Article ID Journal Published Year Pages File Type
2486428 Journal of Pharmaceutical Sciences 2011 9 Pages PDF
Abstract
The aims of this study were to prepare fine pidotimod-containing water-in-oil-in-water (W/O/W) double emulsions and to investigate the possibility of those emulsions as a delivery system for promoting the oral bioavailability of pidotimod. A modified two-step emulsification procedure was applied to prepare the double emulsions using medium-chain triglyceride as the oil phase, Tween 80 as the hydrophilic emulsifier, and Span 80 alone or in combination with different amount of phospholipids as the lipophilic emulsifiers. A fine W/O/W emulsion, with the encapsulation efficiency of 82 ± 3.4%, mean oil-droplet diameter of 3.93 ± 0.25 μm, and viscosity of 36.4 ± 0.93 mPa·s at 25°C and 300 s−1, was stable for 1 month at 4°C. In addition, the oral bioavailability of pidotimod in rats, after intragastric administration of W/O/W double emulsions, was significantly higher than that of pidotimod control solution. Moreover, the maximum uptake time was significantly prolonged, suggesting an extra absorption pathway for W/O/W emulsions: a lymphatic circulation pathway. Those results demonstrated that W/O/W emulsions could become a potential formulation for improving the oral bioavailability of poorly absorbable drugs and suggested an important technology platform for the oral administration of peptide and peptidomimetic drugs.
Related Topics
Health Sciences Pharmacology, Toxicology and Pharmaceutical Science Drug Discovery
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