title: Nanoemulsion: for improved oral delivery of repaglinide.
abstract: Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic β-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% w/w of oil from the o/w nanoemulsion region of phase diagrams. The optimized nanoemulsion formulation constituted sefsol-218 (5% v/v) as an oil phase, 30% v/v of Tween-80 and transcutol as a surfactant and co-surfactant to restrain nanodroplet size and low viscosity and distilled water (65%). In vitro dissolution studies showed higher drug release (98.22%), finest droplet size (76.23 nm), slightest polydispersity value (0.183), least viscosity (21.45 cps) and immeasurable dilution capability from the nanoemulsion as compared with existing oral tablet formulation. The optimized RPG nanoemulsion formulation showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats. No significant variations were also observed in the optimized formulation when subjected to accelerated stability study at different temperature and relative humidity over a period of 3 months.
authors.affiliation: a Department of Pharmacy , Integral University , Lucknow , India .
authors.forename: Juber
authors.initials: J
authors.lastname: Akhtar
authors.affiliation: a Department of Pharmacy , Integral University , Lucknow , India .
authors.forename: Hefazat Hussain
authors.initials: HH
authors.lastname: Siddiqui
authors.affiliation: b Department of Pharmacy , Women Center for Higher Education , Abha , Saudi Arabia , and.
authors.forename: Sheeba
authors.initials: S
authors.lastname: Fareed
authors.affiliation: a Department of Pharmacy , Integral University , Lucknow , India .
authors.lastname: Badruddeen
authors.affiliation: a Department of Pharmacy , Integral University , Lucknow , India .
authors.forename: Mohammad
authors.initials: M
authors.lastname: Khalid
authors.affiliation: c Faculty of Pharmacy , Jamia Hamdard , New Delhi , India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aqil
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001702:Biopharmaceutics; D002219:Carbamates / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy* / Q000378:metabolism; D004355:Drug Stability; D004655:Emulsions / Q000737:chemistry* / Q000493:pharmacokinetics; D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000378:metabolism; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010880:Piperidines / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics*; D011136:Polysorbates / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D012995:Solubility
chemical_list: D002219:Carbamates; D004655:Emulsions; D007004:Hypoglycemic Agents; D008055:Lipids; D010880:Piperidines; D011136:Polysorbates; C072379:repaglinide
keywords: Diabetes mellitus; nanoemulsion; pseudoternary phase diagrams; repaglinide; streptozotocin