In the present study an attempt has been made to address low solubility issue and colonic delivery of Budesonide by developing enteric coated capsule containing Budesonide in a nano emulsifying drug delivery system. Herein, the formulated liquid SNEDDS was transformed to a solid form by spray draying method. Subsequently, it was filled into capsules coated with pH sensitive polymer, Eudragit S-100 along with band sealing. However, the drug solubility is an important parameter which was determined in different oils, surfactants and co-surfactants. Ternary phase diagrams were constructed to obtain maximum nano-emulsion area. SNEDDS containing Capmule ® MCM L8 as oil, Tween-80 as surfactant and polyethylene glycol 400 as co-surfactant were formulated to get maximum nano-emulsion in the phase diagram. In vitro drug release of the optimized SNEDDS (particle size 116.32 nm) revealed enhanced drug release in colonic pH as compared to pure drug. The developed SNEDDS of budesonide also demonstrated better activity against ulcerative colitis as evidenced by the gradually diminishing morphological damages in the histopathological studies in the TNBS induced ulcerative colitis in rats. Thus, SNEDDS enhanced the solubility of Budesonide while the enteric coating provides its colonic release.
Drug repurposing is the finding new activity of the existing drug. Recently, Albendazole’s well-known antihelmintic has got the attention of an anticancer drug. Plausible evidence of the interaction of Albendazole with one of the types of tyrosine kinase protein receptor, vascular endothelial growth factor receptor-2 (VEGFR-2) is still not well understood. Inhibition of the VEGFR-2 receptor can prevent tumor growth. The current study investigated the interaction of Albendazole with VEGFR-2.It was found that the said interaction exhibited potent binding energy ΔG = -7.12 kcal/mol, inhibitory concentration (Ki) = 6.04 μM, and as positive control comparison with standard drug (42Q1170A) showed ΔG = -12.35 kcal/mol and Ki = 881 μM. The key residue Asp1046 was formed involved hydrogen bonding with Albendazole. The molecular dynamics simulation study revealed the stable trajectory of the VEGFR-2 receptor with Albendazole bound complex having significant high free energy of binding as calculated from Molecular Mechanics Generalized Born and Surface Area study ΔG = -42.07±2.4 kcal/mol. The binding energy is significantly high for greater stability of the complex. Principal component analysis of molecular docking trajectories exhibited ordered motion at higher modes, implying a high degree of VEGFR-2 and Albendazole complex stability as seen with the standard drug 42Q. Therefore, the current work suggests the role of Albendazole as a potent angiogenesis inhibitor as ascertained by its potential interaction with VEGFR-2. The findings of research will aid in the future development of Albendazole in anticancer therapy.
The goal of this research is to provide an accurate and exact technique for estimating Albendazole and Paclitaxel simultaneously utilizing gradient RP-HPLC (high performance liquid chromatography). A UV detector fixed at 230 nm was used to estimate albendazole and paclitaxel simultaneously. As the solvent system, acetonitrile and water in the ratio of 50:50 was used in the presence of 0.1 % trifluoroacetic acid. Mobile phase was run on a Inertsil ODS 3V 150 4.6 mm or equivalent column in Gradient mode at a flow rate of 1.0 mL/min. By this method albendazole and paclitaxel showed 6.199 and 9.684 retention time (Rt) respectively with continuous run upto 25 min. In the prescribed concentration range, the calibration curves for each analyte were determined to be linear (r2 > 0.994). The percentage of recovery was found to be within the limit at each level (98.0 %to 102.0 %). All validation parameters were determined to be acceptable, including system precision, method precision, linearity, range, accuracy, ruggedness, robustness, solution, and mobile phase stability findings. This suggests that the HPLC simultaneous approach for determining albendazole and paclitaxel assays is accurate. S
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