scholarly journals Improved Analgesic and Anti-Inflammatory Effect of Diclofenac Sodium by Topical Nanoemulgel: Formulation Development—In Vitro and In Vivo Studies

2020 ◽  
Vol 2020 ◽  
pp. 1-10 ◽  
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Sabna Kotta ◽  
Javed Ahmad ◽  
...  

The present study aimed to develop diclofenac sodium nanoemulgel for managing pain and inflammation using the low-energy emulsification technique. Nanoemulsion of diclofenac was formulated using clove oil with adequate amount of surfactants and cosurfactants, and it was converted to hydrogel form using Carbopol 980 as the gelling agent. The droplet size of the oil globules in the nanoemulsion was found to be 64.07 ± 2.65 nm with a low polydispersity index (0.238 ± 0.02) along with high negative zeta potential (−39.06 mV). The developed nanoemulgel exhibited non-Newtonian and pseudoplastic behavior. The in vitro release profile of the developed nanoemulgel was higher as compared to marketed and conventional gel. The carrageenan-induced paw edema test was performed in rats to evaluate the anti-inflammatory activity of developed nanoemulgel. The developed nanoemulgel showed significantly higher (p<0.01) effect in reducing pain and inflammation symptoms as compared to marketed as well as conventional gel of diclofenac. The overall findings of the study suggest that the developed nanoemulgel formulation of diclofenac can be used as a potential approach for the management of pain and inflammation.

2011 ◽  
Vol 63 (5) ◽  
pp. 679-687 ◽  
Author(s):  
Chang Hwa Jung ◽  
Jeong-Hyun Kim ◽  
Ji Hye Kim ◽  
Joo Hee Chung ◽  
Han-Seok Choi ◽  
...  

2021 ◽  
Vol 12 (3) ◽  
pp. 1699-1708
Author(s):  
Ashish ◽  
Anjali ◽  
Praveen K Dixit ◽  
Nagarajan K

The present study is carried out to evaluate anti-inflammatory and anti-arthritic potential of Justicia gendarussa. Leaves and stem extracted with ethanol and chloroform. These extract is tested against in-vitro (HRBC membrane stabilization method and Inhibition of protein denaturation method) and in-vivo (Carrageenan induced paw edema model) anti-inflammatory models. To assess the anti-arthritic activity, FCA induced arthritis model is used. Assessment of arthritis is done by paw volume, joint diameter, body weight, biochemical parameters, hematological parameters (Hb, RBC, WBC, ESR). The effect of in-vitro anti-inflammatory model depends on concentration. Both test extract and standard Diclofenac sodium has been shown concentration dependent effect. The maximum anti-inflammatory effect of the test extract achieved at 2000μg/ml. The test (JGLE, JGLC, JGSE) has been shown inhibition of paw edema induced by carrageenan at 50mg/kg body weight. The extract JGLE, JGLC, JGSE at 50mg/kg body weight and 100mg/kg body weight orally showed the significant (P< 0.05) and dose dependent inhibitory effect against FCA induced arthritis model. Diclofenac sodium 20mg/kg body weight orally is used as a standard. JGLE exhibit more significant and most promising anti-arthritic and anti-inflammatory effect than other extracts these effects support the traditional role of J. gendarussa in arthritis and other inflammatory condition.


2019 ◽  
Vol 41 (6) ◽  
pp. 568-576 ◽  
Author(s):  
Rani Sasidharan ◽  
Manju Sreedharannair Leelabaiamma ◽  
Ratheesh Mohanan ◽  
Svenia P. Jose ◽  
Bijo Mathew ◽  
...  

2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Godswill Nduka Anyasor ◽  
Azeezat Adenike Okanlawon ◽  
Babafemi Ogunbiyi

Abstract Background Justicia secunda Vahl. is a medicinal plant used in ethnomedical practice as therapy to manage inflammation. Therefore, this study was designed to evaluate the anti-inflammatory activity of methanol extract of J. secunda leaves (MEJSL) using in vitro and in vivo inflammation models. Methods Seventy-percent MEJSL was prepared following standard procedure. In vitro anti-inflammatory assays were performed using heat-induced bovine serum albumin (BSA) denaturation and erythrocyte membrane stabilization assays. Carrageenan and formaldehyde induced inflammation in rat models were used to evaluate the anti-inflammatory activity of MEJSL in vivo. Diclofenac sodium was used as a reference drug. In addition, liver and kidney function assays and hematological analysis were carried out. Results Data revealed that varying concentrations of MEJSL significantly (P < 0.05) inhibited heat-induced BSA denaturation and stabilized erythrocyte membrane against hypotonicity-induced hemolysis when compared with diclofenac sodium in a concentration-dependent manner. In vivo study showed that 10 mg/kg body weight (b.w.) diclofenac sodium, 100 and 300 mg/kg b.w. MEJSL suppressed carrageenan-induced paw edema at the sixth hour by 71.14%, 83.08%, and 89.05%, respectively. Furthermore, 10 mg/kg b.w. diclofenac sodium, 100 and 300 mg/kg b.w. MEJSL inhibited formaldehyde-induced paw edema by 72.53%, 74.73%, and 76.48%, respectively. Animals treated with varying doses of MEJSL had reduced plasma aspartate aminotransferase and alanine aminotransferase activities; urea and creatinine concentrations; and modulated hematological parameters when compared with the untreated control group. Conclusions Findings from this study showed that MEJSL exhibited substantial anti-inflammatory actions in the in vitro and in vivo models. It also indicated that MEJSL anti-inflammatory mechanisms of action could be through interference with phase 2 inflammatory stressors, upregulation of cytoprotective genes, stabilization of inflammatory cell membranes and immunomodulatory activity.


