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Enhanced ileal absorption of a hydrophilic macromolecule, pentosan polysulfate sodium (PPS)
Liang Dong1, Alicia Yum, Joe Nguyen
1ALZA Corporation, 1010 Joaquin Road, P.O. Box 7210, Mountain View, CA 94039-7210, USA. ldong2@alzus.jnj.com
Abstract:
An in situ gelling, bioadhesive liquid formulation was developed to enhance the bioavailbility (BA) of a polysaccharide, pentosan polysulfate sodium (PPS). The formulation was tested to determine its bioavailability enhancement in a non-flush/non-ligated rat ileal model. A potent synergistic effect was found with a gelling agent Cremophor and a permeation enhancer sodium salicylate. The absolute bioavailabilities were 1.9%, 4.6%, 6.3% and 46.4%, respectively, for the PPS solution in saline, sodium salicylate/PPS, Cremophor/PPS and Cremophor/sodium salicylate/PPS. Therefore, we successfully demonstrated the approach of utilizing an in situ gelling/bioadhesive liquid carrier to enhancing the bioavailability of a hydrophilic macromolecule at the distal small intestine.
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