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.

Highlights

  • 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

  • The drug is dissolved in a mixture of oil, surfactant and co-solvent which forms oil-in-water (o/w) micro- or nano-emulsion with the gastrointestinal aqueous fluids after oral administration under gentle agitation by the digestive s­ ystem[4,5,6,7]

  • The highest solubility of FUR was in Castor oil (1.23 ± 0.045 mg/g) and Oleic acid (1.1 ± 0.057 mg/g) as oily phase, and in Cremophor EL (47.62 ± 2.227 mg/g) and Polyethylene glycol 400 (PEG 400) (158.48 ± 6.379 mg/g) as surfactant and co-solvent, respectively

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Summary

Introduction

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. The theoretical model was used to calculate the amounts of the carrier (Avicel PH101) and coating materials (Aerosil 200) to prepare liquisolid powder. 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. Self-emulsifying drug delivery systems (SEDDS) present a useful mean to enhance both solubility and permeability of both class II and IV d­ rugs[2,3]. The preparation of tablets is highly beneficial since hard capsules may only be filled up to about 400 mg due to the low bulk density of the carriers used (e.g. silicates)[21]

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