Lym-X-Sorb®: Drug Delivery:
Fenretinide & Cyclosporine
- Compatible with a large number of diverse drug structures, especially water insoluble drugs.
- Binds one mole of drug per Lym-X-Sorb® monomeric structure.
- Stable in the hostile environs of the stomach and upper intestine.
- Greatly (300-500%) improves oral drug bioavailability, i.e., from 10-20% absorption to 60-90% absorption.
- Readily absorbed from the intestine.
- Does not cause any damage to the intestinal villi.
- Composed of GRAS (Generally Regarded As Safe) lipids.
- Safe as demonstrated by a one-year double blind oral feeding study in Cystic Fibrosis (CF) children.
As a lipid-based monomer, the patented Lym-X-Sorb® drug complex is recognized in the intestinal lumen as a nutrient and therefore allowed to proceed into the thoracic lymph for systemic delivers; thus avoiding the liver and subsequent first pass metabolism. This recognition and metabolic by-pass greatly enhances the ultimate drug concentration in plasma. When examined at equivalent doses in beagle dogs, Lym-X-Sorb® - N -(4-hydroxyphenyl) (fenretinide) complexes demonstrated 3 to 4 times the peak plasma concentrations of current delivery systems. Human bio-equivalence studies demonstrate 65mg doses of fenretinide complexed with Lym-X-Sorb® present nearly identical plasma levels to 300 mg dosages via conventional corn oil delivery—5 times the Lym-X-Sorb® dose. Image #9
Lym-X-Sorb® molecular structure coupled with a drug
Lym-X-Sorb® improves the solubility and stability of drugs:
Feasibility trials have shown fenretinide, insulin, histrelin, a estradiol, nifedipin analogues, hydrochlorothiazide, MCN-5703, capsaicin, diltiazen, renin inhibitors, hydrocortisone, cromolyn, pramoxine, bruprenorphine, progesterone, clyclosporin A, metronidazole, and gentamicin to be stable within the Lym-X-Sorb® monomer.
Complexed with the drug of choice in a 1:1 molar ratio, the matrix forms stable particles 10 to 70nm in size that are readily absorbed in the presence of sodium bicarbonate and bile salt. The small and enveloping nature of the Lym-X-Sorb® monomer serves to not only protect the drug from digestive degradation but it also protects the stomach and intestine from potential drug-induced cytotoxicity.