Safety and efficacy of sodium caprate in promoting oral drug absorption : from in vitro to the clinic

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Title: Safety and efficacy of sodium caprate in promoting oral drug absorption : from in vitro to the clinic
Authors: Maher, Sam
Leonard, Thomas W
Jacobson, Jette
Brayden, David James
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Date: 17-Dec-2009
Abstract: A major challenge in oral drug delivery is the development of novel dosage forms to promote absorption of poorly permeable Class III drugs across the intestinal epithelium. To date, no absorption promoter has been approved in a formulation specifically designed for oral delivery of Class III molecules. Promoters that are designated safe for human consumption have been licensed for use in a recently approved buccal insulin spray delivery system and also for many years as part of an ampicillin rectal suppository. Unlike buccal and rectal delivery, oral formulations containing absorption promoters have the additional technical hurdle whereby the promoter and payload must be co-released in high concentrations at the small intestinal epithelium in order to generate significant but rapidly reversible increases in permeability. The most advanced promoter in the clinic is the medium chain fatty acid (MCFA), sodium caprate (C10) , a compound already approved as a direct food additive. We discuss how it has evolved to a matrix tablet format suitable for administration to humans under the headings of mechanism of action at the cellular and tissue level and in vitro and in vivo efficacy and safety studies. In specific clinical examples, we review how C10-based formulations are being tested for oral delivery of bisphosphonates using Gastro Intestinal Permeation Enhancement Technology, GIPET (Merrion Pharmaceuticals, Ireland) and in a related solid dose format for anti-sense oligonucleotides (ISIS Pharmaceuticals, USA).
Funding Details: Science Foundation Ireland
Type of material: Journal Article
Publisher: Elsevier
Journal: Advanced Drug Delivery Reviews
Volume: 61
Issue: 15
Start page: 1427
End page: 1449
Copyright (published version): 2009 Elsevier B.V.
Keywords: Sodium caprateAbsorption promoterOral drug deliveryDrug delivery platformsClinical trialsOral formulationDrug delivery systems
Subject LCSH: Drug delivery systems
Fatty acids
Intestinal absorption
Oral medication
DOI: 10.1016/j.addr.2009.09.006
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Language: en
Status of Item: Peer reviewed
Appears in Collections:Irish Drug Delivery Network Research Collection

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