Abstract
The purpose of present study was aimed at developing self emulsifying drug delivery system in liquid and then in pellet form that would result in improved solubility, dissolution and permeability of the poorly water soluble drug carvedilol. Pellets were prepared using extrusion-spheronization technique incorporating liquid SEDDS (carvedilol, capmul MCM EP, cremophore EL, tween 20, propylene glycol), adsorbents ( and crospovidone), microcrystalline cellulose and binder (povidone K-30). Ternary phase diagram was constructed to identify different oil-surfactant-cosurfactant mixtures according to the proportion of each point in it. The optimal CAR-SEDDS pellets showed a quicker redispersion with a droplet size of the reconstituted microemulsion being 160.47 nm, which was almost unchanged after solidification. SEM analysis confirmed good spherical appearance of solid pellets; DSC and XRD analysis confirmed that there was no crystalline carvedilol in the pellets. Pellets were then capable of transferring lipophilic compounds into the aqueous phase and significantly enhancing its release with respect to pure drug.
Highlights
In recent years, an increasing number of new chemical entities and many already existing drugs show low aqueous solubility, which are prone to poor oral absorption, high intra-inter-subject variability and lack of dose availability
Self-emulsifying drug delivery system (SEDDS) is among the methods used to improve the oral bioavailability of poorly soluble drugs by presenting and maintaining the drug in a dissolved state, in small droplets of oil, all over its transit through the gastrointestinal tract (GIT)
We developed a novel CAR-loaded solubility of drugsSelf-emulsifying drug delivery system (SEDDS) pellets using extrusion-spheronization technique
Summary
An increasing number of new chemical entities and many already existing drugs show low aqueous solubility, which are prone to poor oral absorption, high intra-inter-subject variability and lack of dose availability. Self-emulsifying drug delivery system (SEDDS) is among the methods used to improve the oral bioavailability of poorly soluble drugs by presenting and maintaining the drug in a dissolved state, in small droplets of oil, all over its transit through the gastrointestinal tract (GIT). SEDDS are present in the liquid state, which can be packed in hard or soft gelatin capsule directly but suffer from the drawbacks related to stability and compatibility. Incorporation of liquid SEDDS into solid dosage form is compatible and desirable where spray drying, self emulsifying granules, tablet or pellets can be a preferred and viable option (Iosio et al, 2008)
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