Cribado de la actividad hipoglucémica in vitro de Murraya koenigii y Catharanthus roseu

Objective: The study aimed to verify the hypoglycemic effect of Murraya koenigii (M. koenigii) and Catharanthus roseus (C. roseus) by using various in-vitro techniques. Method: The extracts were studied for their effects on glucose adsorption capacity, in-vitro glucose diffusion, in-vitro amylolysis kinetics and glucose transport across the yeast cells. Results: It was observed that the extracts of M. koenigii and C. roseus adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both the plant extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The extracts also promoted glucose uptake by the yeast cells and the enhancement of glucose uptake was dependent on both the sample and glucose concentration. The extract of M. koenigii exhibited significantly higher (p≤0.05) activity than the extract of C. roseus at all concentrations used in the study. Our report suggests the mechanism(s) for the hypoglycemic effect of M. koenigii and C. roseus. Conclusion: The said effect was observed to be mediated by inhibiting alpha amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by in-vitro model of yeast cells. However, these effects need to be affirmed by using different in vivo models and clinical trials.Objetivo: El estudio tuvo como objetivo verificar el efecto hipoglucémico de Murraya koenigii (M. koenigii) y Catharanthus roseus (C. roseus) mediante el uso de diversas técnicas in vitro. Método: Los extractos se estudiaron por sus efectos sobre la capacidad de adsorción de glucosa, la difusión de glucosa in vitro, la cinética de amilolisis in vitro y el transporte de glucosa a través de las células de levadura. Resultados: se observó que los extractos de M. koenigii y C. roseus adsorbieron glucosa y la adsorción de glucosa aumentó notablemente con un aumento en la concentración de glucosa. No hubo diferencias significativas (p≤0.05) entre sus capacidades de adsorción. En el modelo experimental cinético de amilolisis, se encontró que la velocidad de difusión de glucosa aumentaba con el tiempo de 30 a 180 min y ambos extractos de planta exhibían efectos inhibitorios significativos sobre el movimiento de la glucosa hacia la solución externa a través de la membrana de diálisis en comparación con el control. Los extractos también promovieron la absorción de glucosa por las células de levadura y la mejora de la captación de glucosa dependió tanto de la muestra como de la concentración de glucosa. El extracto de M. koenigii exhibió una actividad significativamente mayor (p≤0.05) que el extracto de C. roseus en todas las concentraciones utilizadas en el estudio. Nuestro informe sugiere el mecanismo (s) para el efecto hipoglucemiante de M. koenigii y C. roseus. Conclusión: Se observó que dicho efecto estaba mediado por la inhibición de la alfa amilasa, la inhibición de la difusión de glucosa por la adsorción de glucosa y el aumento del transporte de glucosa a través de las membranas celulares según lo revelado por el modelo in vitro de células de levadura. Sin embargo, estos efectos deben ser afirmados mediante el uso de diferentes modelos in vivo y ensayos clínicos

In vitro hypoglycemic effects of unripe and ripe fruits of Musa sapientum

The present study was undertaken to verify the hypoglycemic potential of unripe and ripe fruit extracts of Musa sapientum by using various in-vitro techniques, namely glucose adsorption capacity, glucose diffusion, amylolysis kinetics and glucose transport across the yeast cells. The results revealed that the unripe and ripe fruit extracts of Musa sapientum adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The plant extracts also promoted glucose uptake by the yeast cells and enhancement of glucose uptake was dependent on both the sample and glucose concentration. The hypoglycemic effect exhibited by the extracts was observed to be mediated by inhibiting α-amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by an in-vitro model of yeast cells

Nanoemulsion drug delivery system loaded with imiquimod: a QbD-based strategy for augmenting anti-cancer effects

