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1.
The production of biodegradable dressing capable of sustained drug release, along with the monitoring of wound conditions, represents new heights of multifunctional platforms for wound care. The reported curcumin-loaded silk fibroin has shown sustained drug release over the time of 10 days through a non-Fickian diffusion process satisfying Korsmeyer-Peppas' model along with the visual monitoring of wound healing through notable color variation with pH as a biomarker. The superhydrophobic nature (water contact angle = 163.7) of the SF, along with the lipophilicity (CA = 0 (Blood)) and hygroscopic nature prevents wetting of wound surface, whereas the excess exudates from wounds are absorbed along with sufficient water and oxygen permeability. The pH responsiveness as a result of the keto-enol tautomerism in curcumin was utilized for wound monitoring through visual indication enabling even ordinary people to detect the state of the wound. The in-situ biodegradation studies verified using cow-dung slurry, the degradability of the material with 25.3% weight loss within 30 days following first-order kinetics (R2 = 0.994), as a result of the attack of proteolytic enzymes on the amino acid units of SF, mitigating the concerns of medical wastes.  相似文献   

2.
Justicia vahlii Roth. (acanthaceae) is an important medicinal food plant used in pain relief and topical inflammation. The present study aimed to evaluate phytochemical composition, toxicity, anti-inflammatory, antioxidant and enzyme inhibition potential of n-butanol extract of J. vahlii (BEJv). The extract prepared through maceration was found rich in total phenolic contents (TPC) 196.08 ± 6.01 mg of Gallic acid equivalent (mg GAE/g DE) and total flavonoid contents (TFC) 59.08 ± 1.32 mg of Rutin equivalent (mg RE/g DE). The UPLC-Q-TOF-MS analysis of BEJv showed tentative identification of 87 compounds and 19 compounds were detected in GC–MS analysis. The HPLC-PDA quantification showed the presence of 14 polyphenols amongst which kaempferol (3.45 ± 0.21 µg/ mL DE) and ferulic acid (2.31 ± 1.30 µg/ mL DE) were found in highest quantity. The acute oral toxicity study revealed the safety and biocompatibility of the extract up to 3000 mg/kg in mice. There was no effect of BEJv on human normal liver cells (HL 7702) and very low cytotoxic effect on liver cancer cells (HepG2) and breast cancer cells (MCF-7). In anti-inflammatory evaluation, the BEJv treated groups showed significant inhibition (p < 0.001) of late phase carrageenan induced paw edema at 400 mg/kg and increased the levels of oxidative stress markers; catalase, superoxide dismutase (SOD) and glutathione (GSH) while decreased the inflammatory markers; interleukin-1beta (IL-β) and tumor necrosis factor alpha (TNF-α) in paw tissue of mice. BEJv displayed highest results in Ferric reducing antioxidant power (FRAP) assay 97. 21 ± 2.34 mg TE (trolox equivalent)/g DE, and highest activity 3.32 ± 0.31 mmol ACAE (acarbose equivalent)/g D.E against α-glucosidase. Docking study showed good docking score by the tested compounds against the various clinically significant enzymes. Conclusively the current study unveiled J. vahlii as novel non-toxic source with good antioxidant-mediated anti-inflammatory potential which strongly back the traditional use of the species in pain and inflammation.  相似文献   

