Lym-X-Sorb®: Drug Delivery, Fenretinide & Cyclosporine:
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.
- 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:
|Pharmacokinetics Parameters:||65mg Drug/Lym-X-Sorb®:||300mg Drug/Corn oil/surf:||Ratio (Lym-X-Sorb®/Oil):|
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.