Impact of quercetin on pharmacokinetics of quetiapine: insights from in-vivo studies in wistar rats

Xenobiotica ◽  
2020 ◽  
Vol 50 (12) ◽  
pp. 1483-1489
Author(s):  
Priyadeep Bhutani ◽  
Prabhakar K. Rajanna ◽  
Atish T. Paul
Keyword(s):  
Author(s):  
Carlos Edmundo Rodrigues FONTES ◽  
Ana Paula de ABREU ◽  
Aretuza Zaupa GASPARIM

ABSTRACT Background: Researches on Chagas disease still use several animals and rats, due to size and susceptibility were preferred by many authors. Aim: To develop an experimental model of megacolon in rats inoculated with the strain Y of Trypanosoma cruzi. Methods: Thirty male Wistar rats were distributed in three groups inoculated with different inoculants: Group A: 600000, Group B: 1000000 and Group C: 1500000 blood trypomastigotes of T. cruzi. Animals were sedated intramuscularly at zero inoculation time (T0) and 60 days after inoculation (T60), to perform the barium enema in order to evaluate the dilatation of the different segments of colon in a comparative study of the measurements obtained, using a digital caliper. Evidence of infection was performed by blood smear collected from the animal’s tail 18 days after inoculation with observation of blood forms. Results: Comparing the intestinal diameter of the inoculated animals with 60,0000 trypomastigotes in the T0 of infection with T60 days after the inoculation, significant dilatation was observed between the proximal, medial and distal segments (p<0.01), indicating the establishment of the megacolon model. In addition, comparing intestinal diameter between the different segments, with in the T0 of infection and the T60 after inoculation, significant alterations were observed (p<0.05). Conclusion: The proposed model was possible for in vivo studies of alterations due to infection by T. cruzi and functional alterations of the colon. In addition, the changes manifested in the colon are not directly proportional to the size of the inoculum, but to the time of infection that the animals were submitted, since the animals inoculated with 60,0000 blood forms were the ones which presented the most significant alterations.


2019 ◽  
Vol 20 (7) ◽  
pp. 1572 ◽  
Author(s):  
Diego López Tenorio ◽  
Carlos Valencia ◽  
Cesar Valencia ◽  
Fabio Zuluaga ◽  
Mayra Valencia ◽  
...  

In the last few years, graphene oxide (GO) has gained considerable importance in scaffold preparation for tissue engineering due to the presence of functional groups that allow the interaction between the extracellular matrix and the components of the cellular membrane. The interaction between GO and chitosan (CS) can not only improve the biomechanical properties of the scaffold but also generate a synergistic effect, facilitating tissue recovery. In vivo studies on GO are scarce; therefore, biocompatibility tests on CS-GO scaffolds and bone regeneration experiments on critical size defects were carried out on Wistar rats. Scaffolds made of CS, CS-GO 0.5%, and CS-GO 1% were prepared and implanted on Wistar rats cranial bones for three months. Scaffold samples were analyzed through histochemistry and scanning electron microscopy. The analysis performed showed reabsorption of the material by phagocytic activity and new bone formation. The CS-GO 0.5% formulation gave the best performance in bone regeneration, with excellent biocompatibility. These results show the potential of this compound for tissue regeneration opening and medical applications.


2021 ◽  
Vol 22 (22) ◽  
pp. 12277
Author(s):  
En-Shao Liu ◽  
Nai-Ching Chen ◽  
Tzu-Ming Jao ◽  
Chien-Liang Chen

Medial vascular calcification has emerged as a key factor contributing to cardiovascular mortality in patients with chronic kidney disease (CKD). Vascular smooth muscle cells (VSMCs) with osteogenic transdifferentiation play a role in vascular calcification. Nicotinamide adenine dinucleotide phosphate (NADPH) oxidase inhibitors reduce reactive oxygen species (ROS) production and calcified-medium–induced calcification of VSMCs. This study investigates the effects of dextromethorphan (DXM), an NADPH oxidase inhibitor, on vascular calcification. We used in vitro and in vivo studies to evaluate the effect of DXM on artery changes in the presence of hyperphosphatemia. The anti-vascular calcification effect of DXM was tested in adenine-fed Wistar rats. High-phosphate medium induced ROS production and calcification of VSMCs. DXM significantly attenuated the increase in ROS production, the decrease in ATP, and mitochondria membrane potential during the calcified-medium–induced VSMC calcification process (p < 0.05). The protective effect of DXM in calcified-medium–induced VSMC calcification was not further increased by NADPH oxidase inhibitors, indicating that NADPH oxidase mediates the effect of DXM. Furthermore, DXM decreased aortic calcification in Wistar rats with CKD. Our results suggest that treatment with DXM can attenuate vascular oxidative stress and ameliorate vascular calcification.


