Novel delivery systems for coagulation proteins

Haemophilia. 1998 Jul;4(4):436-42. doi: 10.1046/j.1365-2516.1998.440436.x.

Abstract

Long-term haemophilia prophylaxis with clotting factors administered by alternative delivery modes requires stable liquid formulations of these factors. We developed an aqueous-formulated human coagulation factor IX (hCFIX) with in vitro half-life (T 1/2) of 6 weeks at 37 degrees C and 18 months at 4 degrees C. Upon bolus subcutaneous (s.c.) injection in animals, hCFIX had a bioavailability of up to 16% compared to intravenous (i.v.) dose. When delivered by s.c. implanted pumps, hCFIX attained > 2% of normal human levels in the animal plasma. Hydrogels of hCFIX in a chitosan derivative, N,O-carboxymethyl chitosan (NOCC), released hCFIX slowly in vitro, and when injected s.c., gave prolonged plasma levels over those obtained by bolus i.v. or s.c. injection. Freeze-dried human coagulation factor VIII (hCFVIII) formulated in non-aqueous solvents had in vitro T 1/2 up to 80 days at 37 degrees C.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Drug Delivery Systems*
  • Factor IX / administration & dosage*
  • Factor IX / pharmacokinetics
  • Factor IX / therapeutic use
  • Half-Life
  • Hemophilia A / drug therapy*
  • Humans
  • Hydrogels
  • Injections, Intravenous
  • Rabbits

Substances

  • Hydrogels
  • Factor IX