scholarly journals Development and In Vivo Evaluation of Multidrug Ultradeformable Vesicles for the Treatment of Skin Inflammation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 644 ◽  
Author(s):  
Roberto Molinaro ◽  
Agnese Gagliardi ◽  
Antonia Mancuso ◽  
Donato Cosco ◽  
Mahmoud E. Soliman ◽  
...  
Keyword(s):  
Inflammatory Diseases ◽  
Sodium Deoxycholate ◽  
Skin Inflammation ◽  
Biological Properties ◽  
In Vivo Evaluation ◽  
Drug Concentrations ◽  
Anti Inflammatory ◽  
Transdermal Route ◽  
Inflammatory Effect

The aim of this work was to evaluate the effect of two chemically different edge activators, i.e., Tween® 80 and sodium deoxycholate, on (i) the physical, mechanical, and biological properties of ultradeformable vesicles, and (ii) the administration of naproxen sodium-loaded multidrug ultradeformable vesicles for the transdermal route in order to obtain therapeutically meaningful drug concentrations in the target tissues and to potentiate its anti-inflammatory effect by association with the antioxidant drug idebenone. The results obtained in this investigation highlighted a synergistic action between naproxen and idebenone in the treatment of inflammatory disease with a more pronounced anti-inflammatory effect in multidrug ultradeformable vesicles compared to the commercial formulation of Naprosyn® gel. Systems made up of Tween® 80 appeared to be the most suitable in terms of percutaneous permeation and anti-inflammatory activity due to the greater deformability of these vesicles compared to multidrug ultradeformable vesicles with sodium deoxycholate. Our findings are very encouraging and suggest the use of these carriers in the topical treatment of inflammatory diseases.

scholarly journals Anti-Inflammatory Effect of Mallotus Philippinensis Bark Extracts in a Mouse Atopic Dermatitis Model

2020 ◽  
Vol 7 (1) ◽  
pp. 1-8
Author(s):  
Sae Asayama ◽  
Ayaka Iwasaki ◽  
Shunya Sahara ◽  
Koichi Nakaoji ◽  
Masamitsu Ichihashi ◽  
...  
Keyword(s):  
Atopic Dermatitis ◽  
Inflammatory Diseases ◽  
Radical Scavenging ◽  
Skin Inflammation ◽  
In Vivo Model ◽  
Anti Inflammatory ◽  
Anti Inflammation ◽  
Inflammatory Effect

Background: Atopic Dermatitis (AD) is a chronic inflammatory skin disease that causes functional disruption of the skin barrier. We previously found that ethanol Extracts of Mallotus Philippinensis Bark (EMPB) promoted migration of mesenchymal stem cells and improved wound healing probably through anti-inflammatory action. However, direct evidence of the anti-inflammatory effect of EMPB and the underlying mechanisms of this action remain unknown. In the present study, we evaluated whether EMPB has an effective action on anti-inflammation using an in vitro and in vivo model. We found that topical application of EMPB improved house dust miteinduced AD-like skin inflammation in NC/Nga mice. In addition, EMPB significantly inhibited various kinds of inflammatory mediators such as interleukin-1ß, inducible nitric oxide synthases, and nuclear factorkappa B in lipopolysaccharide-stimulated macrophage cells. Moreover, EMPB exhibited marked radical scavenging ability. Taken together, these results suggest that EMPB may be useful in the treatment of skin inflammatory diseases such as AD. Keywords: Mallotus Philippinensis Bark; Anti-Inflammation; Atopic Dermatitis; Macrophages

scholarly journals Betulinic Acid-Azaprostanoid Hybrids: Synthesis and Pharmacological Evaluation as Anti-inflammatory Agents

