Stability determination of solid lipid nanoparticles (SLN) in aqueous dispersion after addition of electrolyte.
The contribution of mono-, di- and trivalent ions to the destabilization of solid lipid nanoparticle (SLN) dispersions was investigated, i.e. particle growth and subsequent formation of semi-solid gels. Sodium, calcium and aluminium chloride were added in varying concentrations to a Compritol formulation which had proved to be highly sensitive towards destabilizing effects. Dispersions containing up to 10(-3) M sodium chloride remained stable for 14 days. The same concentrations of calcium or aluminium induced slight and rapid particle growth, respectively. Generally, a pronounced destabilizing effect was observed with increasing electrolyte concentration and increasing valence. Higher concentrations of electrolyte (10(-2), 10(-1) M) induced gelation of the systems. The extent of solidification was highly dependent on the crystallinity of the lipid phase. The recrystalization indices of the gels were distinctly higher compared to the liquid systems. Additionally, unstable modifications, being present in liquid dispersions, were transformed into stable ones with increasing solidification. The mechanisms of the destabilizing effect of the electrolytes are reduced electrostatic repulsion and transformation of the lipid Compritol to the beta' modification promoting gel formation.
Freitas
C
C
Department of Pharmaceutics, Biopharmaceutics & Biotechnology, Free University of Berlin, Germany.
Müller
R H
RH
D000077410:Aluminum Chloride; D017607:Aluminum Compounds / Q000737:chemistry; D002122:Calcium Chloride / Q000737:chemistry; D002412:Cations / Q000737:chemistry; D002712:Chlorides / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D004573:Electrolytes / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry*; D005227:Fatty Acids / Q000737:chemistry*; D005782:Gels; D008055:Lipids / Q000737:chemistry*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry*; D012965:Sodium Chloride / Q000737:chemistry; D013696:Temperature