scholarly journals Optimized Ellagic Acid–Ca Pectinate Floating Beads for Gastroprotection against Indomethacin-Induced Gastric Injury in Rats

Biomolecules ◽  
2020 ◽  
Vol 10 (7) ◽  
pp. 1006 ◽  
Author(s):  
Nabil A. Alhakamy ◽  
Shaimaa M. Badr-Eldin ◽  
Osama A. A. Ahmed ◽  
Abdulrahman A. Halwani ◽  
Hibah M. Aldawsari ◽  
...  

A peptic ulcer is an alimentary tract injury that leads to a mucosal defect reaching the submucosa. This work aimed to optimize and maximize ellagic acid (EA) loading in Ca pectinate floating beads to maximize the release for 24 h. Three factors were selected: Ca pectinate concentration (X1, 1–3 w/v %), EA concentration (X2, 1–3 w/v %) and the dropping time (X3, 10–30 min). The factorial design proposed eight formulations. The optimized EA–Ca pectinate formulation was evaluated for the gastric ulcer index and the oxidative stress parameter determination of gastric mucosa. The results indicated that the optimum EA–Ca pectinate formula significantly improved the gastric ulcer index in comparison with raw EA. The protective effect of the optimized EA–Ca pectinate formula was further indicated by the histopathological features of the stomach. The results of the study indicate that an EA formulation in the form of Ca pectinate beads would be effective for protection against gastric ulcers because of Nonsteroidal anti-inflammatory drugs (NSAID) administration.

2014 ◽  
Vol 9 ◽  
pp. BMI.S15918 ◽  
Author(s):  
Kenichiro Takeuchi ◽  
Maki Ohishi ◽  
Keiko Endo ◽  
Kenichi Suzumura ◽  
Hitoshi Naraoka ◽  
...  

Gastrointestinal symptoms are a common manifestation of adverse drug effects. Non-steroid anti-inflammatory drugs (NSAIDs) are widely prescribed drugs that induce the serious side effect of gastric mucosal ulceration. Biomarkers for these side effects have not been identified and ulcers are now only detectable by endoscopy. We previously identified five metabolites as biomarker candidates for NSAID-induced gastric ulcer using capillary electrophoresis–mass spectrometry (CE–MS)-based metabolomic analysis of serum and stomach from rats. Here, to clarify mechanism of changes and limitations of indications of biomarker candidates, we performed CE–MS-based metabolomic profiling in stomach and serum from rats with gastric ulcers induced by ethanol, stress, and aspirin. The results suggest that a decrease in hydroxyproline reflects the induction of gastric injury and may be useful in identifying gastric ulcer induced by multiple causes. While extrapolation to humans requires further study, hydroxyproline can be a new serum biomarker of gastric injury regardless of cause.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 140 ◽  
Author(s):  
Osama A. A. Ahmed ◽  
Usama A. Fahmy ◽  
Rana Bakhaidar ◽  
Mohamed A. El-Moselhy ◽  
Solomon Z. Okbazghi ◽  
...  

Peptic ulcer disease is an injury of the alimentary tract that leads to a mucosal defect reaching the submucosa. This study aimed to formulate and optimize omega-3 oil as a self-nanoemulsifying drug delivery system (SNEDDS) to achieve oil dispersion in the nano-range in the stomach to augment omega-3 oil gastric ulcer protection efficacy. Three SNEDDS components were selected as the design factors: the concentrations of the oil omega-3 (X1, 10–30%), the surfactant tween 20 and Kolliphor mixture (X2, 20–40%), and the cosurfactant transcutol (X3, 40–60%). The mixture experimental design proposed twenty-three formulations with varying omega-3 SNEDDS formulation component percentages. The optimized omega-3 SNEDDS formula was investigated for gastric ulcer protective effects by evaluating the ulcer index and by the determination of gastric mucosa oxidative stress parameters. Results revealed that optimized omega-3-SNEDDS achieved significant improvement in the gastric ulcer index in comparison with pure omega-3 oil. Histopathological findings confirmed the protective effect of the formulated optimized omega-3 SNEDDS in comparison with omega-3 oil. These findings suggest that formulation of omega-3 in the form of a SNEDDS would be more effective in gastric ulcer protection than the administration of omega-3 as a crude oil.


Dose-Response ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 155932582110012
Author(s):  
Shaimaa M. Badr-Eldin ◽  
Usama A. Fahmy ◽  
Hibah M. Aldawsari ◽  
Osama A. A. Ahmed ◽  
Nabil A. Alhakamy ◽  
...  

