scholarly journals Preclinical Screening of Antidepressant Activity of Formulated Sertraline Hydrochloride-Loaded Solid Lipid Nanoparticles in Rats

Author(s):  
Sachin R. Hangargekar ◽  
Pradeep K. Mohanty ◽  
Janki Prasad Rai

Objective: The main goal of our study was to investigate the antidepressant activity of Formulated Sertraline hydrochloride-loaded Solid Lipid Nanoparticles (SLNPs) by using a rat forced swimming test (FST) and tail suspension test (TST). Materials and Methods: Animals were divided into three groups, consisting of six rats in each group. Out of these,  one  group  served  as  control  that received distilled water, second group was standard received Sertraline  HCl  (20  mg/kg  intranasal)  and  third  group  was  received  test formulation (SLNPs 50 mg/kg intranasal). To assess the effect of SLNPs on immobility activity through FST and TST were used to take as a measure of antidepressant activity. Results: SLNPs reduced the immobility duration in TST as well as in FST. In both methods, there was a statistical significant decrease in immobility of SLNPs group when compared to the control group. Conclusion: The results suggested that SLNPs produced significant antidepressant effect in rats which was comparable with control group and standard Sertraline HCl group animals.

Author(s):  
Kobra Kohansal ◽  
Abdollah Rafiei ◽  
Heibatullah Kalantari ◽  
Ali Jelowdar ◽  
Anayatollah Salimi ◽  
...  

Purposes: Cystic echinococcosis (CE) is a serious contemporary public health problem. Different CE treatment methods are of considerable importance, with albendazole (ABZ) being one of the most preferred drugs for CE treatment and prophylaxis. In this study, we evaluated the nephrotoxicity caused by ABZ and ABZ-loaded solid lipid nanoparticles (SLNs) in mice with experimental hydatid cyst. Methods: ABZ-loaded SLNs were produced by micro-emulsification and a high shear homogenization technique. Thereafter, we evaluated the physicochemical characterization of the product. Live protoscolices were injected into mice to induce experimental hydatidosis. Mice were then treated with ABZ and ABZ-loaded SLNs. The nephrotoxicity effects were evaluated by biochemical and histopathological surveys. Results: Significantly different blood urea nitrogen (BUN) levels were observed between the two infected groups (ABZ treatment and ABZ-loaded SLN treatment) and the control group. The kidney malondialdehyde (MDA) and glutathione (GSH) levels of the infected groups were not significantly different from those of the control group. The histopathological study revealed nephropathic and pathologic changes in the ABZ and ABZ-loaded SLN groups. Conclusion: ABZ formulated for ABZ-loaded SLNs had a more prominent chemoprophylactic efficacy on CE and fewer side effects than ABZ alone. Neither ABZ nor ABZ-loaded SLNs caused significant biochemical and histopathological defects on the kidney, and all functional biochemical markers stayed within the normal range. Therefore, ABZ-loaded SLNs could be a potential new product for CE treatment.


Author(s):  
Ajoy Borah ◽  
Binita Singha ◽  
Swopna Phukan

Objective: Depression is a major psychiatric disorder affecting nearly 350 million people worldwide and imposes a substantial health burden on the society. Ceftriaxone has demonstrated neuroprotective effects in animals. It has also undergone trials as a treatment option for amyotrophic lateral sclerosis. This study was therefore undertaken to evaluate the antidepressant-like effect of ceftriaxone in mice.Methods: Ceftriaxone was administered at three different doses (0.130, 0.195 and 0.260g/kg) to Swiss albino mice of either sex by intra peritoneal (i. p.) route. The period of immobility in control and drug-treated mice were recorded in forced swimming test (FST) and tail suspension test (TST). The antidepressant effect of ceftriaxone indicated by the decrease in duration of immobility was compared to that of fluoxetine (0.020 g/kg, i. p.).Results: Ceftriaxone decreased the duration of immobility in mice. It showed a significant dose-dependent antidepressant effect. The antidepressant effect of 0.260g/kg of ceftriaxone was comparable to that of fluoxetine in the TST but not in the FST.Conclusion: The results of the present study indicate antidepressant activity of Ceftriaxone. The study shows that ceftriaxone has additional action on the central nervous system other than neuroprotection. Ceftriaxone therapy in cases of encephalomeningitis and in various cases of hemorrhages in the brain can, therefore, prevent the development of depression in future


