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1.
Int J Pharm ; 663: 124564, 2024 Sep 30.
Artículo en Inglés | MEDLINE | ID: mdl-39117062

RESUMEN

PURPOSE: The present work seeks to develop, assess and refine a nanoethosomal vaginal in situ gel containing Berberine, aimed at enhancing its efficacy in treating Poly Cystic Ovary Syndrome (PCOS). This formulation aims to augment drug permeation, enable controlled release kinetics, and mitigate oral adverse effects commonly associated with Berberine administration. METHOD: Nanoethosomes formulated using diverse soya lecithin-ethanol concentrations within a 32 full-factorial-design, sought optimal formulations based on particle size and %entrapment-efficiency. Subsequent scrutiny involved PDI, Zeta potential and drug-content evaluation. TEM analysis authenticated morphology, while in vitro drug release from Nanoethosomes was examined. Pluronic F-127 concentrations (16%-21%w/v) were explored for the in situ gel, analyzing pH, gelation time and gelation temperature. The refined gel underwent evaluations for viscosity and in vitro diffusion. In vivo assessment covered pharmacokinetics, vaginal irritancy and Mifepristone-induced PCOS management, validated through histopathological and biochemical analysis, juxtaposing findings across normal, diseased, plain Berberine gel and standard metformin administered groups. RESULTS: Optimized Nanoethosomal Formulation(F3) displayed particle size of 183.5 nm, 82.58 % as %entrapment-efficiency, PDI of 0.137, -50.34 mV as zeta potential and 81.64 ± 1.57 % drug-content. TEM analysis confirmed spherical, nano-sized particles. In vitro studies exhibited 80.45 % drug release over 24 h. The formulated gel with 18 % Pluronic F-127 showed viscosity ranging from 193.01 ± 0.16cps to 1817.08 ± 1.67cps with temperature changes from 25 ± 2.0 °C to 38 ± 2.0 °C. In vitro diffusion revealed 85.99 %drug release from optimized gel. In vivo animal studies demonstrated increased plasma drug concentration, non-irritating properties in vaginal tests, and efficacy in managing Mifepristone-induced PCOS compared to other treatments. Short-term stability evaluations confirmed thermodynamic stability at room-temperature.


Asunto(s)
Berberina , Liberación de Fármacos , Síndrome del Ovario Poliquístico , Ratas Wistar , Cremas, Espumas y Geles Vaginales , Femenino , Animales , Berberina/administración & dosificación , Berberina/farmacocinética , Berberina/química , Berberina/farmacología , Síndrome del Ovario Poliquístico/tratamiento farmacológico , Cremas, Espumas y Geles Vaginales/química , Cremas, Espumas y Geles Vaginales/administración & dosificación , Vagina/efectos de los fármacos , Vagina/patología , Tamaño de la Partícula , Ratas , Administración Intravaginal , Poloxámero/química , Nanopartículas/química , Metformina/administración & dosificación , Metformina/farmacocinética , Metformina/química , Viscosidad
2.
J Diabetes Metab Disord ; 22(2): 1817, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37969921

RESUMEN

[This retracts the article DOI: 10.1007/s40200-021-00749-8.].

3.
Pharmacol Rep ; 75(6): 1454-1473, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37926795

RESUMEN

Snake bite is a neglected disease that affects millions of people worldwide. WHO reported approximately 5 million people are bitten by various species of snakes each year, resulting in nearly 1 million deaths and an additional three times cases of permanent disability. Snakes utilize the venom mainly for immobilization and digestion of their prey. Snake venom is a composition of proteins and enzymes which is responsible for its diverse pharmacological action. Snake venom phospholipase A2 (SvPLA2) is an enzyme that is present in every snake species in different quantities and is known to produce remarkable functional diversity and pharmacological action like inflammation, necrosis, myonecrosis, hemorrhage, etc. Arachidonic acid, a precursor to eicosanoids, such as prostaglandins and leukotrienes, is released when SvPLA2 catalyzes the hydrolysis of the sn-2 positions of membrane glycerophospholipids, which is responsible for its actions. Polyvalent antivenom produced from horses or lambs is the standard treatment for snake envenomation, although it has many drawbacks. Traditional medical practitioners treat snake bites using plants and other remedies as a sustainable alternative. More than 500 plant species from more than 100 families reported having venom-neutralizing abilities. Plant-derived secondary metabolites have the ability to reduce the venom's adverse consequences. Numerous studies have documented the ability of plant chemicals to inhibit the enzymes found in snake venom. Research in recent years has shown that various small molecules, such as varespladib and methyl varespladib, effectively inhibit the PLA2 toxin. In the present article, we have overviewed the knowledge of snake venom phospholipase A2, its classification, and the mechanism involved in the pathophysiology of cytotoxicity, myonecrosis, anticoagulation, and inflammation clinical application and inhibitors of SvPLA2, along with the list of studies carried out to evaluate the potency of small molecules like varespladib and secondary metabolites from the traditional medicine for their anti-PLA2 effect.


