scholarly journals The In Vitro–In Vivo Safety Confirmation of PEG-40 Hydrogenated Castor Oil as a Surfactant for Oral Nanoemulsion Formulation

2017 ◽  
Vol 85 (2) ◽  
pp. 18 ◽  
Author(s):  
Heni Rachmawati ◽  
Miranti Novel ◽  
Sri Ayu ◽  
Guntur Berlian ◽  
Olivia Tandrasasmita ◽  
...  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Lena Dalal ◽  
Abdul Wahab Allaf ◽  
Hind El-Zein

AbstractSelf-nanoemulsifying drug delivery systems (SNEDDS) were used to enhance the dissolution rate of furosemide as a model for class IV drugs and the system was solidified into liquisolid tablets. SNEDDS of furosemide contained 10% Castor oil, 60% Cremophor EL, and 30% PEG 400. The mean droplets size was 17.9 ± 4.5 nm. The theoretical model was used to calculate the amounts of the carrier (Avicel PH101) and coating materials (Aerosil 200) to prepare liquisolid powder. Carrier/coating materials ratio of 5/1 was used and Ludipress was added to the solid system, thus tablets with hardness of 45 ± 2 N were obtained. Liquisolid tablets showed 2-folds increase in drug release as compared to the generic tablets after 60 min in HCl 0.1 N using USP apparatus-II. Furosemide loaded SNEDDS tablets have great prospects for further in vivo studies, and the theoretical model is useful for calculating the adequate amounts of adsorbents required to solidify these systems.


2020 ◽  
Author(s):  
Safaet Alam ◽  
Nazim Uddin Emon ◽  
Mohammad A. Rashid ◽  
Mohammad Arman ◽  
Mohammad Rashedul Haque

AbstractBackgroundColocasia gigantea is locally named as kochu and also better known due to its various healing power. This research is to investigate the antidiarrheal, antimicrobial, and antioxidant possibilities of the methanol soluble extract of Colocasia gigantea.MethodsAntidiarrheal investigation was performed by using in vivo castor oil induced diarrheal method where as in vitro antimicrobial and antioxidant investigation have been implemented by disc diffusion and DPPH scavenging method respectively. Moreover, in silico studies were followed by molecular docking analysis of several secondary metabolites were appraised with Schrödinger-Maestro v 11.1.ResultsThe induction of plant extract (200 and 400 mg/kg, b.w, p.o), the castor oil mediated diarrhea has been minimized 19.05 % (p < 0.05) and 42.86 % (p < 0.001) respectively. The methanolic extract of C. gigantea showed mild sensitivity against almost all the tested strains but it shows high consistency of phenolic content and furthermore yielded 67.68 μg/mL of IC50 value in the DPPH test. The higher and lower binding affinity was shown in beta-amyrin and monoglyceryl stearic acid against the kappa-opioid receptor (PDB ID: 4DJH) with a docking score of -3.28 kcal/mol and -6.64 kcal/mol respectively. In the antimicrobial investigation, Penduletin and Beta-Amyrin showed the highest and lowest binding affinity against the selected receptors with the docking score of -8.27 kcal/mol and -1.66 kcal/mol respectively.ConclusionThe results of our scientific research reflect that the methanol soluble extract of C. gigantea is safe which may provide possibilities of alleviation of diarrhea and as a potential wellspring of antioxidants which can be considered as an alternate source for exploration of new medicinal products.


2019 ◽  
Vol 5 (1) ◽  
Author(s):  
Mirazul Islam ◽  
Tabassum Jannat ◽  
Md. Ruhul Kuddus ◽  
Mohammad Abdur Rashid ◽  
Mohammad Rashedul Haque

Abstract Background Campsis radicans L. is a flowering plant in Bangladesh, traditionally used for the treatment of several human diseases. In this study, in vitro antioxidant, thrombolytic, membrane stabilizing and in vivo analgesic, hypoglycemic, anti-diarrheal and CNS antidepressant activities of organic soluble fractions of crude methanol extract of C. radicans leaf were investigated using appropriate experimental models. Methods The leaves of C. radicans were collected, authenticated, dried and extracted with methanol at room temperature for 30 days. The concentrated methanol extract was partitioned to petroleum-ether (PESF), dichloromethane (DMSF) and ethyl acetate (EASF) soluble fractions. The antioxidant activity of these fractions was determined by DPPH free radical scavenging method. Total phenolic content was determined by the Folin-Ciocalteau’s spectrophotometric method. The thrombolytic activity was assessed by measuring clot lysis ability whereas the membrane stabilizing activity was evaluated by heat- and hypotonic solution-induced hemolysis assay. Tail immersion procedure and acetic acid- induced writhing model were used to measure the analgesic activity of C. radicans. The hypoglycemic, anti-diarrheal and CNS antidepressant activities were determined by oral glucose tolerance test, castor oil-induced diarrheal model and thiopental-sodium induced sleeping time test in mice, respectively. Results All the organic soluble fractions of C. radicans contained phenolic compounds varying from 6.38 to 60.13 mg of GAE/gm of extractive, while in DPPH assay, EASF showed the highest free radical scavenging activity with IC50 is 4.69 μg/ml. The PESF exhibited highest thrombolytic activity (57.14% clot lysis) and the DMSF showed maximum 53.95% inhibition of heat-induced hemolysis of human RBCs. In both tail immersion and acetic acid induced writhing models, the PESF, DMSF, EASF at the doses of 200 and 400 mg/kg body weight, induced a significant (P < 0.001) decrease in the painful sensation in mice. Substantial (P < 0.05) anti-hyperglycemic activity of test samples was found in mice loaded with glucose at the same doses mentioned earlier. Castor oil induced diarrheal test of the plant extractives has shown significant effect in comparison to control group. In CNS antidepressant activity assay, the test samples were able to reduce the duration of sleep in mice caused by thiopental administration. Conclusion All these findings revealed that C. radicans possess significant antioxidant, thrombolytic, membrane stabilizing, analgesic, hypoglycemic, anti-diarrheal and CNS antidepressant activities.