2020 ◽  
Vol 19 (3) ◽  
pp. 254-267
Author(s):  
Tatyana S. Khlebnicova ◽  
Yuri A. Piven ◽  
Fedor A. Lakhvich ◽  
Iryna V. Sorokina ◽  
Tatiana S. Frolova ◽  
...  
Keyword(s):  
Cell Lines ◽  
Betulinic Acid ◽  
Inflammatory Diseases ◽  
Toxic Agent ◽  
Analgesic Effects ◽  
Low Toxic ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Background: Prevention and treatment of chronic inflammatory diseases require effective and low-toxic medicines. Molecular hybridization is an effective strategy to enhance the biological activity of new compounds. Triterpenoid scaffolds are in the focus of attention owing to their anti-inflammatory, antiviral, antiproliferative, and immunomodulatory activities. Heteroprostanoids have different pleiotropic effects in acute and chronic inflammatory processes. Objective: The study aimed to develop structurally new and low toxic anti-inflammatory agents via hybridization of betulinic acid with azaprostanoic acids. Methods: A series of betulinic acid-azaprostanoid hybrids was synthesized. The synthetic pathway included the transformation of betulin via Jones' oxidation into betulonic acid, reductive amination of the latter and coupling obtained by 3β-amino-3-deoxybetulinic acid with the 7- or 13-azaprostanoic acids and their homo analogues. The hybrids 1-9 were investigated in vivo on histamine-, formalin- and concanavalin A-induced mouse paw edema models and two models of pain - the acetic acid-induced abdominal writhing and the hotplate test. The hybrids were in vitro evaluated for cytotoxic activity on cancer (MCF7, U- 87 MG) and non-cancer humane cell lines. Results: In the immunogenic inflammation model, the substances showed a pronounced anti-inflammatory effect, which was comparable to that of indomethacin. In the models of the exudative inflammation, none of the compounds displayed a statistically significant effect. The hybrids produced weak or moderate analgesic effects. All the agents revealed low cytotoxicity on human immortalized fibroblasts and cancer cell lines compared with 3β- amino-3-deoxybetulinic acid and doxorubicin. Conclusion: The results indicate that the principal anti-inflammatory effect of hybrids is substantially provided with the triterpenoid scaffold and in some cases with the azaprostanoid scaffold, but the latter makes a significant contribution to reducing the toxicity of hybrids. Hybrid 1 is of interest as a potent low toxic agent against immune-mediated inflammation.

Antinociceptive and Anti-Inflammatory Activities ofCuscuta chinensisSeeds in Mice

2014 ◽  
Vol 42 (01) ◽  
pp. 223-242 ◽  
Author(s):  
Jung-Chun Liao ◽  
Wen-Te Chang ◽  
Meng-Shiou Lee ◽  
Yung-Jia Chiu ◽  
Wei-Kai Chao ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Inflammatory Diseases ◽  
Antinociceptive Effect ◽  
Inflammatory Mechanism ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Highly Correlated ◽  
Cuscuta Chinensis ◽  
Inflammatory Effect

The seeds of Cuscuta chinensis, Cuscutae Semen, are commonly used as a medicinal material for treating the aching and weakness of the loins and knees, tonifying the defects of the liver and the kidney, and treating the diarrhea due to hypofunction of the kidney and the spleen. Since aching and inflammation are highly correlated with such diseases, the aim of this study is to investigate the possible antinociceptive and anti-inflammatory mechanisms of the seeds of C. chinensis. The antinociceptive effect of the seeds of C. chinensis was evaluated via the acetic acid-induced writhing response and formalin-induced paw licking methods. The anti-inflammatory effect was evaluated via the λ-carrageenan induced mouse paw edema method. The results found that 100 and 500 mg/kg of the methanol extract of the seeds of C. chinensis( CCMeOH) significantly decreased (p < 0.01 and p < 0.001, respectively) the writhing response in the acetic acid assay. Additionally, 20–500 mg/kg of CCMeOHsignificantly decreased licking time at the early (20 and 100 mg/kg, p < 0.001) and late phases (100 mg/kg, p < 0.01; 500 mg/kg, p < 0.001) of the formalin test, respectively. Furthermore, CCMeOH(100 and 500 mg/kg) significantly decreased (p < 0.01 and p < 0.001, respectively) edema paw volume four hours after λ-carrageenan had been injected. The results in the following study also revealed that the anti-inflammatory mechanism of CCMeOHmay be due to declined levels of NO and MDA in the edema paw by increasing the activities of SOD, GPx and GRd in the liver. In addition, CCMeOHalso decreased IL-1β, IL-6, NF-κB, TNF-α, and COX-2 levels. This is the first study to demonstrate the possible mechanisms for the antinociceptive and anti-inflammatory effects of CCMeOHin vivo. Thus, it provides evidence for the treatment of Cuscutae Semen in inflammatory diseases.