3.
The impregnation of magnetite (Mt) nanoparticle (NPs) onto Musa acuminata peel (MApe), to form a novel magnetic combo (MApe-Mt) for the adsorption of anionic bromophenol blue (BPB) was studied. The SEM, EDX, BET, XRD, FTIR and TGA were used to characterize the adsorbents. The FTIR showed that the OH and CO groups were the major sites for BPB uptake onto the adsorbent materials. The average Mt crystalline size on MApe-Mt was 21.13 nm. SEM analysis revealed that Mt NPs were agglomerated on the surface of the MApe biosorbent, with an average Mt diameter of 25.97 nm. After Mt impregnation, a decrease in BET surface area (14.89 to 3.80 m2/g) and an increase in pore diameter (2.25–3.11 nm), pore volume (0.0052–0.01418 cm3/g) and pH point of zero charge (6.4–7.2) was obtained. The presence of Pb(II) ions in solution significantly decreased the uptake of BPB onto both MApe (66.1–43.8%) and MApe-Mt (80.3–59.1%), compared to other competing ions (Zn(II), Cd(II), Ni(II)) in the solution. Isotherm modeling showed that the Freundlich model best fitted the adsorption data (R2 > 0.994 and SSE < 0.0013). In addition, maximum monolayer uptake was enhanced from 6.04 to 8.12 mg/g after Mt impregnation. Kinetics were well described by the pseudo-first order and liquid film diffusion models. Thermodynamics revealed a physical, endothermic adsorption of BPB onto the adsorbents, with ΔHo values of 15.87–16.49 kJ/mol, corroborated by high desorption (over 90%) of BPB from the loaded materials. The viability of the prepared adsorbents was also revealed in its reusability for BPB uptake.  相似文献   

4.
The aim of the present study was to magnetize Plantago ovata Forssk. hydrogel and produce a nanosphere system to carrier mefenamic acid as the drug model. For this propose, P. ovata seeds hydrogel (POSH) was extracted and magnetized by Fe3O4 being functionalized using tetraethyl orthosilicate and trimethoxyvinysilane. Thereafter, mefenamic acid (MFA) was loaded on the carrier system. The final product, as the magnetic drug loaded nanosphere (Fe/POSH/MFA), was fully characterized through different techniques involving X-ray diffraction (XRD), scanning electron microscopy (SEM), vibrating-sample magnetometer (VSM), thermal gravimetric analysis (TGA), dynamic light scattering (DLS), and FT-IR spectroscopy. The results confirmed the successful production of the drug loaded nanosphere system with particles magnetization of 25 emu/g over a range size of 40–50 nm. However, the size distribution less than 100 nm was measured through DLS analysis. The hydrogel showed a pH sensitivity swelling behavior representing the best efficacy at pH 7.4. The efficiency of the drug encapsulation was found to be 64.35%. The drug releasing was studied using a dialysis bag at pH = 7.4. The highest in vitro drug releasing was found to be 57.3 ± 0.6% after 72 h, as well. The findings of the current report account for the potential use of P. ovata hydrogel as an effective delivery system for encapsulation of water insoluble basic drugs, e.g., MFA in a magnetized carrier system.  相似文献   

5.
Lepidium sativum is cultivated mainly for the edible oil from its seeds, and considered as an unutilized and neglected crop despite its important properties. Its oil fraction is used to produce soap and stabilize linseed oil when it is mixed with wild mustard seed oil. Once converted into fatty acid methyl esters, it represents a good substitute for imported petroleum diesel after alkaline transesterification reaction. In the current study, Lepidium sativum seeds cultivated in Tunisia and the physicochemical properties and nutrient profile of its cold pressed seed oil were investigated. The antioxidant, antibacterial, and anti-inflammatory activities of the above oil were also assessed. Lepidium sativum seed oil was abundant in both linolenic (35.59 ± 1.9%) and oleic (21.14 ± 0.63%) acids, and high amounts of β-sitosterol (42.57 ± 2.96 mg/100 g), campesterol (20.04 ± 1.4 mg/100 g) and Δ 5,24 stigmastadienol (11.82 ± 0.45 mg/100 g) were detected. The total tocopherol content of Lepidium sativum seed oil reached 136.83 ± 7.6 mg/100 g with a predominance of γ-tocopherol (86.23%). Its seed oil exhibited an IC50 of 10.33 ± 0.05 mg/mL and a radical scavenging activity of 415.6 ± 40 Trolox Equivalent Antioxidant Capacity (TEAC) for the DPPH and the ABTS assays, respectively. While the thermal analysis proved a high thermal stability of Lepidium sativum seed oil, that of eight bacteria and one fungal strain showed no noticeable bacterial or antifungal effects. It was also revealed that Lepidium sativum seed oil held a remarkable anti-inflammatory activity. Hence, the obtained results evidenced remarkable chemical, antioxidant and anti-inflammatory properties of Lepidium sativum seed oil, which might potentially be promising for enhancing human health and preventing age-related diseases.  相似文献   

