Effects of various absorption enhancers on transport of clodronate through Caco-2 cells

Raiman, Johanna; Törmälehto, Soili; Yritys, Kirsi; Junginger, Hans E.; Mönkkönen, Jukka

doi:10.1016/s0378-5173(03)00300-4

Cited by 38 publications

(18 citation statements)

References 26 publications

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“…To answer the question as to whether Au-NP transport is mediated by a transcellular or paracellular route, pre-treatment of the FAE model with ethylene glycol tetraacetic acid (EGTA) was carried out, which is known to increase molecule uptake by paracellular pathway [29]. The transported levels of Au-NP and Au 3+ ions were not affected by EGTA treatment (Figure 3b).…”

Section: Resultsmentioning

confidence: 99%

“…Their energy-dependent and transcellular transport by M cells was also confirmed by decrease in transport amounts at 4 °C (61%) and after pre-treatment with clathrin-mediated endocytosis inhibitor (61%). No significantly different transport of Au-NPs after EGTA treatment, which induces the opening of enterocyte tight junctions [29], indicates their transcytosis mechanism by M cells, not by a paracellular route. On the other hand, Au 3+ ions were found to have different transport mechanism compared to Au-NPs, showing much high transport by M cells and significantly increased translocation through Caco-2 monolayers as well.…”

Section: Discussionmentioning

confidence: 99%

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Oral Toxicity and Intestinal Transport Mechanism of Colloidal Gold Nanoparticle-Treated Red Ginseng

Bae

Jin

et al. 2016

Nanomaterials

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(1) Background: Application of nanotechnology or nanomaterials in agricultural food crops has attracted increasing attention with regard to improving crop production, quality, and nutrient utilization. Gold nanoparticles (Au-NPs) have been reported to enhance seed yield, germination rate, and anti-oxidant potential in food crops, raising concerns about their toxicity potential. In this study, we evaluated the oral toxicity of red ginseng exposed to colloidal Au-NPs during cultivation (G-red ginseng) in rats and their intestinal transport mechanism. (2) Methods: 14-day repeated oral administration of G-red ginseng extract to rats was performed, and body weight, hematological, serum biochemical, and histopathological values were analyzed. An in vitro model of human intestinal follicle-associated epithelium (FAE) and an intestinal epithelial monolayer system were used for intestinal transport mechanistic study. (3) Results: No remarkable oral toxicity of G-red ginseng extract in rats was found, and Au-NPs did not accumulate in any organ, although Au-NP transfer to G-red ginseng and some increased saponin levels were confirmed. Au-NPs were transcytozed by microfold (M) cells, but not by a paracellular pathway in the intestinal epithelium. (4) Conclusion: These findings suggest great potential of Au-NPs for agricultural food crops at safe levels. Further study is required to elucidate the functional effects of Au-NPs on ginseng and long-term toxicity.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Oral Toxicity and Intestinal Transport Mechanism of Colloidal Gold Nanoparticle-Treated Red Ginseng

Bae

Jin

et al. 2016

Nanomaterials

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“…This could be explained by the ability of chitosan to cause opening of tight junctions (111). Raiman et al (112) studied the effects of four different permeation enhancers, palmitoyl‐ dl ‐carnitine chloride (PCC), TMC, sodium caprate (C10) and ethylene glycol bis(2‐aminoethyl ether)‐ N , N , N ′, N ′‐tetraacetic acid (EGTA) on the transport of clondronate through CCM. At the investigated concentrations, PCC, TMC, and EGTA led to a strong enhancement in the clondronate permeation, without reducing the viability of the cells.…”

Section: Applications Of Ccmmentioning

confidence: 99%

Role of Caco-2 Cell Monolayers in Prediction of Intestinal Drug Absorption

Shah¹,

Jogani²,

Bagchi³

et al. 2006

Biotechnol. Prog.

204

125

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The usefulness of Caco-2 cell monolayers in determining the intestinal drug absorption of potential drug candidates as such and from delivery systems, elucidating the underlying mechanisms thereof, presystemic metabolism, cellular uptake and cytotoxicological assessment has been exemplified in this review. The role of Caco-2 cell monolayers in studying the effectiveness, involved mechanism and toxicity of various excipients for drug absorption promotion has also been discussed.

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“…Surfactants such as sodium lauryl sulphate and medium chain fatty acid esters were found to increase bisphosphonate absorption (Boulenc et al, 1995;Lindmark et al, 1998). Comparative evaluation of different enhancers was carried out by Raiman et al (2003). It was observed that enhancers acting on the tight junctions were most effective over other categories.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Floating Risedronate Sodium–Gelucire® 43/01 Formulations

Chauhan

Shimpi

Mahadik

et al. 2005

Drug Development and Industrial Pharmacy

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Single and multi-unit floating matrices of risedronate sodium were prepared using Gelucire 43/01 by melt solidification and melt granulation technique, respectively. The controlled release floating matrices were evaluated for in vitro and in vivo floating ability and in vitro drug release. Effect of aging on Gelucire 43/01 was evaluated by hot stage microscopy (HSM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), in vitro floating ability, and in vitro drug release. Multi-unit system obtained has shown initial burst release, which was suppressed in single unit system. Both single- as well as multi-unit systems showed increase in rate of drug release on aging due to changes in the properties of the Gelucire 43/01. Multi-unit matrices obtained by melt granulation were relatively easier for scale up and advantageous if the initial burst release does not cause any significant clinical adversity.

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Effects of various absorption enhancers on transport of clodronate through Caco-2 cells

Cited by 38 publications

References 26 publications

Oral Toxicity and Intestinal Transport Mechanism of Colloidal Gold Nanoparticle-Treated Red Ginseng

Oral Toxicity and Intestinal Transport Mechanism of Colloidal Gold Nanoparticle-Treated Red Ginseng

Role of Caco-2 Cell Monolayers in Prediction of Intestinal Drug Absorption

Preparation and Evaluation of Floating Risedronate Sodium–Gelucire® 43/01 Formulations

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