Asunto(s)
Mordeduras de Serpientes , Venenos de Serpiente , Animales , Ovinos , Humanos , Caballos , Venenos de Serpiente/uso terapéutico , Acetatos/uso terapéutico , Mordeduras de Serpientes/tratamiento farmacológico , Mordeduras de Serpientes/metabolismo , Fosfolipasas A2/metabolismo , Fosfolipasas A2/uso terapéutico , Inflamación
4.
J Biophotonics ; 16(8): e202300012, 2023 08.
Artículo en Inglés | MEDLINE | ID: mdl-37074708

RESUMEN

The loss and progressive dysfunction of neurons are hallmarks of neurodegenerative diseases. The aim of the current study is to explore the effects of photobiomodulation at 460-660 nm (100-1000 lux units) on the progression of scopolamine-induced cognitive dysfunctions in Wistar male rats. Photobiomodulation (PBM) is defined as "the use of monochromatic or quasi-monochromatic light from a low-power laser or light-emitting diode (LED) source to modify or modulate biological functions." Neuroprotective activity was assessed by in vivo models such as the Morris water maze, the elevated plus maze (EPM), and the T-maze. After using scopolamine (1 mg/kg/day) as a dementia induction model for 21 days, the induction was primarily due to impairments in cholinergic transmission, oxidative stress, and inflammation. The in vitro determinations, including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), reduced glutathione (GSH), malondialdehyde (MDA), superoxide dismutase (SOD), tumor necrosis factor-alpha (TNF-α), Interleukin 1 beta (IL-1ß), and alkaline phosphatase (ALP), were assessed biochemicals and biomarkers. The structural and morphological integrity of the cortex and hippocampus was investigated through histopathology. In vivo studies of exteroceptive behavior models such as the Morris water maze, the EPM, and the T-maze revealed that administration of scopolamine resulted in enhanced escape latency time (ELT), transfer latency (TL), and decreased percentage alternation, respectively. The levels of AChE, BChE, reduced, GSH, SOD, TNF-α, IL-1ß and ALP were increased, while MDA level was decreased. In contrast to normal and control groups with treatment groups, histopathology of the cortex and hippocampus examination revealed the maintenance of structural integrity and densities of CA1 and CA3 neuronal cells. However, network pharmacology predicted Ca+2 modulation of various pathways, among the treatments with red LED light showed highly significant amelioration compared with normal and control groups. Photobiomodulation by hormesis, chromophores in cells, and tissues excitation can influence neuroprotective effect mainly by scavenging of ROS, variation in the level of GSH MDA and SOD mitochondrial electron transfer, the improved abscopal effects on improved in gut microbiome by resembles the of fecal ALP level correlation of intestinal microbiome, cholinergic neurotransmissions, anti-inflammatory, and antioxidant activities.


Asunto(s)
Enfermedades Neurodegenerativas , Fármacos Neuroprotectores , Ratas , Masculino , Animales , Escopolamina/efectos adversos , Fármacos Neuroprotectores/farmacología , Fármacos Neuroprotectores/metabolismo , Fármacos Neuroprotectores/uso terapéutico , Acetilcolinesterasa/metabolismo , Acetilcolinesterasa/farmacología , Acetilcolinesterasa/uso terapéutico , Hormesis , Butirilcolinesterasa/metabolismo , Butirilcolinesterasa/farmacología , Butirilcolinesterasa/uso terapéutico , Factor de Necrosis Tumoral alfa/farmacología , Ratas Wistar , Aprendizaje por Laberinto , Trastornos de la Memoria/tratamiento farmacológico , Trastornos de la Memoria/inducido químicamente , Trastornos de la Memoria/metabolismo , Estrés Oxidativo , Colinérgicos/metabolismo , Colinérgicos/farmacología , Colinérgicos/uso terapéutico , Superóxido Dismutasa/metabolismo , Superóxido Dismutasa/farmacología , Superóxido Dismutasa/uso terapéutico , Hipocampo/metabolismo
5.
Metab Brain Dis ; 37(2): 411-426, 2022 02.
Artículo en Inglés | MEDLINE | ID: mdl-35023027

