Oral bioavailability of cyclosporine: Solid lipid nanoparticles (SLN®) versus drug nanocrystals

For the development of an optimized oral formulation for cyclosporine A, 2% of this drug has been formulated in solid lipid nanoparticles and as nanocrystals

R.H. Müller

2006

Scholarcy highlights

  • For the development of an optimized oral formulation for cyclosporine A, 2% of this drug has been formulated in solid lipid nanoparticles and as nanocrystals
  • For the assessment of the pharmacokinetic parameters the developed formulations have been administered via oral route to three young pigs
  • Comparison studies with a commercial Sandimmun Neoral/Optoral® used as reference have been performed
  • The blood profiles observed after oral administration of the commercial microemulsion Sandimmun® revealed a fast absorption of drug leading to the observation of a plasma peak above 1000 ng/ml within the first 2 h
  • For drug nanocrystals most of the blood concentrations were in the range between 30 and 70 ng/ml over a period of 14 h
  • In this study it has been proved that using SLN™ as a drug carrier for oral administration of cyclosporine A a low variation in bioavailability of the drug and simultaneously avoiding the plasma peak typical of the first Sandimmun® formulation can be achieved

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