Peptic ulcer disease is an injury of the alimentary tract that leads to a mucosal defect reaching the submucosa. Alpha-lipoic acid (ALA), a natural potent antioxidant, has been known as a gastroprotective drug yet its low bioavailability may restrict its therapeutic efficacy. This study aimed to formulate and optimize ALA using a self-nanoemulsifying drug delivery system (SNEDDS) with a size of nano-range, enhancing its absorption and augmenting its gastric ulcer protection efficacy. Three SNEDDS components were selected as the design factors: the concentrations of the pumpkin oil (X1, 10–30%), the surfactant tween 80 (X2, 20–50%), and the co-surfactant polyethylene glycol 200 (X3, 30–60%). The experimental design for the proposed mixture produced 16 formulations with varying ALA-SNEDDS formulation component percentages. The optimized ALA-SNEDDS formula was investigated for gastric ulcer protective effects by evaluating the ulcer index and by the determination of gastric mucosa oxidative stress parameters. Results revealed that optimized ALA-SNEDDS achieved significant improvement in gastric ulcer index in comparison with raw ALA. Histopathological findings confirmed the protective effect of the formulated optimized ALASNEDDS in comparison with raw ALA. These findings suggest that formulation of ALA in SNEDDS form would be more effective in gastric ulcer protection compared to pure ALA.


2016 ◽  
Vol 2016 ◽  
pp. 1-5
Author(s):  
U. Akpamu ◽  
H. O. Otamere ◽  
I. O. Ernest-Nwoke ◽  
C. N. Ekhator ◽  
U. C. Osifo

Gastric ulcer has shown association with changes in sex hormones, with impact exacerbated in males. Also, males are known to be more exposed to ulcer risk factors. This study investigates the effect of testosterone on indomethacin induced gastric ulcers in adult female rats. Eighteen female rats (225 ± 25 g body weight) were randomly assigned to 3 groups under standard laboratory condition. After acclimatization, animals fasted for 40 hrs but were given water ad libitum. Group A served as control while group B served as the ulcer control, in which ulcer was induced without treatment using indomethacin (40 mg/kg single orally dose). Group C was pretreated with testosterone (1 mg/kg IM) eight hours before ulcer induction. Eight hours after ulcer induction, animals were sacrificed and the stomach was harvested for analysis. Results showed a significant reduction in mucus content in groups C (0.79±0.11 g) and B (0.87±0.02 g) compared to A (1.11±0.03 g). Gastric mucus pH was significantly acidic in group B (4.40±0.55) compared to C (5.20±0.45) and A (5.80±0.45). There was a significantly higher ulcer index in group B (4.60±0.55 mm) compared to C (3.60±0.89 mm) and testosterone pretreatment resulted in a 21.74% ulcer inhibition. Although weak, the findings suggest that testosterone might protect the gastric mucosa against NSAIDs in females.


2015 ◽  
Vol 64 (4) ◽  
pp. 403-405
Author(s):  
Ancuta Ignat ◽  
◽  
Gabriela Paduraru ◽  
Angelica Cristina Marin ◽  
Anamaria Ciubara ◽  
...  

Nonsteroidal anti-inflammatory agents (NSAIDs) produce gastric lesions through two mechanisms: local irritation and systemic action. A 2 year and 10 months old female received NSAID for acute upper respiratory infection for 2 days and she developed coffee ground vomitus one day later. Upper gastrointestinal endoscopy revealed a gastric ulcer. She was negative for H. pylori infection, and she was diagnosed with NSAID – induced acute gastric ulcer in the absence of other causes of gastric ulcer. Gastric ulcers develop very rarely after a short-term administration of NSAIDs, which prompted us to report this case. Balancing the risk and the benefit of eradication therapy, it is indicated, for every patient who must follow a chronic treatment with anti-inflammatory drugs, to look for possible associated risk factors.