2021 ◽  
Author(s):  
Xuancheng Zhang ◽  
Ang Li ◽  
Kang Han ◽  
He Zhang ◽  
Xiaoqiao Huangfu ◽  
...  

Abstract Background: Glucocorticoids (GCs) injections are commonly used to relieve pain and improve function in patients with multiple shoulder disability, they cause detrimental effects on the rotator cuff tendons. Adipose stem cell-derived exosomes (ASC-Exos) reportedly recover impaired tendon matrix metabolism by maintaining tissue homeostasis. It is unclear whether additional ASC-Exos treatment overrides the detrimental effects of GCs without interfering with their anti-inflammatory effects.Methods: The in vitro studies included inflammatory analysis and cytoprotective analysis. In the inflammatory analysis, rat raw cells were treated with saline, GCs, or GCs + ASC-Exos and evaluated regarding cellular proliferation, migration, and secretion of inflammatory-related cytokines. In the cytoprotective analysis, rat tenocytes were treated with saline, GCs, or GCs + ASC-Exos and evaluated regarding cellular proliferation, migration, senescence, apoptosis, and transcription of tenocytic genes. In the in vivo studies, a subacromial injection of saline, GCs, or GCs + ASC-Exos was performed in a chronic injured-intact rotator cuff rat model. Histological and biomechanical analysis were performed 1 week to evaluate the protective effect of ASC-Exos against GCs-induced detriments on injured-intact in rotator cuffs.Results: In the in vitro inflammatory analysis, GCs treatment significantly decreased the proliferation, migration, and secretion of pro-inflammatory cytokines in raw cells, and increased the secretion of anti-inflammatory cytokines; additional ASC-Exos treatment further significantly decreased the secretion of pro-inflammatory cytokines and increased the secretion of anti-inflammatory cytokines, while restoring GCs-suppressed cellular proliferation and migration. In the in vitro cytoprotective analysis, GCs treatment significantly decreased the proliferation, migration, and transcription of tenocytic matrix molecules of tenocytes, and significantly increased their senescence, apoptosis, and transcription of ROS and tenocytic degradative enzymes; additional ASC-Exos treatment significantly improved the GCs-suppressed cellular proliferation, migration, and transcription of tenocytic matrix molecules, transcription of tenocytic degradative enzyme inhibitors, and significantly decreased the GCs-induced cell senescence, apoptosis, and transcription of ROS and tenocytic degradative enzymes. In the in vivo studies, an additional ASC-Exos injection restored the impaired histological and biomechanical properties owing to GCs administration.Conclusion: ASC-Exos may exert a stronger anti-inflammatory effect in combination with GCs, and override their detrimental effects on the rotator cuff.


Author(s):  
Kamalakararao Konuku ◽  
Krishna Chaithanya Karri ◽  
Velliyur Kanniappan Gopalakrishnan ◽  
Zenebe Hagos ◽  
Haftom Kebede ◽  
...  

Objective: Manilkara zapota is a medicinal plant which is native to Mexico and Central America, and widely distributed in India. Various parts of this plant are traditionally used for treatment of several diseases, including inflammation-associated ailments. The main aim of the present study is to evaluate the anti-inflammatory potential of ethyl acetate and methanolic extracts of M. zapota leaf.Methods: In vitro secretary phospholipase A2 (PLA2) and 5-Lipoxygenase (5-LOX) assays and In vivo studies using carrageenan induced rat paw edema model were performed to assess the anti-inflammatory activity of M. zapota leaf extracts.Results: In vitro studies suggest that M. zapota leaf extracts exhibited significant SPLA2 and 5-LOX inhibitory activities. In in vivo studies M. zapota leaf extracts showed dose dependent inhibition of carrageenan induced paw edema in rats. The anti-inflammatory activity of ethyl acetate leaf extract was superior to methanolic extract.Conclusion: This study concluded that ethyl acetate leaf extract of M. zapotaexhibited significant anti-inflammatory activity and warranted further investigation to isolate and identify the components. 


Author(s):  
Shiva Murthy N. ◽  
Srinivas V. ◽  
Shanthi M.

Background: NSAIDS are associated with side effects and research should continue for developing safer drugs. This study aims to evaluate newer thiazolidine-4-ones for their anti-inflammatory and ulcerogenic activities in wister rats.Methods: Five groups of wister rats, 6 in each were used.  Anti-inflammatory and ulcerogenic activities of diclofenac (30mg/kg), nimesulide (50mg/kg), thia-1 (50mg/kg) and thia-2 (50mg/kg) are compared with control group (4% Gum Acacia). Carrageenin-induced paw edema, formaline induced acute peritonitis and cotton pellet-induced granulomatous tissue formation models were used for evaluating anti-inflammatory activity. After removing cotton pellets with granuloma on 8th day gastric ulcerogenicity was assessed by using macroscopic and microscopic scoring of ulcers.Results: Diclofenac, nimesulide and thia 2 reduced both paw edema and peritoneal exudate volume significantly (p <0.01). Wet weight of cotton pellets reduced significantly (p <0.01) by diclofenac, nimesulide and thia 2. Diclofenac (p <0.01) and thia 2 (p <0.05) reduced dry weight of cotton pellets significantly. nimesulide and thia-1 reduced it by 19.14% and 2.68% respectively and was considered statistically not significant (p>0.05). Nimesulide, thia-1 and thia-2 did not increase gastric ulcer score significantly (p >0.05). Diclofenac increased ulcer score significantly (p <0.01).Conclusions: Thia-2 demonstrated significant anti-inflammatory activity in acute and chronic models. In addition to inhibition of cyclooxygenase pathway, PPAR agonistic activity may be involved in its anti-inflammatory activity.  No significant ulcerogenicity was observed on comparing with nimesulide and control. Further in-vitro and in-vivo studies are recommended to confirm the results of this study.


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