Effect of Formulation Components on the In Vitro Permeation of Microemulsion Drug Delivery System of Fluconazole

Abstract

Abstract. The purpose of this study was to evaluate the effect of formulation components on the in vitro skin permeation of microemulsion drug delivery system containing fluconazole (FLZ). Lauryl alcohol (LA) was screened as the oil phase of microemulsions. The pseudo-ternary phase diagrams for microemulsion regions were constructed using LA as the oil, Labrasol (Lab) as the surfactant and ethanol (EtOH) as the cosurfactant. The formulation which showed a highest permeation rate of 47.15± 1.12 µg cm −2 h −1 and appropriate physicochemical properties was optimized as containing 2% FLZ, 10%LA, 20% Lab/EtOH (1:1), and 68% double-distilled water (w/w). The efficiency of microemulsion formulation in the topical delivery of FLZ was dependent upon the contents of water and LA as well as Lab/EtOH mixing ratio. It was concluded that the percutaneous absorption of FLZ from microemulsions was enhanced with increasing the LA and water contents, and with decreasing the Lab/EtOH ratio in the formulation. Candida albicans was used as a model fungus to evaluate the antifungal activity of the best formula achieved, which showed the widest zone of inhibition as compared to FLZ reference. The studied microemulsion formulation showed a good stability for a period of 3 months. These results indicate that the studied microemulsion formulation might be a promising vehicle for topical delivery of FLZ.

Preparation and in vitro/ex vivo evaluation of nanoemulsion for transnasal delivery of paliperidone

“…Water was added dropwise to each oilEmix mixture under vigorous stirring. After equilibrium, the samples were visually checked and determined as being clear/transparent (Elshafeey et al 2009;Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a.…”

“…The globule size was calculated using Stokes-Einstein relationship by Zetasizer Software. Electrophoretic mobility (lm/s) was measured using small volume disposable zeta cell and converted to zeta potential by in-built software using Helmholtz-Smoluchowski equation (Elshafeey et al 2009;Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a.…”

“…Further, prepared nanoemulsion formulations were characterized by the measurement of pH, conductivity, percentage transmittance, and refractive index (Patel et al 2009). …”

“…Different evaluation parameters such as % drug diffused, flux, diffusion co-efficient and enhancement ratio (E r = -PALI flux at steady state (Jss) of NE formulation/Jss of control vehicle) were derived. The permeation kinetic of PALI from each formulation was evaluated by fitting different kinetic models (Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a.…”

“…Three sheep nasal mucosa pieces (P1, P2, P3) with uniform thickness were selected and mounted on Franz diffusion cells. P1 was treated with 0.5 mL of PBS (pH 6.4, negative control), P2 with 0.5 mL of isopropyl alcohol (positive control), and P3 was treated with PMNE6 for 1 h. After 1 h, the mucosa were rinsed with PBS (pH 6.4) and subjected to histological studies and photographed by microscope (Polarizing Microscope RPL-55 Series, Radical Instruments, India) (Jogani et al 2008;Kumar et al 2008;Patel et al 2009Patel et al , 2013a. Each formulation contains paliperidone 5 mg/mL a PNE4, PNE5 and PNE 6 formulations additionally contain 0.5 %wt/wt of polycarbophil as mucoadhesive agent, and further referred as PMNE4, PMNE5 and PMNE6 respectively Appl Nanosci (2016) 6:1095-1104 1097…”