NMR relaxometric investigations of solid lipid nanoparticles (SLN) containing gadolinium(III) complexes.
This work deals with the preparation and relaxometric investigations of solid lipid nanoparticles (SLN) containing [Gd-DTPA(H2O)]2- and [Gd-DOTA(H2O)]-. These paramagnetic chelates are commonly used as contrast agents (CA) for magnetic resonance imaging (MRI) owing to their ability to strongly increase the tissue water proton relaxation rate. The amount of gadolinium(III) (Gd(III)) complex included in the SLN has been evaluated and, on this basis, it has been found that the longitudinal relaxivity of these Gd(III) chelates apparently does not vary, at physiological pH, following their inclusion in SLN. We are unable to establish whether this is due to the free exchange of water from the inner compartment containing the Gd(III) chelate to the bulk water or whether the observed relaxation rate is essentially determined by a fraction of the complex which is close to the surface of the SLN in a region easily accessible to the bulk water. At acidic pH values, the relaxivity of the paramagnetic SLN containing the less thermodynamically and kinetically stable [Gd-DTPA(H2O)]2- markedly increases. This effect may be ascribed to an increased immobilization and/or to an enhanced hydration of the complex on SLN.
Dipartimento di Scienza e Tecnologia del Farmaco, Torino, Italy.
S
S
Morel
E
E
Terreno
E
E
Ugazio
S
S
Aime
M R
MR
Gasco
D003287:Contrast Media / Q000737:chemistry*; D004337:Drug Carriers; D004655:Emulsions / Q000737:chemistry; D005682:Gadolinium / Q000737:chemistry*; D019786:Gadolinium DTPA / Q000737:chemistry; D006571:Heterocyclic Compounds / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008863:Microspheres; D009942:Organometallic Compounds / Q000737:chemistry
D003287:Contrast Media; D004337:Drug Carriers; D004655:Emulsions; D006571:Heterocyclic Compounds; D008055:Lipids; D009942:Organometallic Compounds; C050823:gadolinium 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetate; D005682:Gadolinium; D019786:Gadolinium DTPA