Syrupy herbal formulation of green bean pod extract of Phaseolus vulgaris L.: Formulation optimization by central composite design, and evaluation for anti-urolithiatic activity.

The green bean pods of Phaseolus vulgaris L. are traditionally used as a folk remedy for treating calcium oxalate kidney stones. The current research aimed to develop a syrup formulation containing green bean pod extract for anti-urolithiatic activity. The syrup was prepared using a simple blending method and optimized through a central composite design (CCD) with two independent variables: the ratio of pod juice (PJ) to sugar solution (SS) ranging from 1:0.5 to 1:1.5, and the percentage of CMC from 0.2% to 0.4% w/v. These variables were analyzed for their impact on viscosity (CP) and sedimentation percentage, helping to identify the best formulation out of 13 variants. The finalized formulation (F-opt) underwent assessment for physicochemical characteristics such as organoleptic properties, viscosity, density, sedimentation rate, and stability. Additionally, a microbiological assessment was performed utilizing the spread plate method. Further, it was evaluated for in vitro, ex vivo, and in vivo anti-urolithiatic activity in rat models for 28 days and compared with that of the reference standard (Cystone syrup). Additionally, acute toxicity was assessed in albino Swiss mice. Histopathological evaluations were then conducted on the kidneys of the Wistar rats that had been used for the in vivo studies, providing insight into the treatment effects on kidney tissue structure. The optimized formulation (F-opt) was a green, viscous, clear syrup with a pH of 5.8, a viscosity of 256.38 CP, a density of 1.31 g/ml, and a sedimentation rate of 0.69%. The optimized formulation was found to be stable, showing no significant changes in physicochemical and microbiological properties. The results of the in vitro, ex vivo, and in vivo anti-urolithiatic studies indicated that the optimized formulation effectively inhibited the aggregation of calcium oxalate. The acute toxicity studies revealed no mortality or adverse effects for both the optimized formulation and pure bean pod juice at a dose of 2000 mg/kg body weight. Histopathological examination revealed that rats treated with the optimized formulation exhibited a significant reduction in both the number and size of calcium oxalate deposits within various parts of the renal tubules. It can be concluded that the syrupy formulation of Phaseolus vulgaris L. green bean pod extract demonstrated significant anti-urolithiatic activity. This activity could be due to its diuretic properties and its ability to inhibit the formation of calcium oxalate crystals. However, limitations of the study included a lack of elucidation of the mechanism and limited generalizability of the findings.

Glyceryl behenate-based solid lipid nanoparticles as a carrier of haloperidol for nose to brain delivery: formulation development, in-vitro, and in-vivo evaluation

Abstract This study was aimed to develop the haloperidol (HPL) loaded solid lipid nanoparticles (SLNs) for brain targeting through the intranasal route. SLNs were fabricated by the emulsification diffusion technique using glyceryl behenate as lipid and tween 80 as a surfactant. SLNs were evaluated for particle size, zeta potential, structure, entrapment efficiency, solid state characterization by differential scanning calorimetry (DSC), and in-vitro release. In-vivo biological evaluation was performed on albino Wistar rats for the determination of pharmacokinetic as well as brain targeting parameters. Particle size, PDI, zeta potential, and entrapment efficiency of optimized formulation (HPL-SLNs 6) were found to be 103±09 nm, 0.190±0.029, -23.5±1.07 mV, and 79.46±1.97% respectively. In-vitro drug release studies exhibited that 87.21± 3.63% of the entrapped drug was released from the SLNs within 24 h. DSC curves confirmed that during entrapment in SLNs, the drug was solubilized in the lipid matrix and converted into the amorphous form. Enhanced HPL targeting to the brain was observed from HPL-SLNs as compared to HPL-Sol when administered intranasally. The value of AUC 0-∞ in the brain for HPL-SLNs i.n. was found to be nearly 2.7 times higher than that of HPL-Sol i.v., whereas 3.66 times superior to HPL-Sol administered i.n. Stability studies revealed that the formulation remains unchanged when stored at 4±2 °C (refrigerator) and 25±2 °C /60 ±5% RH up to six months. Finally, it could be concluded that SLN is a suitable carrier for HPL with enhanced brain targeting through i.n administration, as compared to the HPL-Sol, administered i.n. and i.v.

InCl3 mediated one-pot multicomponent synthesis, anti-microbial, antioxidant and anticancer evaluation of 3-pyranyl indole derivatives.

A simple and convenient method for the one-pot three-component synthesis of 3-pyranyl indoles has been accomplished by tandem Knoevenagel-Michael reaction of 3-cyanoacetyl indole, various aromatic aldehydes and malononitrile catalyzed by InCl(3) in ethanol under reflux conditions. The newly synthesized 3-pyranyl indoles were evaluated for anti-microbial, antioxidant, and anticancer activities. Some of the compounds showed good anticancer activity against MCF-7 breast cancer cell lines on comparison with of standard drug.