title: Microemulsions containing lecithin and sugar-based surfactants: nanoparticle templates for delivery of proteins and peptides.
abstract: Two pseudo-ternary systems comprising isopropyl myristate, soybean lecithin, water, ethanol and either decyl glucoside (DG) or capryl-caprylyl glucoside (CCG) as surfactant were investigated for their potential to form microemulsion templates to produce nanoparticles as drug delivery vehicles for proteins and peptides. All microemulsion and nanoparticle compounds used were pharmaceutically acceptable and biocompatible. Phase diagrams were established and characterized using polarizing light microscopy, viscosity, conductivity, electron microscopy, differential scanning calorimetry and self-diffusion NMR. An area in the phase diagrams containing optically isotropic, monophasic systems was designated as the microemulsion region and systems therein identified as solution-type microemulsions. Poly(alkylcyanoacrylate) nanoparticles prepared by interfacial polymerisation from selected microemulsions ranged from 145 to 660nm in size with a unimodal size distribution depending on the type of monomer (ethyl (2) or butyl (2) cyanoacrylate) and microemulsion template. Generally larger nanoparticles were formed by butyl (2) cyanoacrylate. Insulin was added as a model protein and did not alter the physicochemical behaviour of the microemulsions or the morphology of the nanoparticles. However, insulin-loaded nanoparticles in the CCG containing system decreased in size when using butyl (2) cyanoacrylate. This study shows that microemulsions containing sugar-based surfactants are suitable formulation templates for the formation of nanoparticles to deliver peptides.
authors.affiliation: School of Pharmacy, University of Otago, Dunedin, New Zealand. anja.graf@stonebow.otago.ac.nz
authors.forename: Anja
authors.initials: A
authors.lastname: Graf
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Ablinger
authors.forename: Silvia
authors.initials: S
authors.lastname: Peters
authors.forename: Andreas
authors.initials: A
authors.lastname: Zimmer
authors.forename: Sarah
authors.initials: S
authors.lastname: Hook
authors.forename: Thomas
authors.initials: T
authors.lastname: Rades
mesh_terms: D002152:Calorimetry, Differential Scanning; D004553:Electric Conductivity; D004655:Emulsions; D007328:Insulin / Q000008:administration & dosage / Q000737:chemistry; D054709:Lecithins / Q000008:administration & dosage*; D009682:Magnetic Resonance Spectroscopy; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010455:Peptides / Q000008:administration & dosage*; D011506:Proteins / Q000008:administration & dosage*; D013501:Surface-Active Agents / Q000008:administration & dosage*; D014783:Viscosity
chemical_list: D004655:Emulsions; D007328:Insulin; D054709:Lecithins; D010455:Peptides; D011506:Proteins; D013501:Surface-Active Agents