Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting

Nanotechnology Science and Applications, Journal Year: 2024, Volume and Issue: Volume 17, P. 1 - 19

Published: Jan. 1, 2024

Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation develop enhanced intranasal binary nano-ethosome gel.‎. Methods: Binary ethosomes prepared using different concentrations phospholipid PLH90, ethanol, propylene glycol, cholesterol by thin film hydration characterized particle size, zeta potential, entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, histopathological studies done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best parameters other formulas; with lowest size (154.1± 4.38‎ nm), PDI (‎ 0.213± 0.05), highest potential (‎-46.94± 1.05), efficiency (89.34± 2.37%). gel formulation, G2 showed drug content 99.82± 0.02‎%) spreadability (12.88 g/cm 2 ). In-vitro study results that, in first 30 minutes, around 22.3% released, whereas, after 24 hours, about 98.56% released G2. Conclusion: Based on enhancing bioavailability sustaining release, it can be concluded that Frovatriptan-Loaded ethosome Gel as nano-delivery was developed a promising non-invasive delivery system for treating migraine. Keywords: intranasal, frovatriptan, brain delivery,

Language: Английский

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Evaluation of empagliflozin efficacy as a promising anti-aging treatment in mice: In-vivo study

Pharmacia, Journal Year: 2024, Volume and Issue: 71, P. 1 - 9

Published: Jan. 17, 2024

Aim : Evaluation of the anti-aging properties Empagliflozin (EMP) associated with aging process in mice. Methods The mice were allocated into four groups: negative control received normal saline without receiving D-galactose (DGA); all three other groups DGA (200 mg/kg/day orally) for eight weeks; second group saline; third vitamin C, final EMP and continued another weeks. Results Treatment reduced levels TNF-α, IL-1β, MDA significantly compared to induction (91.7±9.6 ng/ml, 30.6±5.5 pg/ml, 66.7±8.3 ng/ml vs. 304.0±102.9 70.2±6.8 204.7±56.9 ng/ml; respectively), while GSH-Px increased (3.3±0.6 0.3±0.2 ng/ml). In addition, increases level both COL-1 COL-3 (1,783.6±186.9, 1,583.6±186.9, 885.7±242.5, 685.7±242.5 pg/ml; respectively). Conclusion positively affects several parameters

Language: Английский

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SGLT2i relieve proteinuria in diabetic nephropathy patients potentially by inhibiting renal oxidative stress rather than through AGEs pathway

Diabetology & Metabolic Syndrome, Journal Year: 2024, Volume and Issue: 16(1)

Published: Feb. 16, 2024

Abstract Aims To estimate the effects of sodium-glucose cotransporter 2 inhibitor (SGLT2i) on proteinuria and oxidative stress expression in type diabetes patients. Materials methods 68 patients with mellitus (T2DM) were divided into three groups according urinary albumin-to-creatinine ratio (UACR), including T2DM non-albuminuria group (UACR < 30 mg/g), microalbuminuria (30 ≤ UACR 300 macroalbuminuria (UACR>300 mg/g). They all received SGLT2 inhibitors treatment for 12 weeks. The advanced glycation end products (AGEs) plasma 8-hydroxy-2-deoxyguanosine (8-OHdG) urine measured as indications stress. 24-hour samples collected to measure concentration 8-OHdG before after weeks SGLT2i treatment. Plasma renin activity (PRA), angiotensin II (Ang II) Aldosterone (ALD) evaluate aldosterone system (RASS) levels. Results After treatment, median values decreased compared baseline (970 vs. 821 mg/d, P = 0.006). AGEs when baseline, (777 136 ug/ml, 0.003) (755 210 0.001), (8.00 1.88 ng/ml, 0.001) (11.18 1.90 respectively. Partial correlations showed that relevant 24-h ( r 0.389, p reduction OHdG (Δ8-OHdG) positively correlated decrease (Δ24-h proteinuria) 0.283, 0.031). There was no significant correlation between −0.059, 0.640) well ΔAGEs Δ24-h 0.022, 0.872) after12 Conclusions may reduce diabetic nephropathy patients, potentially by inhibiting renal stress, but not through pathway does induce RAAS activation. Trial registration This clinical trial registered 15/10/2019, ClinicalTrials.gov, registry number is NCT04127084.

