Studies on the Intestinal Absorption of Low Molecular Weight Heparin Using Saturated Fatty Acids and Their Derivatives as an Absorption Enhancer in Rats

Mori, Shiori; Matsuura, Akihiro; Prasad, Y. V. Rama; Takada, Kanji

doi:10.1248/bpb.27.418

Cited by 34 publications

(23 citation statements)

References 18 publications

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“…27 Fondaparinux, like Hp, is presumed unstable under acidic enzymatic conditions. 48 Few studies support the observations that Hps are absorbed by the gastrointestinal tract but they do not reach therapeutic concentration. 49 Active transport is involved and is pH-dependent, preferably around pH = 7.…”

Section: Discussionmentioning

confidence: 99%

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

Ramadan¹,

Lagarce²,

Tessier-Marteau³

et al. 2011

IJN

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Abstract:Oral anticoagulant therapy could be advanced using lipid-based nanoparticulate systems. This study examined lipid nanocapsules for their oral absorption potential as the first step in developing oral fondaparinux (Fp) novel carriers. Using phase inversion method and cationic surfactants such as hexadecyltrimethyl ammonium bromide (CTAB) or stearylamine (SA), cationic lipid nanocapsules (cLNCs), loaded with Fp on their surface, were prepared and characterized (zeta potential, size and Fp association efficiency and content). In vivo studies were conducted after single oral increasing doses of Fp-loaded cLNCs (0.5 to 5 mg/kg of Fp) in rats and the concentration of Fp in the plasma was measured by anti-factor Xa activity assay. The monodisperse, (∼50 nm), positively charged Fp-cLNCs with high drug loadings demonstrated linear pharmacokinetic profiles of the drug with an increased oral absolute bioavailability (up to ∼21%) compatible with therapeutic anticoagulant effect (.0.2 µg/mL).

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Section: Discussionmentioning

confidence: 99%

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

Ramadan¹,

Lagarce²,

Tessier-Marteau³

et al. 2011

IJN

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“…PEs cannot avoid endogenous bile salts within the upper GI, where levels are 2-6 mM in the fasted state and 7-16mM in the fed state [160], although one would expect such loss of efficacy to be reduced at in vivo PE dose levels above their CMC, as free monomer concentration would be efficiently restored and can offset initial removal into mixed micelles by the presence of bile salts. Low concentrations of surfactant-based PEs often cause a rapid decrease in TEER in Caco-2 monolayers, but then no further decrease is detected over time [150,161]. Initially, the predominant monomeric form is likely to have stripped phospholipids from the plasma membrane to reduce TEER and increase paracellular permeability, but then the free monomer concentration is reduced due to incorporation into the membrane and into mixed micelles.…”

Section: Cmc In Permeation Enhancementmentioning

confidence: 99%

“…A growing number of delivery systems based on lipoidal dispersions improve oral peptide delivery. In many cases, the surfactants used in the stabilisation of lipoidal dispersions also function as transcellular PEs [161]. improved absorption of heparin following jejunal delivery in rats in vivo [279].…”

Section: Permeation Enhancement From Complex Lipoidal Dispersionsmentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

291

201

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Publication informationAdvanced Drug Delivery Reviews, (Part B): 277-319 Publisher ElsevierItem record/more information http://hdl.handle.net/10197/7800Publisher's statement þÿ T h i s i s t h e a u t h o r s v e r s i o n o f a w o r k t h a t w a s a c c e p t e d f o r p u b l i c a t i o n i n A d v a n c e d D r u g Delivery Reviews. Changes resulting from the publishing process, such as peer review,

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“…10 Strategic functionalization with some membrane permeation enhancers or ligands for receptors expressed on the cellular membrane may also promote the transcellular transport of entrapped drugs. 11,12,15 In addition to transcellular transport, nanodrugs equipped with bioadhesive polymers or chelators could enhance the paracellular transport of entrapped drugs, via the regulation of tight junctions. 16,17 Surface modification of nanodrugs, with specific proteins, antibodies, and other biomolecules, can be used to design drugs that act selectively on particular tissues, 18 and this approach has been employed to provide improved therapeutic potential and reduced side effects of some anticancer drugs.…”

mentioning

confidence: 99%

Nanodrugs: pharmacokinetics and safety

Onoue¹,

Yamada²,

Chan³

2014

IJN

316

153

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To date, various nanodrug systems have been developed for different routes of administration, which include dendrimers, nanocrystals, emulsions, liposomes, solid lipid nanoparticles, micelles, and polymeric nanoparticles. Nanodrug systems have been employed to improve the efficacy, safety, physicochemical properties, and pharmacokinetic/pharmacodynamic profile of pharmaceutical substances. In particular, functionalized nanodrug systems can offer enhanced bioavailability of orally taken drugs, prolonged half-life of injected drugs (by reducing immunogenicity), and targeted delivery to specific tissues. Thus, nanodrug systems might lower the frequency of administration while providing maximized pharmacological effects and minimized systemic side effects, possibly leading to better therapeutic compliance and clinical outcomes. In spite of these attractive pharmacokinetic advantages, recent attention has been drawn to the toxic potential of nanodrugs since they often exhibit in vitro and in vivo cytotoxicity, oxidative stress, inflammation, and genotoxicity. A better understanding of the pharmacokinetic and safety characteristics of nanodrugs and the limitations of each delivery option is necessary for the further development of efficacious nanodrugs with high therapeutic potential and a wide safety margin. This review highlights the recent progress in nanodrug system development, with a focus on the pharmacokinetic advantages and safety challenges.

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Studies on the Intestinal Absorption of Low Molecular Weight Heparin Using Saturated Fatty Acids and Their Derivatives as an Absorption Enhancer in Rats

Cited by 34 publications

References 18 publications

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

Intestinal permeation enhancers for oral peptide delivery

Nanodrugs: pharmacokinetics and safety

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