6.
Inflammatory skin diseases (ISD) cause very severe itchy skin and dryness which is now a days an important issue which has to be taken care. Nanotechnology plays a main role in manufacturing cosmetic ingredients at a nanoscale size. Among different nanoparticles, gold (Au) is one of the non-toxic materials synthesized organically or inorganically. For synthesizing nanoparticles (NPs), using inorganic methods may cause some toxicity to cells, but using organic synthesis like plant extract is less toxic and environmentally friendly. Therefore, we synthesized DK-AuNPs using Diospyros kaki fruit extract. UPLC-MS/MS was used to evaluate phytochemicals responsible for converting salt into nanoparticles. The DK-AuNPs were characterized to confirm the formation of NPs. Furthermore, we analyzed the activity of DK-AuNPs on human keratinocytes (HaCaT cells). The DK-AuNPs showed 98.2 % cell survival upto 200 µg/mL against HaCaT cells. Additionally, compared to DK treatment, DK-AuNPs therapy decreased ROS production in TNF-α/IFN-γ (T + I) stimulated HaCaT cells by 68.7 %, whereas DK treatment reduced ROS generation by 27.8 %. Moreover, the skin anti-inflammatory potential and moisturizing effect of DK-AuNPs were analyzed using HaCaT cells. Furthermore, skin inflammatory activity biomarkers were downregulated through the MAPK/NFκB signaling pathway and showed significant inhibition by DK-AuNPs. Also, the skin moisturizing biomarkers such as HAS (1–3) were upregulated and HYAL (1–2) were downregulated by PI3K/AKT/NFκB through HAS2 regulation. Therefore, skin anti-inflammatory and moisturizing activity were enhanced by treatment with DK-AuNPs. In summary, we conclude that the DK-AuNPs could be a new alternative for skin disease.  相似文献   

7.
《Arabian Journal of Chemistry》2020,13(12):9145-9165
A series of novel 3, 4-dihydro-3-methyl-2(1H)-quinazolinone derivatives with substituted amine moieties (113) and substituted aldehyde (S) were designed and synthesized by a reflux condensation reaction in the presence of an acid catalyst to get N-Mannich bases. Mannich bases were evaluated pharmacologically for their antioxidant, α-amylase enzyme inhibition, antimicrobial, cell cytotoxicity and anti-inflammatory activities. Most of the compounds exhibited potent activities against these bioassays. Among them, SH1 and SH13 showed potent antioxidant activity against DPPH free radical at IC50 of 9.94 ± 0.16 µg/mL and 11.68 ± 0.32 µg/mL, respectively. SH7, SH10 and SH13 showed significant results in TAC and TRP antioxidant assays, comparable to that of ascorbic acid. SH2 and SH3 showed potent activity in inhibiting α-amylase enzyme at IC50 of 10.17 ± 0.23 µg/mL and 9.48 ± 0.17 µg/mL, respectively, when compared with acarbose (13.52 ± 0.19 µg/mL). SH7 was the most active against gram-positive and gram-negative bacterial strains, SH13 being the most potent against P. aeruginosa by inhibiting its growth up to 80% (MIC = 11.11 µg/mL). SH4, SH5 and SH6 exhibited significant activity against some fungal strains. Among the thirteen synthesized compounds (SH1-SH13), four were screened out based on the results of brine shrimp lethality assay (LD50) and cell cytotoxicity assay (IC50), to determine their anti-cancer potential against Hep-G2 cells. The study was conducted for 24, 48, and 72 h. SH12 showed potent results at IC50 of 6.48 µM at 72 h when compared with cisplatin (2.56 µM). An in vitro nitric oxide (NO) assay was performed to shortlist compounds for in vivo anti-inflammatory assay. Among shortlisted compounds, SH13 exhibited potent anti-inflammatory activity by decreasing the paw thickness to the maximum compared to the standard, acetylsalicylic acid (ASA).  相似文献   

