Development and Optimization of Rizatriptan Benzoate Ethosomes

Abstract

Objective: The objective of this study was to assess the development of ethosomal drug delivery system for site-specific topical delivery of rizatriptan benzoate (RBZ) for sustained action.Methods: In the present study ethosomes were prepared using the cold method. The formulation was optimized using 33 full factorial designs. The lipid concentration (X1), ethanol concentration (X2) and stirring speed (X3) were selected as independent factors and the vesicle size (Y1) and % entrapment efficiency (Y2) were selected as dependent variables.Results: The equation of multiple regression revealed that there was no significant interaction among factors. The lipid concentration had a positive effect on vesicle size while ethanol concentration and stirring speed had a negative effect. For entrapment efficiency, all factors showed a positive effect while lipid concentrative found to be the main influencing factor. The formulation F4E459 (4% SPC, 45% v/v ethanol 900 RPM), which was characterized by optimum vesicle size (5.5 µm) and high entrapment efficiency (93.32%), was considered to be an optimal formulation. The scanning electron microscopy (SEM) results showed that RBZ ethosome have a smooth surface. The polydispersity index (PI) and zeta potential of the optimized formulation were found to be 0.493±0.021and–21.3 mV respectively. In vitro permeation through rat abdominal skin from the ethosomal gel followed Higuchi diffusion model over a period of 8 h.Conclusion: The results obtained in this research work clearly indicated a promising potential of ethosomal carrier system of RBZ for migraine treatment with a topical approach for sustained action.

Statistical Optimization and Evaluation of Ethosomal Miconazole Nitrate Suspension

“…The polymer was soaked in water for 2 h and then dispersed in distilled water using a magnetic stirrer to obtain a homogeneous gel adjusting the pH by using triethanolamine solution. For the preparation of ethosomal gel, the ethosomal suspension was centrifuged at 14000 rpm for 20 min, and the obtained suspension was incorporated into the prepared gel base [15].…”

“…The stability studies were performed at 40 °C±2 °C; samples were analyzed at periodic time intervals for 3 mo for the estimation of pH, viscosity, and drug content [15].…”

“…4A,4B,5A,5B displayed the 2D contour and the 3D response surface plot emphasized the positive impact of variable Y2. Several studies revealed that the optimized lecithin concentration, ethanol concentration, and Isopropyl alcohol concentration play a notable role in the entrapment of the drug and drug release of the dispersion system [15].…”

“…Stability study of the optimized ethosomal gel formulation was conducted at temperature 40 ͦ C±2 ͦ C for a period of 3 mo. There was an insignificant difference in all the parameters and as per the results to achieve the best stability, ethosomal suspension should be stored in a refrigerator before converting to ethosomal gel [15].…”