Sublingual Heparin in Hyperlipemia

Fuller, Harvey L.

doi:10.1177/000331975800900511

Cited by 13 publications

(1 citation statement)

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“…The oral mucosa, floor of mouth, underside of tongue and gingival mucosa offers excellent accessibility, is not easily traumatized and avoids degradation of macromolecular drug resulting from oral gastrointestinal absorption and first-pass hepatic metabolism [31]. The early claims for sublingual delivery of heparins [32][33][34][35][36] have been challenged and did not survive critical investigations [10,37,38]. For example, tablets containing 20,000 U of UFH with and without ethylenediamine tetraacetic acid (EDTA) as penetration enhancers did not show any significant changes in bioactivity in the plasma of treated patients [10].…”

Section: Heparin Containing Dds For Sublingual Routementioning

confidence: 99%

The quest for non-invasive delivery of bioactive macromolecules: A focus on heparins

Motlekar

Youan

2006

Journal of Controlled Release

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The development of a non-invasive drug delivery system for unfractionated heparin (UFH) and low molecular weight heparins (LMWHs) has been the elusive goal of several research groups since the initial discovery of this glycosaminogylcan by McLean in 1916. After a brief update on current parenteral formulations of UFH and LMWHs, this review revisits past and current strategies intended to identify alternative routes of administration (e.g. oral, sublingual, rectal, nasal, pulmonary and transdermal). The following strategies have been used to improve the bioavailability of this bioactive macromolecule by various routes: (i) enhancement in cell-membrane permeabilization, (ii) modification of the tight-junctions, (iii) increase in lipophilicity and (iv) protection against acidic pH of the stomach. Regardless of the route of administration, a simplified unifying principle for successful non-invasive macromolecular drug delivery may be: "to reversibly overcome the biological, biophysical and biochemical barriers and to safely and efficiently improve the in vivo spatial and temporal control of the drug in order to achieve a clinically acceptable therapeutic advantage". Future macromolecular drug delivery research should embrace a more systemic approach taking into account recent advances in genomics/proteomics and nanotechnology.

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