2002 ◽  
Vol 282 (6) ◽  
pp. F1034-F1042 ◽  
Author(s):  
David A. Spector ◽  
James B. Wade ◽  
Russell Dillow ◽  
Deborah A. Steplock ◽  
Edward J. Weinman

Although mammalian urothelia are generally considered impermeable to constituents of urine, in vivo studies in several species indicate urothelial transport of water and solutes under certain conditions. This study investigates the expression, localization, and regulation of aquaporin (AQP)-1, -2, and -3 in ureteral and bladder tissues in 48-h dehydrated and water-loaded female Wistar rats. Immunoblots of homogenates of whole ureter and bladder identified characteristic ∼28- and 35- to 44-kDa bands for AQP-1, -2, and -3. AQP-1 was localized to capillary and arteriole endothelial cells, whereas AQP-2 and -3 circumferentially lined the epithelial cell membranes except for the apical membrane of the epithelial cells adjacent to the lumens of both ureter and bladder. AQP-2 was also present in epithelial cell cytoplasm. Dehydration resulted in 160–200% increases of AQP-3 signal and 24–49% increases of AQP-2 signal but no change in AQP-1 signal on immunoblots of homogenates of ureters and bladders. AQPs in genitourinary tract urothelia likely play a role in the regulation of epithelial cell volume and osmolality and may play a role in bulk water movement across urothelia.


Nutrients ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 2770 ◽  
Author(s):  
Lídia L. R. Matias ◽  
Rafael O. A. Costa ◽  
Thaís S. Passos ◽  
Jaluza L. C. Queiroz ◽  
Alexandre C. Serquiz ◽  
...  

In vivo studies show the benefits of the trypsin inhibitor isolated from tamarind (Tamarindusindica L.) (TTI) seeds in satiety and obesity. In the present study, TTI nanoencapsulation (ECW) was performed to potentialize the effect of TTI and allow a controlled release in the stomach. The impact on glycemia, insulin, and lipid profile was evaluated in Wistar rats overfed with a high glycemic index diet (HGLI). Characterization of the nanoparticles and in vitro stability in simulated gastrointestinal conditions, monitored by antitrypsin activity and HPLC, was performed. ECW and empty nanoparticles (CW) were administered by gavage, using 12.5 and 10.0 mg/kg, respectively. Both nanoformulations presented a spherical shape and smooth surface, with an average diameter of 117.4 nm (24.1) for ECW and 123.9 nm (11.3) for CW. ECW maintained the antitrypsin activity (95.5%) in the gastric phase, while TTI was completely hydrolyzed. In Wistar rats, the nanoformulations significantly reduced glycemia and HOMA IR, and ECW increased HDL-c compared to CW (p < 0.05).Pancreas histopathology of animals treated with ECW suggested an onset of tissue repair. Thenanoencapsulation provided TTI protection, gradual release in the desired condition, and improvement of biochemical parameters related to carbohydrate metabolism disorders,without compromising insulinemia.


2020 ◽  
Vol 18 (4) ◽  
pp. 237-247
Author(s):  
Salome A. Chime ◽  
Godswill C. Onunkwo ◽  
Anthony A. Attama

Background: Lipid based formulations have been confirmed to lower some side effects of drug and can be tailor made to offer sustained drug release of drugs with short half-life like stavudine. Aim: To evaluate the immunomodulatory properties of stavudine-loaded solid lipid microparticles (SLMs) using immunocompromised Wistar rats. Methods: The SLMs were formulated by homogenization method. The optimized batches were used for further in vivo studies. The effect of formulation on the CD4 count and the haematological properties of immunocompromised Wistar rats were studied. Results: The particle size range of 4 -8 µm, EE range of 85-93 % and maximum drug release at 10 h. The CD4 cells increased from 115 ± 3.17 cell/mm3 at day zero to 495 ± 5.64 cell/mm3 at day 14 of treatment and 538 ± 6.31 cell/mm3 at day 21. The red blood cells increased from 2.64 ± 1.58 (x 106 /mm3 ) at day zero to 6.96 ± 3.47 (x 106 /mm3 ) at day 14 and 7.85 ± 3.64 (x 106 /mm3 ) at day 21. PCV increased significantly (p < 0.05) to about 42 – 50 % at day 21 in the groups that received the SLMs formulations. The white blood cells (WBC) also were 12 x 103 /mm3 , for SLM formulations, while the rats that received plain stavudine exhibited WBC of 9.6 x 103 /mm3 at day 21. The histopathological studies revealed that oral stavudine-loaded SLMs had no significant damage to the kidney, liver, spleen and the brain of Wistar rats. Conclusion: Formulations exhibited significantly higher immunomodulatory properties than plain stavudine (p<0.05) and showed good properties for once daily oral administration and could be a better alternative to plain stavudine tablets for the management of patients living with HIV.


2001 ◽  
Vol 5 (8) ◽  
pp. 645-651
Author(s):  
M. Peeva ◽  
M. Shopova ◽  
U. Michelsen ◽  
D. Wöhrle ◽  
G. Petrov ◽  
...  
Keyword(s):  

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