scholarly journals In Vivo Evaluation of the Anti-Inflammatory Effect ofPistacia lentiscusFruit Oil and Its Effects on Oxidative Stress

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Sameh Ben Khedir ◽  
Masarra Mzid ◽  
Sana Bardaa ◽  
Dorsaf Moalla ◽  
Zouheir Sahnoun ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
New Drugs ◽  
Inflammatory Activity ◽  
Natural Health Products ◽  
Paw Edema ◽  
In Vivo Evaluation ◽  
Anti Inflammatory ◽  
Fruit Oil ◽  
Inflammatory Effect

In order to find new topical anti-inflammatory agents, we had recourse to a medicinal plant. This work was designed to determine the topical anti-inflammatory effect ofPistacia lentiscusfruit oil (PLFO), using carrageenan-induced paw edema rat model, and to evaluate its effects on oxidative stress. The topical anti-inflammatory activity of PLFO was compared to Inflocine® and estimated by measuring the diameter of paw edema, for 5 hours at a 1-hour interval. After that the rats were scarified and the inflamed paw tissue was removed for the exploration of some parameters of oxidative stress and histopathology. PLFO showed a significant anti-inflammatory activity in comparison with the Inflocine. The percentages of edema inhibition were 70% and % 51.5% (p<0.01), respectively, after five hours. The treatment with PLFO and Inflocine led to significant increases (p≤0.05) in the activities of CAT, SOD, and GPX and significant decreases in the MDA level and AOPP activity in the paw tissue after Carr injection, in comparison with the Carr group. Therefore, our findings demonstrate that PLFO might accelerate the development of new drugs which could be used scientifically as a source for natural health products in the treatment of topical inflammation.

scholarly journals A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1658
Author(s):  
Dalia H. Abdelkader ◽  
Ahmed Kh. Abosalha ◽  
Mohamed A. Khattab ◽  
Basmah N. Aldosari ◽  
Alanood S. Almurshedi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
In Vitro Release ◽  
In Vivo Evaluation ◽  
Water Emulsion ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

scholarly journals Nanoemulgel, an Innovative Carrier for Diflunisal Topical Delivery with Profound Anti-Inflammatory Effect: in vitro and in vivo Evaluation

2021 ◽  
Vol Volume 16 ◽  
pp. 1457-1472
Author(s):  
Mehreen Bashir ◽  
Junaid Ahmad ◽  
Muhammad Asif ◽  
Salah-Ud-Din Khan ◽  
Muhammad Irfan ◽  
...  
Keyword(s):  
Topical Delivery ◽  
In Vivo Evaluation ◽  
Anti Inflammatory ◽  
Inflammatory Effect

scholarly journals In Vivo Evaluation of the Anti-Inflammatory Activity of Electrospun Micro/Nanofibrous Patches Loaded with Pinus halepensis Bark Extract on Hairless Mice Skin

Materials ◽  
2019 ◽  
Vol 12 (16) ◽  
pp. 2596 ◽  
Author(s):  
Eleftheria Kotroni ◽  
Eleftheria Simirioti ◽  
Stefanos Kikionis ◽  
Ioannis Sfiniadakis ◽  
Aggeliki Siamidi ◽  
...  
Keyword(s):  
Pinus Halepensis ◽  
Skin Inflammation ◽  
Inflammatory Activity ◽  
Bark Extract ◽  
Common Symptom ◽  
Hairless Mice ◽  
In Vivo Evaluation ◽  
Promising Alternative ◽  
Anti Inflammatory

Skin inflammation is the most common symptom in dermatological diseases. It is usually treated by topically applied products, such as creams, gels and lotions. Skin dressings offer a promising alternative as they are endowed with more controlled administration conditions. In this study, the anti-inflammatory activity of electrospun alginate micro/nanofibrous dressings loaded with the aqueous extract of Pinus halepensis bark (PHBE) was evaluated in vivo in mice. The upper back skin of SKH-1 female hairless mice was exposed to a single dose of ultraviolet radiation (3 MEDs) and the inflamed area was treated daily by the direct application of a nanofibrous patch. The condition of the skin was evaluated primarily on the basis of clinical observation, photo-documentation and histopathological assessment, while measurements of the erythema, hydration, transepidermal water loss (TEWL) and sebum production were also taken into account. The results showed that the topical application of alginate micro/nanofibrous dressings loaded with PHBE on UV-inflamed skin significantly attenuated inflammation damage, reducing the healing period. Increase of the loading dose of PHBE resulted in a proportional reduction of the extent, the density and the depth of skin inflammation. With the steadily increasing interest of the skin dressing industry towards nanofibrous matrices, electrospun nonwovens could serve as ideal candidates for the development of multifunctional anti-inflammatory care systems.

