Abstract
Self-emulsifying drug delivery system is an isotropic mixture of natural or synthetic oils, non-ionic surfactants or, one or more hydrophilic solvent and co-solvents/surfactant and polymer that improve bioavailability and increase solubility of poorly-soluble drugs. This study was aimed to prepare and develop a stable formulation for self-emulsifying drug delivery system to enhance the solubility, release rate, and oral absorption of the poorly-soluble drug, carvedilol. The prepared self-emulsifying drug delivery system formulations were evaluated regarding their particle size, refractory index (RI), emulsifying efficiency, drug release, and rat intestine permeability. The results showed oleic acid as oil with Labrafil as surfactant and Labrafac PG (propylene glycol dicaprylocapraye) as co-surfactant with hydroxypropyl methylcellulose and Poloxamer as polymer prepared stable emulsions with a refractive index higher than acidic medium and water. The particle size of formulations was influenced by the type of polymer so that the mean particle size in the self-emulsifying drug delivery system formulations containing hydroxypropyl methylcellulose have a higher particle size compared to Poloxamer formulations. The percentage of drug release after 24 hours (R24) for Poloxamer and hydroxypropyl methylcellulose formulations were 61.24-70.61% and to 74.26-91.11%, respectively. The correlation between percentages of drug released after 24 hours with type of polymer was significant. In permeation studies, a significant and direct correlation existed between P4 and surfactant/co-surfactant ratio. The self-emulsifying drug delivery system formulations showed drug permeability through the rat intestine 2.76 times more, compared with the control. This study demonstrated that physicochemical properties, in vitro release and rat intestine permeability were dependent upon the contents of S/C, water and oil percentage in formulations.
Highlights
Self-emulsifying drug delivery system is an isotropic mixture of natural or synthetic oils, non-ionic surfactants or, one or more hydrophilic solvent and co-solvents/surfactant and polymer that improve bioavailability and increase solubility of poorly-soluble drugs
Oleic acid and Span 20 were obtained from Merck (Germany) Inc.; hydroxypropyl methylcellulose (HPMC) and Poloxamer were obtained from Sigma-Aldrich Corporation
The particle size of formulations was influenced by the type of polymer so that the mean particle size in self-emulsifying drug delivery systems (SEDDS) formulations prepared with HPMC had higher particle size
Summary
Self-emulsifying drug delivery system is an isotropic mixture of natural or synthetic oils, non-ionic surfactants or, one or more hydrophilic solvent and co-solvents/surfactant and polymer that improve bioavailability and increase solubility of poorly-soluble drugs. Objectives: This study was aimed to prepare and develop a stable formulation for self-emulsifying drug delivery system to enhance the solubility, release rate, and oral absorption of the poorly-soluble drug, carvedilol. SEDDS is one type of LBF that is defined as isotropic mixtures of natural or synthetic oils non-ionic surfactants or one or more hydrophilic solvent and co-solvents/surfactant These formulations are having the droplet size in the range of 200 nm-5 μm and the dispersion has a turbid appearance [1].
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