressing lesions with high imaging contrast shortly after administration.
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| 10. |
- Larsson, Susanna, et al.
(författare)
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Proteome of Personalized Tissue-Engineered Veins
- 2024
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Ingår i: ACS Omega. - : American Chemical Society (ACS). - 2470-1343. ; 9:13, s. 14805-14817
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Tidskriftsartikel (refereegranskat)abstract
- Vascular diseases are the largest cause of death globally and impose a major global burden on healthcare. The gold standard for treating vascular diseases is the transplantation of autologous veins, if applicable. Alternative treatments still suffer from shortcomings, including low patency, lack of growth potential, the need for repeated intervention, and a substantial risk of developing infections. The use of a vascular ECM scaffold reconditioned with the patient's own cells has shown successful results in preclinical and clinical studies. In this study, we have compared the proteomes of personalized tissue-engineered veins of humans and pigs. By applying tandem mass tag (TMT) labeling LC/MS-MS, we have investigated the proteome of decellularized (DC) veins from humans and pigs and reconditioned (RC) DC veins produced through perfusion with the patient's whole blood in STEEN solution, applying the same technology as used in the preclinical studies. The results revealed high similarity between the proteomes of human and pig DC and RC veins, including the ECM texture after decellularization and reconditioning. In addition, functional enrichment analysis showed similarities in signaling pathways and biological processes involved in the immune system response. Furthermore, the classification of proteins involved in immune response activity that were detected in human and pig RC veins revealed proteins that evoke immunogenic responses, which may lead to graft rejection, thrombosis, and inflammation. However, the results from this study imply the initiation of wound healing rather than an immunogenic response, as both systems share the same processes, and no immunogenic response was reported in the preclinical and clinical studies. Finally, our study assessed the application of STEEN solution in tissue engineering and identified proteins that may be useful for the prediction of successful transplantations.
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