title: Design and evaluation of self-nanoemulsifying pellets of repaglinide.
abstract: The aim of study was to develop self-nanoemulsifying pellets (SNEP) for oral delivery of poorly water soluble drug, repaglinide (RPG). Solubility of RPG in oily phases and surfactants was determined to identify components of self-nanoemulsifying drug delivery system (SNEDDS). The surfactants and cosurfactants were screened for their ability to emulsify oily phase. Ternary phase diagrams were constructed to identify nanoemulsification area for the selected systems. SNEDDS formulations with globule size less than 100 nm were evaluated for in vivo anti-hyperglycemic activity in neonatal streptozotocin rat model. A significant reduction in glucose levels was produced by optimized SNEDDS formulation in comparison to the control group. The optimized SNEDDS formulations were pelletized via extrusion/spheronization technique using microcrystalline cellulose and lactose. SNEP were characterized by X-ray powder diffraction and scanning electron microscopy. X-ray diffraction study indicated loss of crystallinity of RPG in SNEP. The SNEP exhibited good flow properties, mechanical strength and formed nanoemulsion with globule size less than 200 nm. SNEP showed in vitro release of more than 80% RPG in 10 min which was significantly higher than RPG containing reference pellets. In conclusion, our studies illustrated that RPG, a poorly water soluble drug can be successfully formulated into SNEP which can serve as a promising system for the delivery of poorly water soluble drugs.
authors.affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (E), Mumbai, 400098, India.
authors.forename: N S
authors.initials: NS
authors.lastname: Desai
authors.forename: M S
authors.initials: MS
authors.lastname: Nagarsenker
mesh_terms: D000818:Animals; D002219:Carbamates / Q000737:chemistry* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D004655:Emulsions; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology; D008855:Microscopy, Electron, Scanning; D049329:Nanostructures; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology; D033362:Powder Diffraction; D051381:Rats; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry
chemical_list: D002219:Carbamates; D004655:Emulsions; D007004:Hypoglycemic Agents; D010880:Piperidines; D013501:Surface-Active Agents; C072379:repaglinide