Design and Evaluation of Self-Nanoemulsifying Pellets of Repaglinide

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 cos...

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Bibliographic Details
Published in:AAPS PharmSciTech 2013-09, Vol.14 (3), p.994-1003
Main Authors: Desai, N. S., Nagarsenker, M. S.
Format: Article
Language:English
Subjects:
Animals
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Carbamates - chemistry
Carbamates - pharmacology
Cellulose
Chromatography, High Pressure Liquid
Drug Design
Emulsions
Hydrogen-Ion Concentration
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacology
Microscopy, Electron, Scanning
Nanostructures
Pharmacology/Toxicology
Pharmacy
Piperidines - chemistry
Piperidines - pharmacology
Powder Diffraction
Rats
Research Article
Solubility
Surface-Active Agents - chemistry
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Summary: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.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-013-9990-9