8.
Libidibia ferrea (Mart. ex Tul.) L.P. Queiroz is a arboreal species found in the Caatinga from Northeast of Brazil that has been used in popular medicine as an anti-inflammatory, healing, analgesic and for the treatment of respiratory system disorders. Therefore, the objective of this work was to evaluate the composition of ethanol extracts from the leaves and inner bark of Libidibia ferrea, as well as to verify its antibacterial activity and as a potential inhibitor of the TetK efflux pump in Staphylococcus aureus strains, in addition to investigating the toxicity of the extracts in a Drosophila melanogaster model. The analysis and quantification of the extracts markers was performed by High Performance Liquid Chromatography (HPLC). To determine the Minimum Inhibitory Concentration (MIC) broth microdilution tests were carried out. The evaluation of efflux pump inhibition was performed by modifying the MIC of antibiotics and ethidium bromide. Mortality and negative geotaxis tests were used to verify the toxicity of extracts on D. melanogaster. Hydrolysable tannins (gallic acid and ellagic acid) and flavonoids were found in HPLC analysis. The extracts did not show antibacterial activity, demonstrating a MIC ≥ 1024 µg/mL, however the ethanolic extract of the leaves decreased the MIC of the antibiotic from 64 µg/mL to 16 µg/mL, but this effect is not associated with the inhibition of the efflux pump. The extracts did not show toxicity in a D. melanogaster model. This is the first study to evaluate the antibacterial activity of L. ferrea extracts on the IS-58 strain of S. aureus, as well as the first to investigate its toxicity using D. melanogaster. From the results, further studies are needed to determine the mechanisms of action of the extract with other antibiotics.  相似文献   

9.
This work investigated the effect of Potassium Permanganate (KMnO4) on graphene oxide (GO) properties, especially on electrical properties. The GO thin films were deposited on a glass substrate using drop casting technique and were analysed by using various type of spectroscopy (e.g. Scanning Electron Microscopy (SEM), Ultra- Violet Visible (UV–VIS), Fourier Transform Infrared (FTIR), X-Ray Diffraction (XRD), optical band gap, Raman Spectroscopy). Furthermore, the electrical experiments were carried out by using current–voltage (I-V) characteristic. The GO thin film with 4.5 g of KMnO4 resulted in higher conductivity which is 3.11 × 10?4 S/cm while GO with 2.5 g and 3.5 g of KMnO4 achieve 2.47 × 10?9 S/cm and 1.07 × 10?7 S/cm, respectively. This further affects the morphological (SEM), optical (band gap, UV–Vis, FTIR, and Raman), and crystalline structural (XRD) properties of the GO thin films. The morphological, elemental, optical, and structural data confirmed that the properties of GO is affected by different amount of KMnO4 oxidizing agent, which revealed that GO can potentially be implemented for electrical and electronic devices.  相似文献   

10.
Dioscorea nipponica Makino exhibits many biological activities, including relieving cough, eliminating phlegm and preventing asthma. The present study extensively evaluated the extraction process, major components, antioxidant, antibacterial and anti-inflammatory activities of total saponins extraction from Dioscorea nipponica Makino. In this study, the optimal extraction process of total saponins extract was optimized by single-factor test and response surface methodology as follows: extraction time 25 min, ethanol concentration 50 % and liquid to material ratio 55:1 ml/g, and the extraction rate was 1.72 %. Eighteen components were initially analyzed by UPLC-QTOF-MS method. Although total saponins extract exhibited mild antibacterial activities against Escherichia coli, Salmonella, Staphylococcus aureus and Streptococcus, and antioxidant activities against ferric-ion, ABTS and DPPH radicals, the perfect anti-inflammatory activity of TSE was demonstrated by significantly reducing the content of NO and the phagocytic activity in LPS induced RAW 264.7 cells, which provided a theoretical basis for the research and development of new anti-inflammatory Chinese medicine.  相似文献   