2021 ◽  
Author(s):  
Burcu Üner ◽  
Samet Özdemir ◽  
Çetin Taş ◽  
Yıldız Özsoy ◽  
Melike Üner

Abstract Purpose Loteprednol etabonate (LE) is a new generation corticosteroid that is used for the treatment of inflammatory and allergic conditions of the eye, and management of seasonal allergic rhinitis nasally. LE which is a poorly soluble drug with insufficient bioavailability, has a high binding affinity to steroid receptors. Sophisticated colloidal drug delivery systems of LE could present an alternative for treatment of inflammatory and allergic conditions of the skin. For this purpose, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were attempted to improve for transdermal LE delivery for the first time. Methods SLN and NLC were produced by hot homogenization and ultrasonication technique. Formulations were characterized by dynamic light scattering, scanning electron microscopy, fourier transform infrared spectroscopy and differential scanning calorimetry. Their physical stability was monitored for 3 months of storage. Drug release profiles and permeation properties of SLN and NLC through the porcine skin were investigated. Results It was determined that SLN and NLC below 150 nm particle size had a homogeneous particle size distribution as well as high drug loading capacities. They were found to be stable both physically and chemically at room temperature for 90 days. In terms of release kinetics, it was determined that they released from SLN and NLC in accordance with Fickian diffusion release. Formulations prepared in this study were seen to significantly increase drug penetration through pig skin compared to the control group (p ≤ 0.05). Conclusion SLN and NLC formulations of LE can be stated among the systems that can be an alternative to conventional systems with less side-effect profile in the treatment of inflammatory problems on the skin.


2020 ◽  
Vol 194 ◽  
pp. 111209 ◽  
Author(s):  
Isra Rana ◽  
Namrah Khan ◽  
Muhammad Mohsin Ansari ◽  
Fawad Ali Shah ◽  
Fakhar ud Din ◽  
...  

Acta Naturae ◽  
2013 ◽  
Vol 5 (4) ◽  
pp. 105-109 ◽  
Author(s):  
S. B. Seredenin ◽  
T. A. Voronina ◽  
T. A. Gudasheva ◽  
T. L. Garibova ◽  
G. M. Molodavkin ◽  
...  

A large amount of clinical and experimental data suggest the involvement of neurotrophins, in particular the brain-derived neurotrophic factor (BDNF), in depression pathogenesis. However, the therapeutic use of BDNF is limited because of its instability in biological fluids, poor blood-brain barrier (BBB) permeability, and the presence of side effects. A low-molecular-weight mimetic GSB-106, which is a substituted dimeric dipeptide bis(N-monosuccinyl-L-seryl-L-lysine)hexamethylenediamide, was designed and synthesized based on the BDNF fourth loop structure at the V.V. Zakusov Institute of Pharmacology (RAMS). GSB-106 was found to exhibit an antidepressant activity in various models of depressive-like state when administered intraperitoneally to outbred mice and rats. An effect for the substance, when administered daily for 4-5 days, was detected in the Porsolt forced swimming test (0.1 and 1.0 mg/kg) and in the tail suspension test in mice (1.0 and 1.5 mg/ kg). An effect for GSB-106 at doses of 0.1 and 0.5 mg/kg was observed after a single application in experiments on rats in the Nomura water wheel test. The obtained evidence supports the hypothesis on the involvement of BDNF in the pathogenesis of various depression conditions, thus opening prospects for searching for new original antidepressants.


Author(s):  
Y. Indira Muzib ◽  
E. Ramya ◽  
Y. R. Ambedkar

Pioglitazone HCl is an oral anti-diabetic agent used for the treatment of diabetes mellitus type II. The aim of the present work is to evaluate the pharmacodynamic activity of solid lipid nanoparticles of pioglitazone HCL prepared by using solvent injection technique and to compare with the control and test group. Among all the formulations, F5 was found to possess highest in-vitro drug release within 24 hrs i.e., 95.02±1.26%. The in vivo studies were performed using male albino rats of wistar strain (150-200g). Rats were divided in to five groups (n=6), group-I normal, group-II diabetes control, group-III   placebo control, group-IV reference, group-V test group. Diabetes was induced by streptazocin (60 mg/kg) by intraperitonial route. The reference group was treated with marketed tablet of pioglitazone HCL, test groups were treated with SLNs suspended in 0.1% Tween 80 and given to animals through oral gavages. Blood samples were collected by retro-orbital puncture before treatment, and after treatment at time intervals 0, 2, 4, 6, 8, 10, 12 and 24h in anti-coagulated vials. Parameters like glucose, tri glycerides (TG), total cholesterol (TC) and HDL-C were estimated by calorimetric method.  Diabetes induced rats showed elevated levels of glucose, TG, TC and reduced HDL. The oral administration of drug loaded SLNs in 0.1% Tween 80 solution showed reduced levels of glucose, TG and elevated levels of HDL-C and slightly reduced levels of TG in 24 h where as the marketed tablet showed reduced levels of glucose, TG and TC up-to 12 h and in 24thh  the glucose levels get elevated. Thus the optimized SLNs showed prolonged activity.


