Thiolated polycarbophil/glutathione: Defining its potential as a permeation enhancer for oral drug administration in comparison to sodium caprate

Perera, Glen; Barthelmes, Jan; Vetter, Anja; Krieg, Christof; Uhlschmied, C.; Bonn, Günther K.; Bernkop‐Schnürch, Andreas

doi:10.3109/10717544.2011.570807

Cited by 11 publications

(7 citation statements)

References 23 publications

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“…In Caco-2 cells, concentrations of 25 mM to 50 mM C 10 are necessary to increase permeability 53 . In all studies, C 10 caused much higher permeation ratios for small molecules (up to 1 kDa) than for large molecules (4 to 20 kDa) 53 , 54 , 57 . This biphasic permeability corresponds to the size-dependent permeation of molecules through Caco-2 or human intestinal epithelial (T84) monolayers, as shown by Watson and colleagues.…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 76%

“…These studies have mostly used cells from the colon 53 , 54 or kidney, 55 , 56 but also freshly isolated brain capillaries 55 and excised rat intestinal mucosa 57 . In these experiments TER decreased and/or the permeability of molecules with a molecular weight between 182 and 10,000 Da increased after incubation with C 10 (Table 2).…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

“…Perhaps this could be explained by the dilution effect in vivo, by the protective intestinal mucus layer or by the high regeneration of mucosa cell 41 . Furthermore, while the t max (time point at which the maximal concentration is reached) of a drug or marker administered with C 10 in vivo is between 10 to 60 min, 43 , 48 , 57 the in vitro effect lasts at least 300 min 56 . After removal of C 10 , it takes 120 min until the TER is back to control values 54 .…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

“…Possibilities include reincubation with C 10 or coadministration in a liquid or solid form, e.g., tablets by spray freeze-drying 43 , 57 , 68 . Because the uptake of C 10 in vivo is quite fast (t max ~7 min, 48 ) after injection, the drug is injected before and after the application of C 10 52 .…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

“…It was found that the solid form enhanced uptake much better than the liquid form. Additionally, the smaller marker is taken up to a greater extent than the larger marker 57 . An in situ drug delivery study showed that co-administration of C 10 and FD4 achieved the optimal effect compared with pre-incubation with C 10 68 .…”

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

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Trends in drug delivery through tissue barriers containing tight junctions

2013

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A limitation in the uptake of many drugs is the restricted permeation through tissue barriers. There are two general ways to cross barriers formed by cell layers: by transcytosis or by diffusion through the intercellular space. In the latter, tight junctions (TJs) play the decisive role in the regulation of the barrier permeability. Thus, transient modulation of TJs is a potent strategy to improve drug delivery. There have been extensive studies on surfactant-like absorption enhancers. One of the most effective enhancers found is sodium caprate. However, this modulates TJs in an unspecific fashion. A novel approach would be the specific modulation of TJ-associated marvel proteins and claudins, which are the main structural components of the TJs. Recent studies have identified synthetic peptidomimetics and RNA interference techniques to downregulate the expression of targeted TJ proteins. This review summarizes current progress and discusses the impact on TJs' barrier function.

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Section: Substances To Modulate Tight Junctionsmentioning

confidence: 76%

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

Section: Substances To Modulate Tight Junctionsmentioning

confidence: 99%

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Trends in drug delivery through tissue barriers containing tight junctions

2013

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Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

Hock¹,

Racaniello

Aspinall

et al. 2021

Advanced Science

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Advances in nanotechnology have generated a broad range of nanoparticles (NPs) for numerous biomedical applications. Among the various properties of NPs are functionalities being related to thiol substructures. Numerous biological processes that are mediated by cysteine or cystine subunits of proteins representing the workhorses of the bodies can be transferred to NPs. This review focuses on the interface between thiol chemistry and NPs. Pros and cons of different techniques for thiolation of NPs are discussed. Furthermore, the various functionalities gained by thiolation are highlighted. These include overall bio-and mucoadhesive, cellular uptake enhancing, and permeation enhancing properties. Drugs being either covalently attached to thiolated NPs via disulfide bonds or being entrapped in thiolated polymeric NPs that are stabilized via inter-and intrachain crosslinking can be released at the diseased tissue or in target cells under reducing conditions. Moreover, drugs, targeting ligands, biological analytes, and enzymes bearing thiol substructures can be immobilized on noble metal NPs and quantum dots for therapeutic, theranostic, diagnostic, biosensing, and analytical reasons. Within this review a concise summary and analysis of the current knowledge, future directions, and potential clinical use of thiolated NPs are provided.

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