scholarly journals Formulation of Topical Dosage Forms Containing Synthetic and Natural Anti-Inflammatory Agents for the Treatment of Rheumatoid Arthritis

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 24
Author(s):  
Tunde Jurca ◽  
Liza Józsa ◽  
Ramona Suciu ◽  
Annamaria Pallag ◽  
Eleonora Marian ◽  
...  

Topical anti-inflammatory and analgesic effect for the treatment of rheumatoid arthritis is of major interest because of their fewer side effects compared to oral therapy. The purpose of this study was to prepare different types of topical formulations (ointments and gels) containing synthetic and natural anti-inflammatory agents with different excipients (e.g.,: surfactants, gel-forming) for the treatment of rheumatoid arthritis. The combination of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), diclofenac sodium, a topical analgesic agent methyl salicylate, and a lyophilized extract of Calendula officinalis with antioxidant effect were used in our formulations. The aim was to select the appropriate excipients and dosage form for the formulation in order to enhance the diffusion of active substances and to certify the antioxidant, analgesic, and anti-inflammatory effects of these formulations. To characterize the physicochemical properties of the formulations, rheological studies, and texture profile analysis were carried out. Membrane diffusion and permeability studies were performed with Franz-diffusion method. The therapeutic properties of the formulations have been proven by an antioxidant assay and a randomized prospective study that was carried out on 115 patients with rheumatoid arthritis. The results showed that the treatment with the gel containing diclofenac sodium, methyl salicylate, and lyophilized Calendula officinalis as active ingredients, 2-propenoic acid homopolymer (Synthalen K) as gel-forming excipient, distilled water, triethanolamine, and glycerol had a beneficial analgesic and local anti-inflammatory effect.

Author(s):  
Chinedu E. Udekwu ◽  
Shirley Ebhohon ◽  
Raymond C. Ibeh ◽  
Henry N. Ogbonna ◽  
Ugonna D. Nwankpa

Aim: The present study was carried out to investigate the antimicrobial, cytotoxic, and anti-inflammatory activities of aqueous stem extract of Loranthus micranthus (African mistletoe) plant. Methods: The Disc agar diffusion method was used for the antimicrobial susceptibility test of test organisms to determine the minimum zone of inhibition. The brine shrimp lethality test method was used in determining cytotoxicity, and the heat-induced membrane diffusion method was used for anti-inflammatory indices. Results: In this study, the antimicrobial activity was evaluated using Escherichia Coli., Salmonella typhi, Pseudomonas aeruginosa, and Staphylococcus aureus as test organisms which showed significant zones of inhibition at increasing concentrations (25, 50 and 100 mg/ml) of the plant extract. The result of the cytotoxic investigation after the use of brine shrimps as test organisms revealed that the plant was not toxic as the LC50 did not fall within the concentrations used in this study. Also, the aqueous stem extract of L. micranthus showed significantly lower optical densities of hemoglobin compared to the corresponding standard (Aspirin) concentrations of 25, 50, 100, 200 and 300 µg/ml. This result was in agreement with the % protection of the experimental plant, which showed a significant increase with an increase in concentration, which implies that the aqueous stem extract of L.micranthus has anti-inflammatory effects. Conclusion: It can, therefore, be concluded that the usage of the aqueous stem extract of Loranthusmicranthus as a therapeutic drug would exert health benefits by virtue of its antimicrobial, anti-inflammatory and less toxicity, proved in this study.


