Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs

Abstract

The ability of polyglycolyzed glycerides (PGG) with varying fatty acid and polyethylene glycol (PEG) chain lengths to produce the self-emulsification of oil in water has been investigated. The quality of the resulting emulsions depends on the oil and emulsifier pair selected. These self-emulsifying drug delivery systems (SEDDS) were prepared using various concentrations of PGG as emulsifiers. Two oils, a medium-chain triglyceride (Neobee M5) and Peanut Oil, were chosen as the vehicle for the drug. A lipophilic drug with excellent oil solubility was selected for this study. The droplet size distribution, the release rate of the drug and the oil/water partition coefficient (PC o/w) of the drug in these systems were evaluated for the SEDDS obtained. The results indicate that PGG are effective emulsifiers for SEDDS. Droplet particle size in combination with droplet polarity in the emulsion are prerequisites for efficient SEDDS. The PC o/w of the drug from these SEDDS is helpful in evaluating these properties. A phase diagram was used to obtain the optimum concentrations of drug, oil and emulsifying agent. The results obtained with PGG were compared with previously reported SEDDS for the efficiency of drug release (Bachynsky et al., (1989) AAPS Annual Meeting). In vitro dissolution and in vivo absorption of a lipophilic drug from SEDDS are compared with those properties of other dosage forms.