2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
A. Folorunsho Ajayi ◽  
S. Babafemi Olaleye

Cell proliferation and angiogenesis are of utmost importance for healing to take place. The KI67 and EGFR proteins are markers of cell proliferation, while CD31 and factor VIII are markers of angiogenesis. To elucidate the mechanism responsible for delayed healing of the gastric injury in old age, we analyzed the expression of these markers in rats of different months during the healing of an acetic acid-induced gastric ulcer. Male Wistar rats (aged 3, 6, 12, and 18 months) divided into four groups, according to their ages, formed the experimental animals. Stomach tissue samples were collected on days 3, 7, 14, and 21 after induction for assessment of ulcer healing. The area of gastric mucosa healed was inversely proportional to age. The expression of markers of proliferation (KI67 and EGFR) and angiogenesis (factor VIII and CD31) decreased significantly (p<0.05) in older rats when compared with younger ones (3 months > six months > 12 months > 18 months) on days 7, 14, and 21 after induction of gastric ulcer. This study revealed that the slower gastric ulcer healing rate in older rats might be due to reduced epithelial cell proliferation and angiogenic activities.


2021 ◽  
Vol 23 (102) ◽  
pp. 72-77
Author(s):  
O. Stefanyk ◽  
L. Slivinska

Gastric ulcers or equine gastric ulcer syndrome (EGUS) is a common pathology in horses of different breeds. The objective of our research work was to investigate and determine the prevalence and severity of equine gastric ulcer syndrome (EGUS) in population of n = 28 riding horses with periods of physical activity and training intensity. Two breeds were presented in this study: English Thoroughbred (n = 15) and Ukrainian riding horse (n = 13). Horses were two age groups 3–7 and 8–16 years, including 17 mares and 11 geldings. Gastric endoscopy was performed as a diagnostic tool using a 3m video endoscope. Mucosal defects was evaluated using grading system proposed by (Equine Gastric Ulcer Council 0–4 grading system)  ranging from 0 (normal mucosa with no lesions) to 4 (diffuse ulceration of mucosa with deep lesions). The study was conducted in two periods. Each period is related to different workload with mixed intensity in exercise during training program. The results of gastroscopic examination of the stomach indicate the prevalence of EGUS in 35.7 % during the first stage in horses with mild training. The severity of mucosal defect during this period which were related to grade 1 was shown in 10.7 % of horses, 2 – 21.4 %, 3 – 10.7 % and 4 – 0 %. Difference in results was found in the presence and severity of gastric ulcers between two periods in this study. During period of intermediate training the prevalence of EGUS was 46.4 % with severity of mucosal defect grade 1 presented in 14.2 % of affected horses, 2 – 28.5 %, 3 – 14.2 % and 4 – 3.5 %. Ulcerations on squamous gastric mucosa was diagnosed  more often during each period (35.7 – 50 %) compare to glandular (7.1 – 10.7 %). The study confirms association between training intensity and gastric ulceration in two breed of horses. The prevalence and severity is dependent of the training intensity.


2019 ◽  
Vol 4 (5) ◽  
pp. 19-25
Author(s):  
E. V. Moroz ◽  
A. Y. Karateev ◽  
E. V. Kryukov ◽  
A. A. Sokolov ◽  
E. N. Artemkin

Intaking antithrombotic funds (ATA) and non-steroidal anti-inflammatory drugs (NSAIDs) is one of the most frequent causes of pathology in gastrointestinal (GI) tract.The purpose of the study: comparison of pathological changes of the mucous membrane in the upper GI tract, that occur against the background of ATA and NSAIDs admission.Material and methods. Endoscopic data of two groups of patients taking ATA and NSAIDS have been compared. The first group of 448 patients from the 10th Gastrointestinal Department in N.N. Burdenko Main Military Clinical Hospital was on record from 2013 to 2017. The patients had erosive ulcerous changes of gastrointestinal mucosa, occurred against the background of the ATA admission. The second group comprised 6431 patients with rheumatic diseases. They were hospitalized in the clinic of V.A. Nasonova Research Institute of Rheumatology in the period from 2007 to 2016 and took NSAIDs regularly.Results. Duodenal and gastric ulcer changes in gastric mucosa and duodenal ulcers were identified in 168 (37.5 %) patients taking ATA and in 1691 (26.3 %) patient treated with NSAIDS. Structure of pathology varied. So, against the background of ATA and NSAIDS admission, the number of acute gastric ulceration amounted to 6.5 % and 15.5 % (p < 0.001); acute ulcers duodenal was 2.9 % and 4.9 %; combined ulcerative lesions of gastric and duodenal was 2.9 % and 2.0 %; multiple erosions of gastroduodenal mucosa were 52.4 % and 15.7 % (p < 0.001); single erosion was 35. 1% and 61.6 %. The factor of ulcer history and age ≥ 65 years old increased significantly the risk of duodenal and gastric ulcer changes in patients taking ATA and NSAIDs: OR 5.182 (95% CI 2.701–9.942) and 3.24 (95% CI 2.19–5.34), 4.537 (95% CI 2.036–10.11) and 2.016 (95% CI 1.230–2.917) respectively. Intaking of proton pump inhibitor (PPI) reduced significantly the risk of complications for both ATA and NSAIDs: OR 0.329 (95% CI 0.199–0.546) and 0.317 (95% CI 0.210–0.428) respectively.Conclusion. The structure of pathology of mucous in the upper gastrointestinal tract that arose against the backdrop of ATA and NSAIDs admission is different. The first is characterized by a multiple erosion, while the second one has single acute distal gastric ulcers. The ulcerative history and advanced age of patients increase significantly the risk of complications concerning the gastroduodenal mucosa when using ATA and NSAIDs. PPI is the effective means of preventing this pathology.