Abstract Background Skin cancer is becoming a public health concern due to increased exposure to environmental pollutants and UV rays, among other factors. In India, skin neoplasms constitute 2–3% of all human cancer cases, whereas in the USA, 2–3 million cases of non-melanoma skin cancer are reported annually. Various drugs are available in the market for treating skin cancer. Imiquimod (IMQ) is one such drug approved by the USFDA for managing basal cell malignancy, external genital warts, and actinic keratosis. The conventional dosage form of IMQ cream has several side effects that can lead to therapy interruption. Therefore, the present work aims to develop an IMQ nanoemulsion with improved solubility, in vitro drug release and stability. Nanoemulsion was formulated using oleic acid/rose oil, with polysorbate 20/propylene glycol selected as the oil phase and Smix, respectively. Optimization carried out using a 32 factorial design with the aid of a quadratic model. Characterization was conducted for parameters, namely viscosity, pH, drug content, globule size, zeta potential and entrapment efficiency. Thermodynamic stability studies were conducted to assess the stability of the formulation. Furthermore, the optimized system was subjected to TEM analysis, in vitro drug release and in vitro cytotoxicity assay (MTT assay). Results Nanoemulsions were found to be in the size range of 152.80–470.13 nm and exhibited a spherical shape. Zeta potential values ranged from − 28.93 to − 58.48 mV. DSC measurements indicated the complete solubilization of IMQ in the nanoemulsion system. The optimized formulation F1 displayed the following characteristics: a globule size  − 55 mV, a polydispersity index < 0.2, % drug content of 102.89 ± 1.06, % entrapment efficiency of 97.59 ± 0.24, a pH of 4.77 ± 0.06, and a viscosity of 4.06 ± 0.06 poise. In vitro IMQ release studies of nanoemulsion and commercial cream showed approximately 70% and 34% drug release, respectively, at the end of 8 h. Moreover, the in vitro cytotoxicity assay depicted that F1 exhibited greater cytotoxic potential compared to the commercial formulation against the A431 cell line. Conclusion The present investigation showed a significant improvement in in vitro drug release of the BCS class IV drug IMQ and enhanced cytotoxic activity against cancerous cells. IMQ-loaded nanoemulsion represents a promising vehicle for delivering treatment to the skin for treating skin cancer. Graphical abstrac

Preparation of Arjunāriṣṭa- Using Microbes Isolated from Woodfordia fruticosa Flowers (Dhayati)

Objective: To verify the utility of isolated fermentative microbes from Woodfordia fruticosa flowers for preparation of Arjunāriṣṭa formulation and its comparative evaluation with the same formulation prepared by traditional method. Methodology: In the present technique, isolated colonies of microorganisms from Woodfordia fruticosa(Dhātakī) flowers on Saubroad dextrose media were separated and suspended in sterile water. This suspension was aseptically added in previously sterilized mixtures containing all intended ingredients for Arjunāriṣṭa which was thereafter incubated for 20 days at 37×C to achieve optimal fermentation. The formulation thus obtained was further subjected to various evaluation tests. Result: Arjunāriṣṭa was prepared using a new approach, and in that, isolated microorganisms from the flowers of Woodfordia fruticosa (Dhātakī) were used. It was found that the new approach was successful in generating approximately same quantities of alcohol content in comparison with traditional methods which have shown varying concentration of alcoholic content. Moreover, the new process prevents the growth of unwanted microbes thus, optimizing standards for purity and safety of the formulation. Conclusion: The formulation prepared by a new procedure showed marked uniformity for different parameters such as alcohol production, total phenol content, total solid content as compared to that prepared by the traditional method. Similarly, the results of thin layer chromatography, high performance thin layer chromatography showed marked uniformity related to quality, safety, efficacy, and reproducibility of the new method as compared to the traditional one. Thus, the modern technique was found to show reproducibility and facilitate easier quality assessment

In vitro hypoglycemic effects of unripe and ripe fruits of Musa sapientum

ABSTRACT The present study was undertaken to verify the hypoglycemic potential of unripe and ripe fruit extracts of Musa sapientum by using various in-vitro techniques, namely glucose adsorption capacity, glucose diffusion, amylolysis kinetics and glucose transport across the yeast cells. The results revealed that the unripe and ripe fruit extracts of Musa sapientum adsorbed glucose and the adsorption of glucose increased remarkably with an increase in glucose concentration. There were no significant (p≤0.05) differences between their adsorption capacities. In the amylolysis kinetic experimental model the rate of glucose diffusion was found to be increased with time from 30 to 180 min and both extracts exhibited significant inhibitory effects on the movement of glucose into external solution across the dialysis membrane as compared to control. The plant extracts also promoted glucose uptake by the yeast cells and enhancement of glucose uptake was dependent on both the sample and glucose concentration. The hypoglycemic effect exhibited by the extracts was observed to be mediated by inhibiting α-amylase, inhibiting glucose diffusion by adsorbing glucose and by increasing glucose transport across the cell membranes as revealed by an in-vitro model of yeast cells