Gastrointestinal absorption of heparin by lipidization or coadministration with penetration enhancers.

Abstract:

:A review with 93 references. Heparins are high molecular weight, hydrophilic polyanions, which are unstable under acidic conditions; and therefore they exhibit poor oral bioavailability. Consequently they must be administered via the parenteral route which is expensive, inconvenient, and limits use by outpatients. The development of an oral form of heparin is warranted. This review examined the literature, mostly published between January 2000 and January 2005, pertaining to the gastrointestinal absorption of heparin by lipidization or coadministration with penetration enhancers. A lipidization strategy that was examined involved conjugation of low molecular weight heparin with deoxycholic acid. The majority of studies examined the ability of different formulations, typically utilizing penetration enhancers, to improve heparin bioavailability. The penetration enhancers used included fatty acids, Labrasol, Gelucire 44/14, polycationic lipophilic-core dendrons, saponins, mono-N-carboxymethyl chitosan, Carbopol 934P, a combination of thiolated polycarbophil and glutathione, polymeric nanoparticles, polymeric microparticles, sodium N-[8-(2-hydroxybenzoyl) amino]caprylate (SNAC), and sodium N-[10-(2-hydroxybenzoyl)amino]decanoate (SNAD). The variety of models used and doses of heparin/penetration enhancers applied, however, made it difficult to compare the results between studies. Nevertheless, all of the reviewed drug delivery systems showed therapeutic value and confirmation of the promising results obtained from animal studies, by progression to clinical trials, is necessary. Overall, progress has been made in the quest for an oral heparin formulation.

journal_name

Curr Drug Deliv

journal_title

Current drug delivery

authors

Ross BP,Toth I

doi

10.2174/1567201054367968

keywords:

subject

Has Abstract

pub_date

2005-07-01 00:00:00

pages

277-87

issue

3

eissn

1567-2018

issn

1875-5704

journal_volume

2

pub_type

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