2019 ◽  
Vol 9 (1) ◽  
pp. 244-247 ◽  
Author(s):  
Sucheta Gautam ◽  
Neetu Sachan ◽  
Alankar Shrivastav ◽  
Dilipkumar Pal

Abstract Objective: Abies webbiana and Berberis aristata is an herbal plant that has several therapeutic effects. It also heals depression, grief, nervous stress and tension. In the present study we evaluated anti-depressant effect of ethanolic extract from Abies webbiana and Berberis aristata by using Forced Swimming Test (FST) and Tail Suspension Test (TST). Methods: Two doses of ethanolic extract of Abies webbiana and berberis aristata (200 mg/kg and 400 mg/kg) was given orally. Immobility time were measured after 30 min after the dosing and compared with control group and Flouxetine (25mg/kg) as a standard group. Results: The ethanolic extract of BA and AW (400 mg/kg) was found to be effective and it exhibited activity similar to that of the conventional drug Flouxetine (25mg/kg) (p<0.001) whereas 200 mg/kg dose showed higher activity with significantly increased swimming time and suspension time and decreased immobility time than 400 mg/kg of ethanolic extracts and Flouxetine (25mg/kg). Conclusion: These results proposed 400 mg/kg of ethanolic extract was showed higher anti-depressant activity as compared to control which is similar to the standard.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Parastoo Mojtahed Zadeh-Ardabili ◽  
Sima Kianpour Rad ◽  
Soheila Kianpour Rad ◽  
Abolfazl Movafagh

AbstractOxidative stress has significant role in pathophysiology of any kind of depression through actions of free radicals, non-radical molecules, and unbalancing antioxidant systems in body. In the current study, antidepressant responses of fish oil (FO), Neptune krill oil (NKO), vitamin B12 (Vit B12), and also imipramine (IMP) as the reference were studied. Natural light was employed to induce stress in the animals followed by oral administration of the drugs for 14 days. The antidepressant effect was assessed by tail suspension test (TST) and forced swimming test (FST), antioxidant enzymes and oxidative stress markers were then measured in the brain tissue of the animals. The administration of FO and NKO could significantly reduce the immobility of the animals; while, increasing climbing and swimming time compared to the normal saline in CUS-control group in TST and FST, similarly to IMP but not with Vit B12. Vit B12 could not effect on SOD activity and H2O2 level, but, cause decrease of the malondialdihydric (MDA) level and CAT activity, as well as increased the GPx and GSH activities. The rest treatments led to decrease of MDA, H2O2 levels and CAT activity and increase of GPx, SOD, GSH activities.


2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
P. Vijayanand ◽  
V. Jyothi ◽  
N. Aditya ◽  
A. Mounika

In alternate systems of medicine like Ayurveda and traditional Chinese medicine, Hibiscus rosa sinensis and its extracts have been traditionally prescribed for their antidepressant activity. Crude extracts and rudimentary formulations approaches are good for proof-of-concept studies; however, these formulations are fraught with problems like poor oral bioavailability and high variability between subjects. Systematic drug delivery approaches could prove effective in addressing some of these problems. In this study, we report the development of Hibiscus rosa sinensis extract loaded solid lipid nanoparticles (HSLNs) using glycerol monostearate or beeswax as lipids. The HSLNs were evaluated for their size, surface charge, and morphology. The optimized HSLNs were tested for antidepressant activity in male Swiss albino mice. It was found that, with the optimized procedure, HSLNs of ~175 nm, carrying negative charge and nearly spherical shape, could be obtained. The in vivo test results suggested that there were marked differences in the immobility times of the test animals. Moreover, with HSLNs, it was found that at doses several times lower than the native crude extract dose, similar pharmacological effect could be obtained. These initial findings suggest that encapsulating phytopharmaceuticals into advanced delivery systems like solid lipid nanoparticles can be an effective strategy in improving their in vivo performance.


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