11.
Artemisia annua L. (A. annua) has been used as herbal medicine in China for thousands of years for clearing deficiency heat, treating malaria and removing jaundice. A rapid, sensitive and specific liquid chromatography coupled with electrospray ionization tandem mass spectrometry (LC–ESI–MS/MS) method was developed, validated, and successfully used for simultaneous quantification of the active components in rat plasma after oral administration of A. annua extract. Molecular docking of each component with drug metabolizing enzymes was carried out to explore the effect of each component on CYP-mediated drug metabolism. Two coumarins (scopolin (SPL) and scopoletin (SPLT)), three flavonoids (rutin (RUT), chrysosplenol D (CHD), casticin (CAS)) and three sesquiterpenes (arteannuin B (ARN), dihydroartemisinic acid (DARM) and artemisinic acid (ARM)) were detected in rat plasma after oral administration. CHD and CAS were rapidly absorbed into rat blood with the Tmax values of 0.11 ± 0.04 h and 0.13 ± 0.05 h, respectively. Their half-lives (t1/2 2.68 ± 3.62 h and 0.33 ± 0.07 h) were shorter. SPLT were also rapidly absorbed into the blood (Tmax 0.15 ± 0.03 h), but exhibited a longer half-life (t1/2 6.53 ± 1.84 h), indicating that it could be effective in vivo for a longer period of time. The peak time of SPL, RUT, DARM and ARM ranged from 1 ~ 4 h, demonstrating that they could maintain considerable concentrations for a longer time. ARN showed strong enterohepatic circulation in rats, leading to slower onset time and longer effect. A few components including SPLT, CHD, CAS and ARN could be metabolized into their corresponding II phase metabolites combining with glucuronic acid or sulfuric acid. RUT could decompose its glycosyl to generate genin. The molecular docking results indicated that those flavonoids and coumarins of A. annua interacting with CYPs mainly through hydrogen bonding and π-π stacking had better CYP450 enzyme binding ability than the sesquiterpenoids, which were easier to induce drug interactions. This study presented an integrated strategy for investigating the pharmacokinetic behaviors of eight components in A. annua and laid the foundation for revealing the mechanism of action of A. annua in the organism.  相似文献   

12.
《Arabian Journal of Chemistry》2020,13(10):7445-7452
Human alpha (α1)-acid glycoprotein (AGP) is an acute phase protein whose plasma concentration increases several-folds in the presence of various diseases. The variability in AGP plasma concentration is expected to have a huge impact on the drug binding equilibrium. Therefore, a precise measurement of AGP-drug binding is of great demand for drug development. In the current study, an ionic liquid-based aqueous two-phase system combined with affinity capillary electrophoresis (ILATPS/ACE) was utilised in order to improve the accuracy of AGP-drug binding analysis through the measurements of electrophoretic mobilities. The utilisation of ILATPS has shown to have a positive impact on the stability of AGP activity solution during the storage for an extended period of time. In addition, the effect of various alkyl chains (C2-C10) of imidazolium-based ILs with concentrations ranging between 10.00 and 1000.0 μmol L−1 on the AGP binding with the anti-cancer drugs chlorambucil (CHL) and dacarbazine (DAC) was examined by the system developed (ILATPS/ACE). A 100.00 μmol L−1 1-ethyl-3-methylimidazolium chloride (EMImCl) prepared in the physiological buffer conditions containing AGP (5.00–100.00 µmol L−1) has provided an accurate apparent binding constant of 1.99 ± 0.11 and 6.95 ± 0.14 L mmol−1 with CHL and DAC respectively. Apart from the ACE analysis, EMImCl/phosphate buffer solution was found to be a distinguished system that could lengthen the stability of AGP activity for a period of time reaching 90 days during the solution storage at 4.00 °C. This effect is thought to be due to the easy conversion of one-phase EMImCl/phosphate buffer/AGP at the ambient lab temperature into the two-phase solution at refrigerator temperature, 4.00 °C, and vice versa. Therefore, the ILATP/ACE system could be used to enhance the accuracy for other AGP-drug bindings with a fast, easy to use, and cost-effective analysis.  相似文献   

