Lym-X-Sorb®: Drug Delivery, Fenretinide & Cyclosporine:


Lym-X-Sorb monomer complexed (in a conceptual model) with a molar equivalent of fenretinide, in yellow.Lym-X-Sorb® monomer complexed (in a conceptual model) with a molar equivalent of fenretinide, in yellow.

Lym-X-Sorb® solubility and stability:
  • Drug is soluble in Lym-X-Sorb® at 1:1 molar ratio.
  • Drug in excess of 1:1 molar ratio remains as a solid.
  • Lym-X-Sorb®/drug formulations are stable at 40°C for 6 months.
  • Drug remains a suspension in corn oil/surfactant formulation.
Oral Bioavailability of Fenretinide:
  • Drug in ethanol (soluble): <1% absorption in fed dogs
  • Drug in corn oil/surfactant (suspension): Estimate 12-15% absorption in fed dogs or in humans who received a high fat meal.
Lym-X-Sorb®/drug (soluble):
  • 70% in fasting dogs
  • 90% in fed dogs
  • 80-90% in humans who received the same high fat diet as above.
Humans: Comparative Bioavailability of Fenretinamide:

Graph that demonstrates the bioavailability of Fenretinamide with Lym-X-Sorb

Pharmacokinetics Parameters: 65mg Drug/Lym-X-Sorb®: 300mg Drug/Corn oil/surf: Ratio (Lym-X-Sorb®/Oil):

CMAX (ng/mL) 715 806 4.1
TMAX (hours) 4.9 5.0
AUC ( 5421 7413 3.4

CMAX (ng/mL) 258 309 3.8
TMAX (hours) 6.3 6.1
AUC ( 4389 6011 3.4


Cyclosporine encapsulated in Lym-X-Sorb® was compared to the current delivery formulations of cyclosporine and administered orally to dogs. The area under the curve showed a 4-5 fold increased absorption of cyclosporine in Lym-X-Sorb® formulation when compared to the commercial formulation. The delayed appearance of drug in plasma for Lym-X-Sorb® formulation indicates that cyclosporine partitions with the chylomicrons into the lymphatic system.

Exclusion Chromatography and Oral Bioavailability of Cyclosporin Graph

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