2021 ◽  
Vol 9 (3) ◽  
pp. 335-342
Author(s):  
Sadia Islam Nishi ◽  
◽  
Niloy Barua ◽  
Mohammed Aktar Sayeed ◽  
Abu Montakim Tareq ◽  
...  

The study reports the in vivo antidiarrheal and in vitro anthelmintic, cytotoxic, and thrombolytic activity of methanol extract of Hedychium coccineum rhizomes (MEHC). The antidiarrheal activity was determined using Castor oil-induced diarrhea and Gastrointestinal motility test in mice at the doses of 200 and 400 mg/kg body weight, whereas an aquarium worm, Tubifex tubifex, was used to determine the anthelmintic activity. The cytotoxic and thrombolytic activity of MEHC was performed by Brine shrimp lethality bioassay and clot lysis method respectively. In antidiarrheal, castor oil-induced diarrhea and gastrointestinal motility exhibited a significant reduction in diarrhea and defecation and an extremely significant inhibition in intestinal motility and peristalsis index by 200 and 400 mg/kg of MEHC. The MEHC (5, 10, and 20 mg/mL) showed a significant dose-dependent manner paralysis time and times to death in multiple comparisons to the different levamisole concentrations (0.5, 0.8, and 1 mg/mL) at in vitro anthelmintic activity. The brine shrimp lethality bioassay exhibited a weak LC50 (681.95 µg/mL; R² = 0.951) while in thrombolytic a significant percentage of clot lysis (32.70%, P < 0.05) demonstrated. The findings demonstrate that H. coccineum rhizomes could be potential sources for biological activity.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Dagninet Derebe ◽  
Mohammedbrhan Abdulwuhab ◽  
Muluken Wubetu ◽  
Faiz Mohammed

Diarrhea is a major health problem throughout the world and it has become more problematic in developing countries like Ethiopia. People, in several parts of the world, use different traditional medicines for treating diarrhea and it has been reported that the roots, leaves, and flowers of various species are used for the same purpose. In Ethiopia, for instance, Discopodium Penninervum is used for the treatment of diarrhea and also to control infection. The aim of the present study was, therefore, to evaluate the in vivo antidiarrheal and in vitro antimicrobial effect of Discopodium Penninervum in mice. For the antimicrobial activity test, four standard bacteria and disc diffusion method were used, while for antidiarrheal experiment, animals had been used, which were divided into 5 groups. The first group served as negative control and was administered with vehicle (0.2-0.3ml of distilled water). Groups two (D100), three (D200), and four (D400) were administered 100, 200, and 400 mg/kg of the extract, respectively. Group five served as positive control group and was administered with either loperamide (3mg/kg) for castor oil induced diarrhea and castor oil induced enteropooling diarrhea models or atropine (1mg/kg) for charcoal meal test. Safety study was performed using a standard acute toxicity study procedure. The effect of the extract on castor oil induced diarrheal drops, onset of diarrhea, weight of faeces, small intestinal fluid accumulation, and intestinal motility was measured and analyzed using one-way ANOVA. Preliminary phytochemical screening of the leaves powder of the plant indicated the presence of various components. Inhibition of castor oil induced diarrhea was observed at all tested doses. It can be concluded that crude extracts of Discopodium Penninervum showed strong activities against diarrhea indicating that it contains some chemical constituents that possibly lead to antidiarrheal drug development.


2018 ◽  
Vol 17 (2) ◽  
pp. 205-211 ◽  
Author(s):  
Syed Intasar Husain Taqvi ◽  
Atiqur Rahman ◽  
Mohammad Ali Versiani ◽  
Hina Imran ◽  
Amna Khatoon ◽  
...  

