Formulation and in vitro evaluation of self-nanoemulsifying liquisolid tablets of furosemide

Abstract

Self-nanoemulsifying drug delivery systems (SNEDDS) were used to enhance the dissolution rate of furosemide as a model for class IV drugs and the system was solidified into liquisolid tablets. SNEDDS of furosemide contained 10% Castor oil, 60% Cremophor EL, and 30% PEG 400. The mean droplets size was 17.9 ± 4.5 nm. The theoretical model was used to calculate the amounts of the carrier (Avicel PH101) and coating materials (Aerosil 200) to prepare liquisolid powder. Carrier/coating materials ratio of 5/1 was used and Ludipress was added to the solid system, thus tablets with hardness of 45 ± 2 N were obtained. Liquisolid tablets showed 2-folds increase in drug release as compared to the generic tablets after 60 min in HCl 0.1 N using USP apparatus-II. Furosemide loaded SNEDDS tablets have great prospects for further in vivo studies, and the theoretical model is useful for calculating the adequate amounts of adsorbents required to solidify these systems.

Figure 1

Schematic representation of the formulation of hybrid LS powder.

Figure 2

Pseudo-ternary phase diagrams of Cremophor El /PEG400:Castor oil:water with different Cremophor El/PEG400 ratios: (A)1:1, (B)2:1 and (C)1:2. (X) Represents the concentrations at which a clear/translucent emulsion was formed. (diamond) Gel-like phase. (triangle) White emulsion.

Figure 3

Angle of slide for admixtures of Avicel PH101 and Aerosil 200 SNEDDS as the liquid vehicle in different ratios.

Figure 4

DSC thermograms of: (A) LS powder, (B) Aerosil 200, (C) Avicel PH101, (D) FUR.

Figure 5

XRD patterns of (A) LS powder, (B) Aerosil 200, (C) Avicel PH101, (D) FUR.

Figure 6

SEM images of (A) Aerosil 200, 1000x. (B) Avicel PH101, 1000x. (C) LS powder, 1000x, (D) LS powder, 2000x.

Figure 7

Percentage drug release of FUR from various tablets against time (min) in different mediums. Data are expressed as mean ± SD (n = 3).