Abstract
Purpose : To improve the oral bioavailability of berberine using a new self-nanoemulsifying drug delivery system (SNEDDS). Methods : Berberine SNEDDS was designed using solubility studies and phase diagram construction. A series of tests were carried out to study the effect of oil content, dilution, and drug loading on particle size. The morphology of the nanoemulsion was examined with a transmission electron microscope. Subsequently, the optimized berberine SNEDDS was investigated for in vitro release and compared with two marketed products (Xiaowei capsules and Beike tablets) Results : The optimized formulation, composed of berberine of 6.0 %, castor oil of 18.8 %, Tween 20 of 37.6 %, and glycerol of 37.6 %, gave a mean particle size of approximately 60 nm, and was not affected by dilution. The optimized formulation released 90 % berberine in 20 min, while the reference products, Xiaowei capsules and Beike tablets, required 2 h to release 90 % of berberine. Conclusion : The optimized formulation of SNEDDS is a potential alternative oral dosage form for improving oral absorption of berberine. Keywords : Berberine, Pseudoternary phase diagram, Self-nanoemulsifying, SNEDDS, Drug release
Highlights
Self-nanoemulsifying drug delivery systems (SNEDDS) are isotropic and thermodynamically stable solutions consisting of oil, surfactant, cosurfactant and drug that can self-emulsify quickly in the stomach aqueous contents
SNEDDS were diluted with aqueous medium (1:50) and centrifuged at 4,000 rpm for 30 min and formulation were observed visually for phase separation and drug precipitation
Enhancement of bioavailability of berberine SNEDDS compared with Beike tablets and Xiaowei capsules may be due to effects of the large quantities of surfactant and cosurfactant used which include improved mucosal permeability, smaller lipid droplets and greater surface area
Summary
Self-nanoemulsifying drug delivery systems (SNEDDS) are isotropic and thermodynamically stable solutions consisting of oil, surfactant, cosurfactant and drug that can self-emulsify quickly in the stomach aqueous contents. It introduces the drug in solution within nanosized oil droplets [1,2,3]. Berberine is one of the major components of Coptis chinensis Franch. It has been clinically applied for decades because of its significant effect. The current commercially marketed dosage forms are tablets and capsules Both of these exhibit low and erratic oral bioavailability, which is mainly due to the poor dissolution of the drug
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