13.
A modified QuEChERS method (Quick, Easy, Cheap, Effective, Rugged, and Safe) for the determination of fifteen phenolic compounds in mustard greens (Brassica juncea) using ultra-high-performance liquid chromatography coupled to tandem mass spectrometry (UHPLC-MS/MS) analysis was developed. The QuEChERS partitioning step and dispersive solid phase extraction (d-SPE) clean-up sorbents were investigated, aimed at phenolic compound extraction and pigment removal, respectively. QuEChERS acetate version combined with 25 mg of diatomaceous earth (DE) and 5.0 mg of graphitized carbon black (GCB) provided the best conditions for sample preparation of the target compounds. Under the optimized conditions, all phenolic compounds showed good linearity (r ≥ 0.99) over the concentration range of 0.1 to 8000 μg kg−1, and the quantification limits were in the range of 0.06–230 μg kg−1. The spectrophotometric analysis showed that the clean-up step promoted a significant removal of chlorophyll, which is the major pigment present in the sample. Furthermore, antioxidant activity analysis was also carried out after the clean-up step and, together with chromatographic data, showed that no significant retention of the phenolic compounds occurs in the clean-up step. Two mustard greens varieties – Southern Giant Curled (SGC) and Florida Broadleaf (FB) - were analyzed with the proposed method. Seven phenolic compounds (4-hydroxybenzoic, p-coumaric, ferulic and sinapic acids, naringenin, apigenin and kaempferol) were found in both varieties, the greatest abundance being for sinapic acid (1261.5 ± 23 μg kg−1 in SGC and 1235.5 ± 26 μg kg−1 in FB) and ferulic acid (2861 ± 24 μg kg−1 in SGC and 3204.5 ± 45 μg kg−1 in FB).  相似文献   

14.
This paper presents the effect of infill patterns (IPs) on the mechanical response of 3D printed specimens by conducting the low-velocity impact test (LVI) and compression test. The poly-lactic acid (PLA, purity 98 wt% >) material has selected and printed using fused deposition modeling (FDM, speed 20 mm/s, layer height 0.2 mm, no of layers 30, extruded at 200 °C) with four different IPs: triangle, grid, quarter cubic, and tri-hexagon. The LVI test on velocity-time, energy-time and force-displacement, and the compression responses have examined and presented in this study. The LVI test was carried out to determine the penetration energy level, energy absorption capacity (toughness), stiffness, and strength of PLA porous parts (60% infill density) for implant/tissue/recyclable product applications. The results have shown that the triangular pattern has produced the highest absorbed energy in LVI test (penetration energy 7.5 J, and stiffness 668.82 N/mm) due to more sheared/contact layers’ perpendicular to impactor (hemispherical insert); while the grid pattern exhibited the highest compressive strength (72 MPa) due to more layers aligned along the compressive loading direction The SEM fracture surface image of Triangular IP has produced effective raster and layer bonding, less number of voids, more amount of circular beach markings, and absence of ratchet lines leading to possess improved mechanical properties.  相似文献   

15.
Silver nanoparticles (AgNPs) have attracted considerable attention owing to their unique biological applications. AgNPs synthesized by plant extract is considered as a convenient, efficient and eco-friendly material. In this work, the aqueous extract of Areca catechu L. nut (ACN) was used as the reducing and capping agents for one-pot synthesis of AgNPs, and their antioxidant and antibacterial activities were investigated. UV (Ultra Violet)-visible spectrum and dynamic light scattering (DLS) analysis revealed that the size of AgNPs was sensitive to the synthesis conditions. The synthesized AgNPs were composed of well-dispersed particles with an small size of about 10 nm under the optimal conditions (pH value of extract was 12.0; AgNO3 concentration was 1.0 mM; reaction time was 90 min). In addition, scanning electron microscope with energy dispersive X-ray (SEM-EDX), transmission electron microscopy (TEM) and X-ray diffraction (XRD) results further verified that the synthesized AgNPs had a stable and well-dispersed form (Zeta potential value of ?30.50 mV and polydispersity index of 0.328) and a regular spherical shape (average size of 15–20 nm). In addition, Fourier transform infrared spectrometry (FTIR) results revealed that phytochemical constituents in ACN aqueous extract accounted for Ag+ ion reduction, capping and stabilization of AgNPs. The possible reductants in the aqueous extract of Areca catechu L. nut were identified by high-performance liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry (HPLC-ESI-qTOF/MS) method. More importantly, the synthesized AgNPs indicated excellent free radical scavenging activity of 1,1-diphenyl-2-picrylhydrazyl (DPPH, IC50 = 11.75 ± 0.29 μg/mL) and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS+, IC50 = 44.85 ± 0.37 μg/mL), which were significant higher than that of ascorbic acid. Moreover, AgNPs exhibited an enhanced antibacterial activity against six selected common pathogens (especially Escherichia coli and Staphylococcus aureus) compared with AgNO3 solution. In a short, this study showed that the Areca catechu L. nut aqueous extract could be applied for eco-friendly synthesis of AgNPs.  相似文献   