Language: Английский

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Glp-1 Mimetic of Sitagliptin Improved Oxidative Stress and Liver Function Tests via Suppressing NOX-4 Enzyme in Hepatic Tissues of Diabetic Rats

Biochemical and Biophysical Research Communications, Journal Year: 2025, Volume and Issue: unknown, P. 151455 - 151455

Published: Feb. 1, 2025

Language: Английский

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In vivo Brain Pharmacokinetics of Dolutegravir Sodium-Loaded Nanostructured Lipid Carrier in situ Gel: Comparative Study with an Intravenous Drug Solution

Al-Rafidain Journal of Medical Sciences ( ISSN 2789-3219 ), Journal Year: 2025, Volume and Issue: 8(1), P. 115 - 125

Published: Feb. 22, 2025

Background: Dolutegravir sodium (DTG), used to treat HIV, faces challenges in delivering effective therapeutic concentrations the brain due blood-brain barrier (BBB). Nanostructured lipid carriers (NLCs) combined with situ gels present a promising strategy for enhancing drug delivery via intranasal route. Objective: To compare pharmacokinetics of DTGs delivered NLC-loaded gel administration conventional intravenous (IV) solution. Methods: 80 Wistar rats, which were divided into three groups: two groups consisting 39 animals each and control group 2 animals. Rats administered dose 1.0 mg/kg IV, intranasally. determined rats’ plasma tissue by high-performance liquid chromatography (HPLC). Results: Intranasal produced significantly higher (Cmax 35344.8ng/ml) compared IV solution 4536.85ng/ml). The area under curve (AUC) formulation was twice that solution, indicating enhanced bioavailability. Furthermore, route exhibited faster onset (lower Tmax) prolonged retention tissue. developed nanoformulation Drug Targeting Efficiency (DTE) 232.5% Potential (DTP) 57%, suggesting improved targeting efficiency. Conclusions: DTGs-loaded NLC shows superior administration, highlighting its potential as an targeting.

Language: Английский

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Empagliflozin demonstrates neuroprotective and cardioprotective effects by reducing ischemia/reperfusion damage in rat models of ischemic stroke and myocardial infarction

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: March 15, 2025

Sodium-glucose co-transporter 2 (SGLT2) inhibitors have demonstrated potential neuroprotective and cardioprotective effects in preliminary studies. This study evaluates the efficacy of empagliflozin (EMPA) reducing ischemia/reperfusion damage both brain heart using rat models. Ischemic stroke myocardial infarction (MI) were induced male Sprague-Dawley rats, which randomized into three groups: (1) Control (no EMPA), (2) Acute treatment (EMPA, 10 mg/kg IV, administered min before ischemia 1 reperfusion), (3) Chronic 20 food for 7 days ischemia). Stroke was by middle cerebral artery occlusion (MCAO) one hour, followed 3 h reperfusion, MI left coronary 30 min, reperfusion. Brain tissues analyzed anatomic size stroke. In brain, significantly smaller EMPA groups compared to controls (acute: 3.7 ± 1.2%, chronic: 6.9 2.1% vs. control: 14.5 2.5%, p < 0.05). Edema also reduced 5.5 0.9%, 5.9 0.8% 9.6 heart, 46.9 2.0%, 48.8 5.8% 70.0 2.6%, 0.05), no-reflow 36.3 3.3%, 33.9 4.3% 53.4 treatment, acute chronic, reduces infarct volume edema, as well models ischemic ischemia/reperfusion, indicating substantial effects.