1994 ◽  
Vol 266 (5) ◽  
pp. R1448-R1453
Author(s):  
K. Honda ◽  
S. Fukuda ◽  
S. E. Ishikawa ◽  
T. Kuzuya ◽  
T. Saito

To elucidate the role of arginine vasopressin (AVP) in the development of stress-induced gastric ulcer, the mucosal lesions after restraint and water immersion were examined in Brattleboro strain rats with hereditary hypothalamic diabetes insipidus (DI) and in Long-Evans rats (LE) used as controls. Restrained animals were immersed in water for 2 h, and the size of lesion was expressed as percentage of the lesion area to the total glandular mucosal area, which were defined as ulcer index (UI). In DI rats, UI was significantly higher than in control LE rats, despite the attenuated responses of plasma adrenocorticotropic hormone (ACTH) to stress. Although subcutaneous injection of selective antidiuretic analogue 1-desamino-8-D-AVP did not affect UI, intracerebroventricular (icv) administration of AVP reduced UI in DI rats, and icv administration of V1 antagonist [d(CH2)5Tyr(Me)]AVP elevated UI in LE rats. These results indicate that endogenous AVP plays a role in preventing the formation of gastric ulcers induced by stress via a central V1 receptor. Furthermore, we suggest that elevation of ACTH in plasma is not essential in the development of stress-induced gastric ulcer in rats.


2015 ◽  
Vol 11 (2) ◽  
Author(s):  
Mohammad Juffrie ◽  
Ina Rosalina ◽  
Wahyu Damayanti ◽  
Ali Djumhana ◽  
A. Ariani ◽  
...  

Hyperacidity causes gastric injury, and in severe situations, ulcer could develop. The growth factors known asthe basic fibroblast growth factor (bFGF) and the epidermal growth factor (EGF) have been recognized to promoteulcer healing. Fucoidan is extracted from a brown seaweed of Okinawa called Mozuku or Cladosiphon okamuranus.Fucoidan is effective for the healing of gastric ulcers by inducing epithelial cells to produce growth factors. The aimof this study is to explore the efficacy of fucoidan in patient who suffered by gastric ulcer. A randomized control trialdouble blind was conducted to 33 eligible samples. By using four-blocks random samples were divided into fucoidanand placebo groups. 100 mg of fucoidan was given to the fucoidan group and 100 mg of glucose was given to theplacebo group. Due to ethical reasons, for both groups were given a proton pump inhibitor. There was no differencein the age category between the fucoidan group (mean: 46.23 ± 14.8 years) and the placebo group (mean: 46.18 ± 18.4years) (p: 0.28). There was also no difference in sex between the fucoidan group (female: 10/33; male 7/33) and theplacebo group (female: 7/33; male: 9/33); p: 0.38. According to the SAKITA and MIWA criterias 32 patients fulfilledA1 which indicate active severe ulcer, and 1 patient fulfilled A2 which indicate active moderate ulcer. Most of theulcers were gastric ulcer. There was a significant improvement of the grade of ulcer in fucoidan group (94%) (16/17)compared to placebo group (37.5%) (6/16,p: 0.005). There was a significant reduction of abdominal pain after 5 daysin the fucoidan group, compared to the placebo group (p: 0.04). Vomiting tends to decrease in day 6 of the fucoidangroup however its proportion is similar with that of the placebo group (p: 0.9). Fucoidan is effective for ulcer healingand reducing ulcer symptoms.Key words : fucoidan, gastric ulcer, anti-peptic activity


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