scholarly journals Electrospun Resveratrol-Loaded Polyvinylpyrrolidone/Cyclodextrin Nanofibers and Their Biomedical Applications

Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 552 ◽  
Author(s):  
Ying-Cheng Lin ◽  
Stephen Chu-Sung Hu ◽  
Pao-Hsien Huang ◽  
Tzu-Ching Lin ◽  
Feng-Lin Yen
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Skin Penetration ◽  
Aqueous Solubility ◽  
Amorphous Structure ◽  
Penetration Ability ◽  
Potential Applications ◽  
Anti Inflammatory ◽  
Franz Diffusion Cells

Resveratrol is a naturally occurring polyphenol compound which has been shown to possess antioxidant and anti-inflammatory properties. However, its pharmaceutical applications are limited by its poor water solubility. In this study, we used electrospinning technology to synthesize nanofibers of polyvinylpyrrolidone (PVP) and hydroxypropyl-β-cyclodextrin (HPBCD) loaded with resveratrol. We used X-ray diffractometry to analyze crystalline structure, Fourier transform infrared spectroscopy to determine intermolecular hydrogen bonding, antioxidant assays to measure antioxidant activity, and Franz diffusion cells to evaluate skin penetration. Our results showed that the aqueous solubility of resveratrol nanofibers was greatly improved (by more than 20,000-fold) compared to the pure compound. Analysis of physicochemical properties demonstrated that following nanofiber formation, resveratrol was converted from a crystalline to amorphous structure, and resveratrol formed new intermolecular bonds with PVP and HPBCD. Moreover, resveratrol nanofibers showed good antioxidant activity. In addition, the skin penetration ability of resveratrol in the nanofiber formulation was greater than that of pure resveratrol. Furthermore, resveratrol nanofibers suppressed particulate matter (PM)-induced expression of inflammatory proteins (COX-2 and MMP-9) in HaCaT keratinocytes. Therefore, resveratrol-loaded nanofibers can effectively improve the solubility and physicochemical properties of resveratrol, and may have potential applications as an antioxidant and anti-inflammatory formulation for topical skin application.

scholarly journals CF3-Substituted Mollugin 2-(4-Morpholinyl)-ethyl ester as a Potential Anti-inflammatory Agent with Improved Aqueous Solubility and Metabolic Stability

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2030
Author(s):  
Ki Hong ◽  
Darong Kim ◽  
Bo-Kyung Kim ◽  
Seo Woo ◽  
Ji Lee ◽  
...  
Keyword(s):  
Cell Adhesion ◽  
Ethyl Ester ◽  
Water Solubility ◽  
Aqueous Solubility ◽  
Plasma Stability ◽  
Inflammatory Agent ◽  
Colon Inflammation ◽  
Tnf Α ◽  
Monocyte Cell ◽  
Anti Inflammatory

Although mollugin, the main ingredient of the oriental medicinal herb Rubia cordifolia, has considerable anti-inflammatory effects, it has poor aqueous solubility as well as poor metabolic and plasma stability. To overcome these shortfalls, various mollugin derivatives have been synthesized and evaluated for their ability to inhibit U937 monocyte cell adhesion to HT-29 colonic epithelial cells in TNF-α- or IL-6-induced models of colon inflammation. The 2-(4-morpholinyl)-ethyl ester of CF3-substituted mollugin (compound 15c) showed good water solubility, improved metabolic and plasma stability, and greater inhibitory activity than mesalazine in both the TNF-α- and IL-6-induced colonic epithelial cell adhesion assays, suggesting that 15c is a potential anti-inflammatory agent.

scholarly journals Therapeutic Liquid Formulations Based on Low Transition Temperature Mixtures for the Incorporation of Anti-Inflammatory Drugs

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1620
Author(s):  
Ana Roda ◽  
Alexandre Paiva ◽  
Ana Rita C. Duarte
Keyword(s):  
Transition Temperature ◽  
Physicochemical Properties ◽  
Aqueous Solubility ◽  
Therapeutic Efficiency ◽  
Promising Tool ◽  
Solubility Improvement ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
L929 Mouse ◽  
State Of Art

Most nonsteroidal anti-inflammatory drugs (NSAIDs) present poor aqueous solubility, impairing their efficiency in physiological media. In this context, Low Transition Temperature Mixtures (LTTMs) are a promising platform to overcome drugs’ poor solubility, forming therapeutic liquid formulations. In this work, the LTTMs of citric acid:L-arginine:water (C:A:W) and glycerol:sorbitol (G:S) were studied in terms of their features and assessed in terms of their ability to increase the solubility of six NSAIDs in physiological media. The physicochemical properties of LTTMs were characterized by state-of-art techniques commonly used for these systems. The cytotoxicity of G:S was also evaluated in L929 mouse fibroblasts and the viscosity, polarity, and pH properties of the studied mixtures were related to the solubility of NSAIDs. The pH and polarity were the parameters that most influenced the drugs’ solubility. Ibuprofen, naproxen, ketoprofen, indomethacin, and flurbiprofen did not present any solubility improvement in the formulations tested. However, concentrated mixtures of C:A:W or G:S in the physiologic-mimicked media (PBS) rendered a celecoxib solubility 4 and 5 times higher than PBS, respectively. These therapeutic liquid formulations of celecoxib in C:A:W or G:S can be a promising tool to increase celecoxib’s therapeutic efficiency in local applications.