2021 ◽  
Vol 17 (3) ◽  
pp. 15-21
Author(s):  
F. V. Hladkykh

Relevance. Cryopreserved placenta extract (CPE) increase the resistance of the mucous membrane of the gastrointestinal tract to the damaging effects of nonsteroidal anti-inflammatory drugs. Preventive administration of CPE can reduce the ulcerogenic effect of meloxicam, ibuprofen, diclofenac sodium (DS) and others. There is evidence of CPE's own anti-inflammatory activity, which can be successfully combined with the pharmacological properties of nonsteroidal anti-inflammatory drugs, while improving their safety profile. Objective: to characterize the therapeutic activity of the combined use of CPE and DS according to hematological parameters in the model of experimental rheumatoid arthritis (RA). Materials and methods. Studies were performed on 28 nonlinear laboratory rats. The rats were divided into 4 groups: I (n = 7) – intact rats; II (n = 7) – rats with experimental RA; ІІІ (n = 7) – rats with experimental RA, treated with DN; IV (n = 7) – rats with experimental RA, treated with DN and CPE. Adjuvant arthritis was modeled by subplantar administration of complete Freund's adjuvant. Treatment was performed from 14 to 28 days. CPE was administered on days 14, 17, 20, 23 and 26, and DS – daily. Blood tests were performed on day 28 of the experiment. Results. The combined use of CPE and DS is accompanied by a more pronounced leveling of inflammatory signs by hematological parameters – erythrocyte clotting rate decreased by 72.2% (p<0.001), and the number of leukocytes decreased by 54.81% (p<0.001) relative to rats with adjuvant arthritis without treatment. There was a leveling of signs of anemia of chronic inflammation – the level of hemoglobin and erythrocytes increased (p<0,001) by 17.6% and 36.8%, respectively, relative to rats with adjuvant arthritis without treatment. Conclusions. The combined use of CPE and DS is superior in therapeutic activity to monotherapy with this nonsteroidal anti-inflammatory drug of experimental rheumatoid arthritis.


Author(s):  
Roland Klingenberg ◽  
Ulf Müller-Ladner

This chapter provides a brief summary of the immune pathogenesis of atherosclerosis, highlighting shared features with inflammatory pathways in rheumatoid arthritis (RA) described in detail in Chapter 25.4. RA constitutes a prototype autoimmune disease primarily affecting the joints but also the heart and vessels associated with increased cardiovascular mortality. Recent years have produced a wealth of novel insights into the diversity of immune cell types which either propagate or dampen inflammation in atherogenesis. Expansion of this inherent anti-inflammatory component carried by regulatory T cells may constitute a new therapeutic target to harness the progression of atherosclerotic cardiovascular disease. Among the various inflammatory mediators involved in RA pathology, cytokines (tumour necrosis factor-α‎ and interleukin-6) have gained major interest as therapeutic targets with approved therapies available. In light of the many common features in the pathogenesis of RA and atherosclerosis, these biologics are currently being evaluated in cardiovascular patients. The recently published CANTOS trial showed that IL-1 inhibition reduced adverse cardiovascular events in patients with coronary artery disease demonstrating that inflammation is a genuine therapeutic target. The near future will provide more information whether inflammation is a bona fide cardiovascular risk factor based on completion of several clinical trials using anti-inflammatory approaches in patients with both cardiovascular disease and rheumatoid arthritis.


2021 ◽  
Vol 11 (5-S) ◽  
pp. 63-70
Author(s):  
G'massampou Datagni ◽  
Aklesso Pouwelong Mouzou ◽  
Kossi Metowogo ◽  
Yaovi-Gameli Afanyibo ◽  
Adodo Sadji ◽  
...  

Annona senegalensis and Securidaca longepedunculata are two plants traditionnaly used in inflammation and wounds infection treatment after snakebites. This study aims to investigate the in vitro anti-inflammatory and antimicrobial activities of the hydroalcoholic extracts of Annona senegalensis and Securidaca longepedunculata. Antimicrobial activity of the two plant extracts was examined against five bacterial strains with the well diffusion method and the inhibition zones diameters (IZD), minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined using the 96-well microplate dilution method. While antiinflammatory activity was assessed by the albumin denaturation method. The results obtained showed that the hydroalcoholic extract of Annona senegalensis has antimicrobial property against Staphylococcus aureus (IZD=12.22 ± 0.24 mm, MIC=62.5 mg/mL, MBC=125 mg/mL) and against Pseudomonas aeruginosa (IZD=12.06 ± 0.06 mm, MIC=125 mg/mL, MBC=250 mg/mL). Securidaca longepedunculata also showed its antimicrobial activity against Staphylococcus aureus (IZD=12.03 ± 0.03 mm, MIC=125 mg/mL, MBC=250 mg/mL) and Candida albicans (IZD=12.12 ± 0.07 mm, MIC=62.5 mg/mL, MFC=125 mg/mL). In the order hand,  Annona senegalensis and Securidaca longepedunculata exhibited concentration-dependent anti-inflammatory activity by reducing significantly (p<0.001)  the denaturation of BSA. In addition  S. longepedunculata inhibited haemolysis significantly (p<0.001) more than Diclofenac sodium at 200 and 400 µg/mL. Hence, it was concluded that Annona senegalensis and Securidaca longepedunculata possessed anti-inflammatory and antimicrobial properties and can be used in the treatment of inflammation and wounds infection after snakebites. Keywords: Annona senegalensis, Securidaca longepedunculata, anti-inflammatory, antimicrobial, BSA.