Objective: To investigate and determine the antidiarrhoeal and spasmolytic potential of fruit of Aegle marmelos is due to CCBs compounds and not tannic acid.Materials and methods: The extract of ripe and dry fruit of A. marmelos (Am.Cr) was prepared in methanol: water (70:30). The antidiarrhoeal activities of the extract, loperamide and tannic acid were studied in vivo; in castor oil induced diarrhoeal model in mice whereas spasmolytic effect was studied in vitro; in isolated mice ileum. Calcium channel blocking (CCB) activity was investigated after preincubation of mice ileum by Am. Cr or loperamide and subsequent adding of K+80 mM.Results: Am. Cr inhibited castor oil-induced diarrhoea: onset of diarrhoea, total no. of faeces, and total no. of wet faeces dose-dependently, the dose of 800 mg/mL was found statistically significant, total weight of feces and total weight of wet faeces were also inhibited. Concentration-dependent inhibition of spontaneous contraction and contractile effect of K+80 mM after pre-incubation by Am. Cr were confirmed in isolated mice ileum. The results of Am. Cr are comparable with Loperamide. Tannic acid produced neither antidiarrhoeal effect nor exhibited CCB activity, however relaxant effect was observed in isolated mice ileum.Conclusion: The antidiarrhoeal and spasmolytic effects of Am.Cr may be mediated through compounds which posses CCB effect. Tannic acid exhibited relaxant effect only which is not sufficient evidence scientifically to classify as antidiarrhoeal.Bangladesh Journal of Medical Science Vol.17(2) 2018 p.205-211


2016 ◽  
Vol 11 (1) ◽  
pp. 175 ◽  
Author(s):  
Imran Ahmad Khan ◽  
Khalid Hussain Janbaz ◽  
Fatima Saqib

<p>This study evaluates the antidiarrheal activity of <em>Rumex vesicarius</em> (leaf) by using in vitro and in vivo assays. Antidiarrheal effect of <em>R. vesicarius</em> was  evaluated using castor oil-induced diarrhea model in rat. Weight and  volume of the intestinal content were assessed using the enteropooling method. Atropine (3 mg/kg, i.p) was used as positive control. <em>R. Vesicarius</em> at the  doses of 200 and 400 mg/kg p.o. significantly retarded castor oil-induced  enteropooling and intestinal transit. The gastrointestinal transit rate was  studied and <em>R. vesicarius</em> at the doses of 200 and 400 mg/kg significantly inhibited (p&lt;0.001) weight and volume of intestinal content. <em>R. vesicarius</em> caused concentration-dependent (0.01–1 mg/mL) relaxation of spontaneous contractions in isolated rabbit jejunum tissue preparation and inhibited K<sup>+</sup>-80 induced contractions (0.01-5 mg/mL), similar to verapamil, suggestive of calcium channel blockade. Results obtained herein indicate that <em>R. vesicarius</em> may contain effective compounds which can be used as an antidiarrheal agent.</p>


Author(s):  
Md. Azimul Islam ◽  
Mohammed Aktar Sayeed ◽  
Md. Abdul Barek ◽  
Enama Nabi Shetu ◽  
Md. Nurul Faisal

Aims: The present study aimed to investigate antidiarrheal and thrombolytic effect of ethanolic extract of leaves of A. dealbatum in mice. Study design: Antidiarrheal effect was evaluated by castor oil-induced diarrhea method at two different concentrations in mice and in vitro thrombolytic activity was analyzed with clot lysis assay of human blood. Place and duration of study: Department of Pharmacy, International Islamic University Chittagong, Kumira, Chittagong-4318, Bangladesh, between December 2018 and February 2019. Methodology: The male Swiss mice’s were divided into four groups (n = 5). First group was orally treated with 1% Tween-80 (10 ml/kg) and second group was orally treated with loperamide (5 mg/kg). Third and fourth group were orally treated with ethanolic extract of leaves of A. dealbatum at 200 and 400 mg/kg accordingly. Human RBCs were collected for conducting thrombolytic assay. During this study, 1.5 ml of venous blood was drawn from healthy volunteers (n = 10) and Streptokinase was employed as positive control and distilled water was employed as negative control. Results: In castor oil induced diarrhea model, ethanolic extract of leaves of A. dealbatum at 200, 400 mg/kg and loperamide (5 mg/kg) significantly reduced the number of feces and increase percent of inhibition of defecations compared to negative control. The extract showed percent of inhibition of defecation of 16.67 and 37.50 for 200 and 400 mg/ml respectively where the positive control loperamide showed 66.67%. Percentage of clot disruptions were 4.51 (p<.001), 75.69 (p<.001) and 26.07 (p<.001) for water, streptokinase and 10 mg/ml extract respectively. Conclusion: Based on the results from in vivo and in vitro activities, the leaves of A. dealbatum were found to be a potential source of new antidiarrheal and thrombolytic agents.


Sign in / Sign up

Export Citation Format

Share Document