scholarly journals What makes flunisolide different among inhaled corticosteroids used for nebulization: a close look at the role of aqueous solubility

2021 ◽  
Vol 16 ◽  
Author(s):  
Ahmad Kantar
Keyword(s):  
Fluticasone Propionate ◽  
Physicochemical Properties ◽  
Beclomethasone Dipropionate ◽  
Water Solubility ◽  
Inhaled Corticosteroids ◽  
Aqueous Solubility ◽  
Pharmacokinetic Profile ◽  
The Elderly ◽  
Metered Dose

Evidence-based management of bronchial asthma and wheezing in children and adults recommends the employment of inhaled corticosteroids (ICSs). Difficulty in using some inhalation devices for ICS delivery, such as pressurized metered-dose and dry-powder inhalers, is common among young children and in the elderly, and for that reason, they are replaced with nebulizers. We reviewed comparative studies that evaluated funisolide with other ICSs currently available on the market, including beclomethasone dipropionate, fluticasone propionate, and budesonide. Moreover, we assessed the physicochemical properties of these ICSs in determining drug fate in the lung. Data indicate that the flunisolide output in respirable particles by any type of pneumatic nebulizer (traditional, open breath or breath-enhanced) is superior to the output of other ICSs. This is principally attributed to the higher water solubility of flunisolide. Furthermore, in vivo simulation studies demonstrate that the intersubject variability of the inhaled dose among asthmatic children was much greater for suspensions of fluticasone propionate and beclomethasone dipropionate than for those of flunisolide. The physicochemical properties and pharmacokinetic profile of flunisolide favor its employment in nebulization.

scholarly journals Oleanolic Acid Nanofibers Attenuated Particulate Matter-Induced Oxidative Stress in Keratinocytes

Antioxidants ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1411
Author(s):  
Hsuan Fu ◽  
Feng-Lin Yen ◽  
Pao-Hsien Huang ◽  
Chun-Yin Yang ◽  
Chia-Hung Yen
Keyword(s):  
Oxidative Stress ◽  
Particulate Matter ◽  
Oleanolic Acid ◽  
Water Solubility ◽  
Airborne Particulate Matter ◽  
Skin Penetration ◽  
Skin Aging ◽  
Particle Size Reduction ◽  
Amino Terminal ◽  
Penetration Ability

Airborne particulate matter (PM) is one of the indicators of air pollution, and it is also the main factor causing oxidative stress in the skin. Oleanolic acid (OA), a natural terpenoid compound, effectively inhibited PM-induced skin aging; however, OA has poor water solubility and skin absorption, which limit its application in medicines and cosmetics. The aim of this study was to prepare oleanolic acid nanofibers (OAnf) and evaluate the effects of OA and OAnf in PM-treated keratinocytes. The results showed that OA dissolved in dissolved in dimethyl sulfoxide (DMSO) attenuated PM-induced reactive oxygen species overproduction, stress-activated protein kinase/Jun-amino-terminal kinase (SAPK/JNK) activation, and the expressions of inflammatory and skin-aging-related proteins. In addition, the nanofiber process of OA effectively improved the water solubility of OA more than 99,000-fold through changing its physicochemical properties, including a surface area increase, particle size reduction, amorphous transformation, and hydrogen bonding formation with excipients. The skin penetration ability of OAnf was consistently over 10-fold higher than that of OA. Moreover, when dissolved in PBS, OAnf displayed superior antioxidant, anti-inflammatory, and anti-skin aging activities in PM-treated keratinocytes than OA. In conclusion, our findings suggest that OAnf could be a topical antioxidant formulation to attenuate skin problems caused by PM.

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

Physicochemical Characterization and Antinociceptive Effect of β-cyclodextrin/Lippia pedunculosa Essential Oil in Mice

2018 ◽  
Vol 18 (9) ◽  
pp. 797-807 ◽  
Author(s):  
Paula dos Passos Menezes ◽  
Francielly de Oliveira Araujo ◽  
Tatianny Araujo Andrade ◽  
Igor Araujo Santos Trindade ◽  
Heitor Gomes de Araujo-Filho ◽  
...  
Keyword(s):  
Essential Oil ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Physicochemical Characterization ◽  
Good Tool ◽  
Main Challenge ◽  
Higher Temperature

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.

Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity

2020 ◽  
Vol 16 ◽  
Author(s):  
Bhim Bahadur Chaudhari ◽  
Alka Bali ◽  
Ajitesh Balaini
Keyword(s):  
Antioxidant Activity ◽  
Oral Absorption ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Antioxidant Potential ◽  
Inflammatory Activity ◽  
In Vivo Models ◽  
Standard Drug ◽  
Hybrid Molecules ◽  
Anti Inflammatory

Background: NSAIDs are the most widely prescribed medications worldwide for their anti-inflammatory, antipyretic, and analgesic effects However, their chronic use can lead to several adverse drug events including GI toxicity. The selective COX-2 inhibitors developed as gastro-sparing NSAIDs also suffer from serious adverse effects which limit their efficacy. Objective: Local generation of reactive oxygen species is implicated in NSAID-mediated gastric ulceration and their combination with H2 antagonists like famotidine reduces the risk of ulcers. The objective of this work was to design and synthesize novel methanesulphonamido isoxazole derivatives by hybridizing the structural features of NSAIDs with those of antiulcer drugs (ranitidine, famotidine, etc.) to utilize a dual combination of anti-inflammatory activity and reducing (antioxidant) potential. Method: The designing process utilized three dimensional similarity studies and utilized an isoxazole core having a potential for anti-inflammatory as well as radical scavenging antioxidant activity. The compounds were assayed for their antiinflammatory activity in established in vivo models. The in vitro antioxidant activity was assessed in potassium ferricyanide reducing power (PFRAP) assay employing ascorbic acid as the standard drug. Results: Compounds (5, 6, 9 and 10) showed anti-inflammatory activity comparable to the standard drugs and were also found to be non-ulcerogenic at the test doses. Compounds 6-10 exhibited good antioxidant effect in the concentration range of 1.0-50.0 µmol/ml. The test compounds were also found to comply with the Lipinski rule suggesting good oral absorption. Conclusion: A new series of isoxazole based compounds is being reported with good anti-inflammatory activity coupled with antioxidant potential as gastro-sparing anti-inflammatory agents.

scholarly journals Phytochemical, Antioxidant and Toxicological Investigation of Morinda citrifolia L. Blossoms

2012 ◽  
Vol 2012 ◽  
pp. 1-5 ◽  
Author(s):  
Shixin Deng ◽  
Brett J. West ◽  
'Afa K. Palu ◽  
C. Jarakae Jensen
Keyword(s):  
Antioxidant Activity ◽  
Iridoid Glycosides ◽  
Radical Scavenging ◽  
Morinda Citrifolia ◽  
Preliminary Evaluation ◽  
Medicinal Uses ◽  
Potential Applications ◽  
History Of ◽  
Toxicological Investigation ◽  
Phytochemical Components

Noni blossoms have a long history of medicinal uses in tropical areas. This study was conducted to investigate the major phytochemical components, toxicological properties, and antioxidant activity of noni blossoms. An HPLC-PDA method was developed and validated for the identification and quantification of major components. The major phytochemicals were iridoid glycosides, deacetylasperulosidic acid and asperulosidic acid, and flavonoids, quercetin-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside and kaempferol-3-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside, each present at 3.764, 3.576, 1.513, and 3.096 mg/g, respectively. The aqueous extract of noni blossoms, at 500 μg/mL, exhibited greater antioxidant activity in the 2,2-diphenylpicrylhydrazyl radical scavenging assay than green tea (88.11 ± 0.01% versus 76.60 ± 0.05%). A primary DNA damage test in E. coli PQ37 (SOS-chromotest) and a twenty-four hour brine shrimp toxicity test did not reveal any genotoxic or cytotoxic activity. These results provide a useful reference for the identification of noni blossoms as well as preliminary evaluation of safety and efficacy. Further evaluation of the potential applications of noni blossoms is warranted.

scholarly journals Relationships Linking the Colour and Elemental Concentrations of Blossom Honeys with Their Antioxidant Activity: A Chemometric Approach

Agriculture ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 702
Author(s):  
Monika Kędzierska-Matysek ◽  
Anna Teter ◽  
Małgorzata Stryjecka ◽  
Piotr Skałecki ◽  
Piotr Domaradzki ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Physicochemical Properties ◽  
Black Locust ◽  
Antioxidant Properties ◽  
Principal Component ◽  
Botanical Origin ◽  
Antioxidant Parameters ◽  
Colour Parameters ◽  
Hue Angle ◽  
Chemometric Approach

The antioxidant activity of honey depends on the botanical origin, which also determines their physicochemical properties. In this study, a multivariate analysis was used to confirm potential relationships between the antioxidant properties and colour parameters, as well as the content of seven elements in five types of artisanal honey (rapeseed, buckwheat, linden, black locust, and multifloral). The type of honey was found to significantly influence most of its physicochemical properties, colour parameters, and the content of potassium, manganese and copper. Antioxidant parameters were shown to be significantly positively correlated with redness and concentrations of copper and manganese, but negatively correlated with the hue angle and lightness. The principal component analysis confirmed that the darkest buckwheat honey had the highest antioxidant activity in combination with its specific colour parameters and content of antioxidant minerals (manganese, copper and zinc). The level of these parameters can be potentially used for the identification of buckwheat honey.

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