2012 ◽  
Vol 10 (5) ◽  
pp. 639-646 ◽  
Author(s):  
Cecilia Chighizola ◽  
Tommaso Schioppo ◽  
Francesca Ingegnoli ◽  
Pier Luigi Meroni

2020 ◽  
Vol 16 (8) ◽  
pp. 1134-1146
Author(s):  
Priyanka Kriplani ◽  
Kumar Guarve ◽  
Uttam S. Baghel

Objective: Helenalin is a natural anti-inflammatory agent that is proving its efficacy to treat various medical conditions. Though many plants are proving their effectiveness but their mechanisms are still not well understood. The objective of the review is to summarize various mechanisms of helenalin to treat inflammatory disorders and cancers, adverse effects, and avenues of further research. Methods: Structured research was carried out including Pub med, Science direct Medline, Research Gate and Google Scholar to find all articles published on helenalin. Various keywords used were “helenalin”, “Arnica”, “cancer”, “anti-inflammatory”, “cardiovascular”, “IBD”, “pharmacokinetics” etc. The aim of the review was to find out the problem prevailing in the data published to date which will help the researchers to investigate the molecule clinically. Results: Seventy articles are included in the review. Helenalin is found to cure chronic conditions like rheumatoid arthritis, ulcers and malignancies like stomach, colon, breast, larynx, lung and skin cancers via multiple mechanisms. These diseases do not proceed via a unilateral pathway. So, it can be a useful molecule to treat numerous diseases. Conclusion: This review article will help us to systemically analyze the wealth of information concerning the medicinal properties of helenalin and to recognize the gaps which have vetoed its pervasive application in the medical community.


2021 ◽  
Vol 22 (15) ◽  
pp. 7828
Author(s):  
Justine M. Webster ◽  
Michael S. Sagmeister ◽  
Chloe G. Fenton ◽  
Alex P. Seabright ◽  
Yu-Chiang Lai ◽  
...  

Glucocorticoids provide indispensable anti-inflammatory therapies. However, metabolic adverse effects including muscle wasting restrict their use. The enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) modulates peripheral glucocorticoid responses through pre-receptor metabolism. This study investigates how 11β-HSD1 influences skeletal muscle responses to glucocorticoid therapy for chronic inflammation. We assessed human skeletal muscle biopsies from patients with rheumatoid arthritis and osteoarthritis for 11β-HSD1 activity ex vivo. Using the TNF-α-transgenic mouse model (TNF-tg) of chronic inflammation, we examined the effects of corticosterone treatment and 11β-HSD1 global knock-out (11βKO) on skeletal muscle, measuring anti-inflammatory gene expression, muscle weights, fiber size distribution, and catabolic pathways. Muscle 11β-HSD1 activity was elevated in patients with rheumatoid arthritis and correlated with inflammation markers. In murine skeletal muscle, glucocorticoid administration suppressed IL6 expression in TNF-tg mice but not in TNF-tg11βKO mice. TNF-tg mice exhibited reductions in muscle weight and fiber size with glucocorticoid therapy. In contrast, TNF-tg11βKO mice were protected against glucocorticoid-induced muscle atrophy. Glucocorticoid-mediated activation of catabolic mediators (FoxO1, Trim63) was also diminished in TNF-tg11βKO compared to TNF-tg mice. In summary, 11β-HSD1 knock-out prevents muscle atrophy associated with glucocorticoid therapy in a model of chronic inflammation. Targeting 11β-HSD1 may offer a strategy to refine the safety of glucocorticoids.


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