Language: Английский

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Effect of Empagliflozin on Serum Ferritin and Its Relationship With Inflammatory Markers in Prediabetic and Diabetic Patients

Journal of Diabetes Research, Journal Year: 2025, Volume and Issue: 2025(1)

Published: Jan. 1, 2025

Background: This research is aimed at evaluating the effects of SGLT2 inhibitor empagliflozin on inflammatory markers, some iron metabolism and their interrelationships before after using empagliflozin. Methods: A quasiexperimental study was conducted 44 prediabetic Type 2 diabetic patients aged 18–65 years. The participants were among those treated clinic affiliated with Kerman Medical Sciences University between 2022 2023. included HbA1c levels 0.5%–1% higher than therapeutic target who not blood sugar control medication. Each patient received a daily dose 10 mg for 3 months. Changes in serum iron, total iron‐binding capacity (TIBC), ferritin, transferrin saturation, markers IL‐6, C‐reactive protein (CRP), uric acid measured months commencing Results: Three starting empagliflozin, mean FPG Hb A1c showed drop ( p < 0.05). ferritin level decreased, TIBC increased significantly 0.05) following treatment. Additionally, CRP 0.05), IL‐6 0.001), 0.001) declined. Analysis correlation use revealed positive = 0.04) 0.03). However, no significant observed change 0.22). Conclusion: Following treatment, interleukin‐6, CRP, declined, indicating relationship inhibition, inflammation, metabolism. Furthermore, suggests that reduced may result from inflammation. Trial Registration: ClinicalTrials.gov identifier: IRCT20090317001774N10

Language: Английский

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The reno-protective effect of Empagliflozin against carbon tetrachloride (CCl4)-induced nephrotoxicity in mice halting JNK/MKK4/NRF2/NF-KB pathway

Food and Chemical Toxicology, Journal Year: 2025, Volume and Issue: unknown, P. 115439 - 115439

Published: April 1, 2025

Language: Английский

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Anti-angiogenesis efficacy of the aqueous extract of Allium sativum and its combination with melatonin in an animal model: in vivo and ex vivo studies

Pharmacia, Journal Year: 2024, Volume and Issue: 71, P. 1 - 8

Published: June 3, 2024

To better understand Allium sativum ’s anti-angiogenesis activity, we undertook this study to examine its effect on the ex vivo rat aortic ring and in chick chorioallantoic membrane. Additionally, compare activity melatonin benefits of their combination. The included six albino male rats (aged 5–7 weeks). were euthanized, then thoracic aorta was removed cut into rings that 1 mm thick. divided three groups: a negative control (1% v/v DMSO), positive (100 μg/mL melatonin), an aqueous extract. test compounds subjected serial dilutions obtain 100, 50, 25, 12.25, 6.25 concentrations. In addition, membrane also undertaken. significantly inhibited ring; IC 50 calculated (IC = 8.04 for 3.313 melatonin). zone inhibition melatonin, , combination showed had strongest CAM assay. This scored (++) (+++), respectively. conclusion, extract provides potent effect, with synergistic further enhancing effect.

Language: Английский

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Design and optimization of pantoprazole sodium mucoadhesive hydrogel microcapsules for the healing of peptic ulcers

Pharmacia, Journal Year: 2024, Volume and Issue: 71, P. 1 - 14

Published: July 18, 2024

Hydrogels have gained much focus as a gastro-retentive technology for drug delivery. The current study aimed to design an oral mucoadhesive sustained-release dosage form lower peptic ulcer complications (PUC). Using the Box-Behnken statistical design, preparation method was developed by incorporating pantoprazole sodium (PZS) into hydrogel microcapsules (HGMC). PZS incorporated HGMC via ion gelation technique, with alginate gelling agent, calcium chloride crosslinking and chitosan agent sustained release. optimized formulation of PZS-HGMC showed diameter 2.506 mm, swelling rate 838.2%, encapsulation efficiency 93.8%. Scanning electron microscopy images revealed microcapsules’ spherical shape. in vitro release from after two hours simulated gastric fluid 13.2%1±0.08%, compared apparent solubility pure under same conditions (95.24%±3.2%). After 24 hours, percent released formula 69.84±2.4%, which indicates pattern. results vivo demonstrated improved healing induced ulcers rats when treated standard therapy; therefore, obtained considered potential delivery strategy PUC therapy.

Language: Английский

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