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1.
Comb Chem High Throughput Screen ; 24(8): 1309-1321, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32928084

RESUMO

BACKGROUND: Boswellic acids are the main constituents of Boswellia serrata gum. These comprise of four pentacyclic triterpenes, 11-keto-ß-boswellic acid (KBA) being one of them. OBJECTIVES: Comparing the extraction efficiency of KBA through microwave-assisted extraction (MAE) and ultrasound-assisted extraction (UAE) followed by optimizing the extraction process using response surface methodology (RSM) and validation of HPTLC. METHODS: UAE and MAE of KBA were carried out employing methanol as an extracting solvent. To figure out the better mode of extraction, single factorial experiments were conducted for further optimization. Design expert software was used for optimization purposes where solvent to drug ratio, extraction temperature and extraction time were taken as input variables. Quantification of KBA in each extract was done through High-Performance Thin Layer Chromatography (HPTLC), and the method was validated as per International Council for Harmonization (ICH) guidelines. RESULTS: UAE stood out to be a better mode of extraction for KBA. Solvent to drug ratio of 20.42 mL/gram, extraction temperature of 44.01°C and extraction time of 11.54 minutes were established as optimum conditions, which yielded 8.44%w/w of KBA. Regarding HPTLC, the Rf value of KBA was measured, and the correlation coefficient was calculated from the standard curve. Accuracy, precision and recovery were found within limits. CONCLUSION: From this study, it was concluded that a non-thermal method is a better choice of extraction for KBA. All the input variables significantly affected KBA content, which was confirmed by model fitting. Moreover, the HPTLC method was developed for the quantification of KBA, which was found to be accurate, reliable and highly sensitive.


Assuntos
Boswellia , Franquincenso , Triterpenos , Boswellia/química , Cromatografia em Camada Fina/métodos , Extratos Vegetais/química , Triterpenos/química
2.
Biomed Pharmacother ; 97: 1514-1520, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29793314

RESUMO

Embelin is a natural compound possessing a plethora of pharmacological activities, including antidiabetic activity. When formulated as niosomes, embelin offers additional advantages of nanoformulations and can be further exploited for clinical use. An oral niosome formulation of embelin was developed using a thin-film hydration technique, and its antidiabetic activity was studied. The formulation was characterized in terms of entrapment efficiency, vesicle size and morphology, in vitro release profile, and stability. Antidiabetic evaluation was performed in streptozotocin (STZ)-induced diabetic Wistar rats. An antioxidant assay was carried out by evaluating superoxide dismutase (SOD), catalase (CAT), thiobarbituric acid reactive substances (TBARS), and glutathione (GSH). The optimized formulation showed a significant hypoglycemic effect, which was comparable with that of repaglinide. Moreover, significant increases in SOD, CAT, and GSH, along with a decrease in the lipid peroxidation level, were observed, which confirmed the antioxidant efficacy of the formulation. Thus, it is evident that the embelin-loaded niosome formulation was efficacious in diabetes management in Wistar rats.


Assuntos
Benzoquinonas/administração & dosagem , Benzoquinonas/uso terapêutico , Diabetes Mellitus Experimental/tratamento farmacológico , Administração Oral , Animais , Antioxidantes/metabolismo , Benzoquinonas/farmacologia , Varredura Diferencial de Calorimetria , Diabetes Mellitus Experimental/patologia , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Lipossomos/ultraestrutura , Tamanho da Partícula , Ratos Wistar , Estreptozocina
3.
Drug Deliv ; 23(3): 1079-84, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25116512

RESUMO

Luteolin (LUT) is a promising molecule with potential anti-arthritic activity. This investigation presents formulation and evaluation of niosomal transgel for enhanced transdermal delivery of LUT. Different non-ionic surfactants and vesicle compositions were employed for preparation of niosomes. The vesicle size analysis showed that all vesicles were in the range from 534.58 to 810.22 nm which favoured efficient transdermal delivery. The entrapment of LUT in vesicle was found to be higher in all surfactant. The developed formulation was proved significantly superior in terms of amount of drug permeation with an enhancement ratio of 2.66 when compared to a control formulation. The in vivo bioactivity studies revealed that the prepared niotransgel formulation of LUT was able to provide good anti-arthritic activity and the results were comparable to standard (diclofenac gel for anti-arthritic and analgesic). Finally, the results were confirmed through radiological analysis which proved that the prepared niotransgel was effectively able to treat arthritis and results were comparable with the standard formulation.


Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/química , Artrite/tratamento farmacológico , Luteolina/administração & dosagem , Luteolina/química , Pele/metabolismo , Tensoativos/química , Administração Cutânea , Animais , Química Farmacêutica/métodos , Diclofenaco/administração & dosagem , Diclofenaco/química , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Lipossomos/administração & dosagem , Lipossomos/química , Tamanho da Partícula , Ratos , Ratos Wistar , Absorção Cutânea
4.
Pharmacogn Mag ; 11(Suppl 1): S166-72, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26109763

RESUMO

BACKGROUND: Embelia ribes Burm is widely used medicinal plant for the treatment of different types of disorders in the Indian traditional systems of medicine. OBJECTIVE: The present work was aimed to optimize the extraction parameters of embelin from E. ribes fruits and also to quantify embelin content in different extracts of the plant. MATERIALS AND METHODS: Optimization of extraction parameters such as solvent: drug ratio, temperature and time were carried out by response surface methodology (RSM). Quantitative estimation of embelin in different extracts of E. ribes fruits was done through high performance liquid chromatography. RESULTS: The optimal conditions determined for extraction of embelin through RSM were; extraction time (27.50 min), extraction temperature 45°C and solvent: drug ratio (8:1). Under the optimized conditions, the embelin yield (32.71%) was equitable to the expected yield (31.07%, P > 0.05). These results showed that the developed model is satisfactory and suitable for the extraction process of embelin. The analysis of variance showed a high goodness of model fit and the accomplishment of the RSM method for improving embelin extraction from the fruits of E. ribes. CONCLUSION: It is concluded that this may be a useful method for the extraction and quantitative estimation of embelin from the fruits of E. ribes.

5.
Asian Pac J Trop Med ; 7S1: S289-93, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-25312138

RESUMO

OBJECTIVE: To find out the ideal organic solvent and extraction technique for the isolation of luteolin from the leaves of Vitex negundo Linn. (V. negundo) by quantitative estimation of luteolin through high performance liquid chromatography (HPLC) method. METHODS: The leaves of V. negundo were identified by a botanist, cleaned, dried under shade and powdered. Maceration, reflux, Soxhlet and ultrasound assisted extraction techniques were used for the extraction of luteolin from the leaves by using four different solvents of varying polarity such as methanol, ethanol, chloroform, and dichloromethane. A simple HPLC method was used to determine the quantity of luteolin in each sample extract. RESULTS: The calibration plot of standard luteolin showed a linear relationship in the concentration range of 100-500 µg/mL with a correlation coefficient, r(2) of 0.998. The methanolic extract was found to contain highest amount of luteolin and among various techniques employed for extraction and isolation of luteolin, reflux technique was observed to be the most efficient. CONCLUSION: Based on the HPLC results, it can be concluded that reflux technique using methanol is better than the other extraction techniques and should be preferred for the extraction and isolation of luteolin from V. negundo leaves extract in research labs or industries.

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