16.
The glucocorticoid derivative of budesonide with a phthalimide group is a drug candidate to treat inflammatory eye diseases; nevertheless, it presents low water solubility. Drug nanocrystals have been proposed to overcome this hurdle. The development of an innovative ophthalmic anti-inflammatory nanosuspension was performed using a design space approach. We obtained the particle size reduction of this glucocorticoid derivative on a nanometer scale (approximately 165.0 nm), applying wet bead milling on a super reduced scale. The design of experiment supported the optimization of the formula evaluating the parameters that influence reducing the particle size and also allowed determining the design space. Considering the two statistical models developed and the size range obtained, we proposed that the optimized formulation for the glucocorticoid derivative nanosuspension may be 1.0 wt% glucocorticoid derivative and 0.092 wt% cetylpyridinium chloride. This formulation was characterized by the morphological, physical–chemical, and mucoadhesive in vitro test and showed potential for ophthalmic use with reduced frequency of product application, improved efficiency, and safety, which may promote better patient compliance.  相似文献   

17.
Double transesterification from vegetable oils could play an important role in biodiesel and biolubricant production, with the possible implementation of biorefineries to replace refineries based on petroleum. The oxidative stability of the original sample will influence the quality of the intermediate and final products, recommending highly stable raw materials or the use of antioxidants to keep quality parameters during storage. The aim of this work was to obtain a stable biolubricant, assessing its production through a double transesterification with methanol and pentaerythritol from high-oleic safflower oil and adding antioxidants, paying attention to quality parameters. Consequently, a biorefinery that produced high-quality products was proposed. In conclusion, high biodiesel and biolubricant yields were obtained (>97 and >94%, respectively) with the following chemical conditions for the latter: FAME/alcohol ratio, 1:0.33; pressure, 260 mmHg; catalyst concentration, 1.0%; temperature, 160 °C. The oxidative stability of biodiesel complied with the standard (10.78 h) due to its high methyl oleate content (exceeding 80%), whereas this parameter was shorter for the biolubricant (2.86 h), possibly due to its molecular structure. Consequently, antioxidant addition was needed, and tert-Butylhydroquinone at low concentration (500 ppm) kept viscosity and acid number of high-oleic safflower biolubricant during oxidation conditions (up to 8 h). However, tannic acid did not keep these properties in biolubricant. In conclusion, by using the right antioxidant, all the products of the proposed biorefinery were stable during oxidizing conditions, making this biorefinery more competitive.  相似文献   

18.
This study aimed to investigate the beneficial role of Millettia ferruginea extract (MF) in preventing cisplatin (Cisp) induced nephrotoxicity in rats. A total of 55 metabolites were identified using LC-MS analysis. The in vivo results indicated that MF pretreatment for 4 weeks (20 mg/kg b.w.) remarkably attenuated the altered renal biomarkers by decreasing the levels of plasma creatinine, urea, and uric acid when compared to the Cisp-group. The nephroprotective capacity of MF was further strengthened by histopathological observations, where Cisp + MF treated rats showed lower number of inflammatory cells and tubular degenerative changes than the Cisp-group. The harmful effects of cisplatin on renal oxidative stress indicators (MDA, SOD, CAT, and GPx), were restored by the treatment of MF. In addition, the reduction of inflammatory markers (IL-6 and TNF-α), associated with alleviating DNA fragmentation, highlighted the preventive effect of MF in kidney tissue. Additionally, MF components presented lower binding energies when docked into the active site of TNF-α and IL-6. The present findings concluded that M. ferruginea extract exhibited nephroprotective potential, which may be attributed to its antioxidant and anti-inflammatory properties. Further work is recommended to confirm the current results, explore the involved mechanism of action, and determine the therapeutic doses and time.  相似文献   