RESUMEN

Parkinsonism is a neurodegenerative disease, mainly imbalance in dopamine and acetylcholine neurotransimitter in mid brain, which manifestation of dysfunctions of extrapyramidal like akinesia, tremor, rigidity and catalepsy etc., even cognitive and memory loss. The current study is framed to evaluate the effect of Vitex negundo (VNL) leaf extract in Haloperidol induced PD in rats. In vitro studies of antioxidant capacity were checked via DPPH and NO assays and identified its Acetylcholinesterase (AChE) inhibitory activity. Secondly the In vivo study of anti-PD activity in Haloperidol induced in rats were evaluated by Rotarod, morris water maze (MWM), cooks pole climb (CPC), actophotometer, novel object recognition (NOR), and T-maze were utilized to assess extrapyramidal, cognitive and memory function. Thirdly, changes in biomarker level viz. (AChE), butyrylcholinesterase. (BChE) in hippocampus and cortex, reduced glutathione (GSH), malondialdehyde (MDA), total protein (TP), superoxide dismutase (SOD), catalase (CAT), and dopamine level in the whole brain were measured. Finally, histopathology of hippocampus and cortex was examined at 40x magnification to access restoring integrity and maintaining the architecture of neuronal cell in the treatment group compared to control group and L-DOPA as a standard treatment group. V. negundo showed potent antioxidant potency on scavenging of DPPH (IC50 84.81 µg/ml) and NO (IC50 133.20 µg/ml) and possess AChE inhibitory potency (IC50 114.35 µg/ml) by in vitro studies. The Rotarod, MWM, CPC, Actophotometer, NOR, T-maze demonstrated that Haloperidol group administration declines performance time, ELT, TL and decreases locomotion, cognitive and memory respectively. The treatment of VNL 100, 200, and 400 mg/kg p.o. significantly (p < 0.05 to p < 0.0001) reversed. Whole brain AChE, BChE, and MDA level were significantly raised and GSH, TP, SOD, CAT and Dopamine were significantly declined in Haloperidol treated group rats, especially V. negundo 400 mg/kg p.o. highly significantly ameliorate the Haloperidol group altered pathological changes through the restoration of the cholinergic function, enhancing the antioxidant defense and by increasing the dopaminergic function. The current study provides validation of V. negundo for its anti-PD activity and could be a valuable source for the treatment of PD in future.


Asunto(s)
Enfermedades Neurodegenerativas , Enfermedad de Parkinson , Vitex , Acetilcolinesterasa , Animales , Butirilcolinesterasa/farmacología , Haloperidol/farmacología , Neuroprotección , Estrés Oxidativo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Ratas
6.
J Diabetes Metab Disord ; 20(1): 329-340, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-34178841

RESUMEN

OBJECTIVE: The present study investigates the anti-obesity activity of Luffa cylindrica in progesterone induced obesity model. METHOD: Swiss albino mice were grouped into 7 (n = 6). Obesity was induced by administration of progesterone (10 mg/kg s.c.) for 28 days. Normal group received ad libitum and water. Disease control, positive control and treatment groups received progesterone (10 mg/kg s.c.). Further positive control group received Orlistat (10 mg/kg p.o). Treatment groups received hydro-alcoholic and fractionation extract of Luffa cylindrica at doses 400, 200, 100 mg/kg b.w. Food and water intake were recorded daily, Body weight, BMI and blood glucose were checked weekly. On completion of the study, animals were sacrificed and blood serum being utilized to accesses in vitro to estimate the various biochemical parameters. Serotonin levels and antioxidant biomarkers were also estimated. Histopathology of liver and adipose tissue was studied. RESULT: After the 28 days of treatment with plant extract and fraction, it was observed to improve the progestrogen-induced obesity by improving BMI, body weight, brain serotionin, locomotor activity, blood glucose level, anti-oxidant biomarkers, and lipid profile. CONCLUSION: After assimilating the In vivo and in vitro studies Luffa cylindrical extract highlighted the antilipidemic, anti-hyperglycaemic, antioxidant potential in hormone-induced obesity.

7.
Int J Biol Macromol ; 57: 238-44, 2013 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-23511060

RESUMEN

We investigated the lipid lowering ability of simvastatin loaded gellan gum-carrageenan composite polyspheres, which were prepared by ionotropic gelation/covalent crosslinking method. The surface morphology revealed that the polyspheres have rough and dense surface. The drug entrapment efficiency of the polyspheres prepared by ionic crosslinking was higher than those prepared by dual crosslinking. The in vitro drug release study indicated that the ionically crosslinked polyspheres discharged the drug quickly whereas, dual crosslinked polyspheres extended the drug release for longer period. The hypolipidemic activity performed on Wistar rats indicated that the polyspheres have effectively reduced the elevated total serum cholesterol and triglycerides.


Asunto(s)
Carragenina , Preparaciones de Acción Retardada , Inhibidores de Hidroximetilglutaril-CoA Reductasas , Polisacáridos Bacterianos , Simvastatina , Animales , Carragenina/química , Carragenina/farmacocinética , Carragenina/farmacología , Colesterol/sangre , Preparaciones de Acción Retardada/química , Preparaciones de Acción Retardada/farmacocinética , Preparaciones de Acción Retardada/farmacología , Polisacáridos Bacterianos/química , Polisacáridos Bacterianos/farmacocinética , Polisacáridos Bacterianos/farmacología , Ratas , Ratas Wistar , Simvastatina/química , Simvastatina/farmacocinética , Simvastatina/farmacología , Triglicéridos/sangre
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