scholarly journals The Anti-Inflammatory Activity of HMGB1 A Box Is Enhanced When Fused with C-Terminal Acidic Tail

2010 ◽  
Vol 2010 ◽  
pp. 1-6 ◽  
Author(s):  
Wei Gong ◽  
Yingru Zheng ◽  
Fan Chao ◽  
Yuan Li ◽  
Zhizhen Xu ◽  
...  
Keyword(s):  
Fusion Proteins ◽  
Inflammatory Diseases ◽  
Inflammatory Activity ◽  
In Vivo Experiments ◽  
Specific Antagonist ◽  
Proinflammatory Activity ◽  
Anti Inflammatory ◽  
Inflammatory Effect

HMGB1, composed of the A box, B box, and C tail domains, is a critical proinflammatory cytokine involved in diverse inflammatory diseases. The B box mediates proinflammatory activity, while the A box alone acts as a specific antagonist of HMGB1. The C tail contributes to the spatial structure of A box and regulates HMGB1 DNA binding specificity. It is unknown whether the C tail can enhance the anti-inflammatory effect of A box. In this study, we generated fusion proteins consisting of the A box and C tail, in which the B box was deleted and the A box and C tail were linked either directly or by the flexible linker sequence(Gly4Ser)3. In vitro and in vivo experiments showed that the two fusion proteins had a higher anti-inflammatory activity compared to the A box alone. This suggests that the fused C tail enhances the anti-inflammatory effect of the A box.

scholarly journals The Anti-Inflammatory Effect of Aptamin C on House Dust Mite Extract-Induced Inflammation in Keratinocytes via Regulation of IL-22 and GDNF Production

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 945
Author(s):  
Dahae Lee ◽  
Yejin Kim ◽  
Hyejung Jo ◽  
Cheolhyeon Go ◽  
Yoojin Jeong ◽  
...  
Keyword(s):  
Vitamin C ◽  
Cell Line ◽  
House Dust ◽  
Inflammatory Responses ◽  
Inflammatory Diseases ◽  
Skin Inflammation ◽  
Skin Lesions ◽  
House Dust Mites ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atopic dermatitis (AD), a chronic inflammatory skin disease, is characterized by eczemous lesions on the skin that manifest as severe itching and last a long time. AD is thought to be a response to local allergens, including house dust mites (HDMs). Aptamin C is a modified form of vitamin C comprised of aptamers (DNA fragments) that bind specifically to vitamin C and inhibit its oxidation, thereby increasing its stability and antioxidant effects. It is already known that vitamin C shows an anti-inflammatory effect on skin inflammation. Oxidative stress is one of the major causes of inflammatory diseases, including HDM-induced skin inflammation, suggesting that the antioxidant activity of Aptamin C could regulate inflammatory responses to HDMs in the skin keratinocyte cell line HaCaT and primary skin keratinocytes. Aptamin C not only inhibited HDM-induced proliferation of both type of cells, but suppressed HDM-induced increases in interleukin (IL)-1α and IL-6 production by these cells. In addition, Aptamin C suppressed the production of IL-17 and IL-22 by T cells, which are closely associated with AD pathogenesis, as well as HDM-induced IL-22Rα expression. Aptamin C also reduced the production of thymus and activation-regulated chemokine (TARC) by suppressing the interaction between IL-22 and IL-22Rα, as well as reducing T cell migration. Although HDM treatment markedly increased the expression of glial cell line-derived neurotrophic factor (GDNF), which is associated with itching in AD skin lesions, this increase was reduced by Aptamin C treatment. Taken together, these results suggest that Aptamin C can effectively regulate inflammatory lesions, such as AD, by regulating the production of inflammatory cytokines and GDNF induced by HDM.

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