19.
Chilean Laureliopsis philippiana has been used in traditional medicine by the Mapuche and their ancestors. To evaluate its pharmacological activity, Laureliopsis philippiana leaf essential oil extract (LP_EO) was chemically and biologically characterized in the present study. In vitro antioxidant potential was analyzed, and antitumor activity was evaluated in non-tumor and tumor cell culture lines. Caenorhabditis elegans was used as a model for evaluating toxicity, and the chemical composition of the essential oil was analyzed using gas chromatography–mass spectrometry. The oil contains six major monoterpenes: eucalyptol (27.7 %), linalool (27.6 %), isozaphrol (19.5 %), isohomogenol (12.6 %), α-terpineol (7.7 %), and eudesmol (4.8 %). Based on quantum mechanical calculations, isosafrole and isohomogenol conferred in vitro antioxidant and antimicrobial activity to LP_EO. In addition, LP_EO showed antimicrobial activity against clinical Helicobacter pylori isolates (MIC 64 and MBC > 128 μg·mL?1), Staphylococcus aureus (MIC 32 and MBC > 64 μg·mL?1), Escherichia coli (MIC 8 and MBC 16 μg·mL?1) and Candida albicans (MIC 64 and > 128 μg·mL?1). LP_EO could selectively inhibit the proliferation of epithelial tumor cell lines but showed low toxicity against Caenorhabditis elegans (0.39 to 1.56 μg·mL?1). Therefore, LP_EO may be used as a source of bioactive compounds in novel pharmacological treatments for veterinary and human application, cosmetics, or sanitation.  相似文献   

20.
Capacitive Deionization (CDI) is an emerging technology with great potential applications. Most researchers view it as a viable water treatment alternative to reverse osmosis. This research reports the preparation and application of a carbon aerogel polypyrrole (CA-PPy) composite for the desalination of NaCl solution by the hybrid CDI method. The carbon aerogel (CA) was prepared from a Resorcinol / Formaldehyde precursor by the sol–gel method. The aerogel obtained from the sol–gel was then pyrolysed in a tube furnace to form CA. Polypyrrole (PPy) was prepared by the Oxidative chemical polymerisation of pyrrole, ferric chloride hexahydrate (oxidant), and sodium dodecyl sulfate (dopant). A composite of CA and PPy was then prepared and used to modify carbon electrodes. The CA-PPy composite was characterised to verify its composition, morphology, thermal properties, and functional groups. The electrochemical properties of the material were determined by Cyclic voltammetry (CV) and Electrochemical impedance spectroscopy (EIS) tests. The electrochemical tests were done using a GAMRY potentiostat electrochemical workstation, a 1.0 M KCl was used as the electrolyte, and the applied potential window was (-0.2 to + 0.6) V for the CV test. The EIS test was done with the same concentration of KCl electrolyte at an applied potential of 0.22 V and at a frequency range of (0.1 – 100, 000) Hz. The optimal specific capacitance of the CA is 115F/g, and that of the composite is 360.1F/g, they were both obtained at a scan rate of 5 mV/s. The CDI desalination study of the CA-PPy composite showed a salt adsorption capacity (SAC) of 10.10 mg/g (300 mg/L NaCl solution) – 15.7 mg/g (800 mg/L NaCl solution) at 1.2 V applied voltage. The salt recovery efficiency of the electrode material in the 300 mg/L solution is 27 %, in the 500 mg/L solution, it is 20.12 %, and in the 800 mg/L solution, it is 15.41 %. The electrode material also showed good electrochemical stability after nine cycles of ion adsorption/desorption study.  相似文献   

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