Stability and CMC determinations of amphiphilic (DSPE-PEG(3400)-CTT2) peptide constructs by microtensiometry Journal Article


Authors: Haikola, M.; Hirvonen, J.; Penate-Medina, O.; Simpura, I.; Kairemo, K.; Peltonen, L.
Article Title: Stability and CMC determinations of amphiphilic (DSPE-PEG(3400)-CTT2) peptide constructs by microtensiometry
Abstract: Controlled formation and stability of micelles and micellar properties are crucial in ensuring pharmaceutical and physiological efficiency of drug targeting/delivering constructs. In this study, the formulative properties of a polymeric, micelle forming, pegylated cancer targeting peptide, DSPE-PEG(3400)-CTT2, were determined in a 96-well plate. A microtensiometer was used to determine the critical micelle concentration (CMC) and micelle formation of the peptide derivative in different aqueous solutions. Particle size and size distribution were measured by dynamic light scattering. The CMC values of DSPE-PEG(3400)-CTT2 were at micrograms in milliliter level. The media exerted clear effects on the CMC values and formation of micelles. Partitioning coefficient, Kaw, values in the acidic media were higher than in pure water, which means that the micellar associates are formed at a lower concentration in an acidic environment. The areas per molecule were also dependent on the medium. Micellar sizes were 18-22 nm in all the media. Accordingly, stability of micellar formulations is highly dependent on the environmental factors.
Keywords: unclassified drug; protein targeting; phosphatidylethanolamine; concentration (parameters); macrogol; particle size; light scattering; critical micelle concentration; dspe-peg derivative; microtensiometry; peptide targeting; surface tension; 1,2 distearoylglycero 3 phosphoethanolamine; 1,2 distearoylglycero 3 phosphoethanolamine polyethylene glycol 3400 cycloglycylarginylglutamylasparaginyltyrosylhistidylglycylcysteinylthreonylthreo nylhistidyltryptophylglycylphenylalanylthreonylleucylcysteinamide; amphophile; glycerophospholipid; glycylarginylglutamylasparaginyltyrosylhistidylglycylcysteinylthreonylthreonylhi stidyltryptophylglycylphenylalanylthreonylleucylcysteinamide; macrogol 3400; micelle; partition coefficient
Journal Title: Journal of Drug Delivery Science and Technology
Volume: 21
Issue: 2
ISSN: 1773-2247
Publisher: Association de pharmacie galénique industrielle  
Date Published: 2011-03-01
Start Page: 183
End Page: 188
Language: English
PROVIDER: scopus
DOI/URL:
Notes: --- - "Export Date: 23 June 2011" - "CODEN: JDDSA" - "Source: Scopus"