Permeation enhancer effect of chitosan and chitosan derivatives: Comparison of formulations as soluble polymers and nanoparticulate systems on insulin absorption in Caco-2 cells

Sadeghi, A.M.M.; Dorkoosh, Farid Abedin; Avadi, Mohammad Reza; Weinhold, Mirko X.; Bayat, Ali Ahmad; Delié, Florence; Gurny, Robert; Larijani, Bagher; Rafiee-Tehrani, Morteza; Junginger, Hans E.

doi:10.1016/j.ejpb.2008.03.004

Cited by 194 publications

(125 citation statements)

References 30 publications

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“…Chitosan exerts maximal cell permeation effect in an acidic environment [52]. The pH in the duodenum region of the intestine is 5.8, and this provides an environment particularly suited for chitosan to act as a mucoadhesive, as the pH is close to its pKa value (5.5) [53]. Our results are in agreement with this; chitosan containing nanocarriers demonstrated high iron absorption, an effect that may be attributed to its mucoadhesive properties at the intestinal physiological pH.…”

Section: Iron Absorption From Ascorbyl Palmitate Nanocarrierssupporting

confidence: 81%

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

Zariwala

Farnaud

Merchant

et al. 2014

Colloids and Surfaces B: Biointerfaces

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Section: Iron Absorption From Ascorbyl Palmitate Nanocarrierssupporting

confidence: 81%

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

Zariwala

Farnaud

Merchant

et al. 2014

Colloids and Surfaces B: Biointerfaces

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“…It is important to understand the possible effects of the protective matrix on intestinal barrier function. For example, the food grade polymer chitosan, used in encapsulation matrices, can itself increase tight junction permeability (Sadeghi et al, 2008). Such particles are used in the drug/medical industry to help open tight junctions to allow particles through (targeted drug delivery).…”

Section: Delivering Probiotic Bacteria To Infantsmentioning

confidence: 99%

The Role of Intestinal Barrier Function in Early Life in the Development of Colitis

Anderson¹,

Dalziel²,

Gopal³

et al. 2012

Colitis

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“…Only a few experimental in vitro methods have so far been established for prediction of drug absorption capability in vivo. Caco-2 monolayers are generally accepted to be a suitable in vitro model for drug transport studies as these cells have been shown to express most of the enzymatic, functional and morphological characteristics of the intestinal and morphological characteristics of the intestinal mucosa [12,13] . However, Caco-2 monolayers cannot be used to predict the regional differences in the permeability of drugs in the gastrointestinal tract.…”

Section: Discussionmentioning

confidence: 99%

Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

Huang¹,

Li²,

Luo³

et al. 2008

WJG

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AIM:To investigate the permeability characteristics of rebamipide across intestinal mucosa, and examine the effects of some absorption enhancers on the permeability across the colonic tissue. Another purpose is to demonstrate the colon-specific delivery of rebamipide with or without absorption enhancers using chitosan capsule as a carrier. METHODS: The permeability of rebamipide was evaluated using an in vitro diffusion chamber system, and the effects of some absorption enhancers on the permeability via colon were further investigated. The release of rebamipide from chitosan or gelatin capsule was studied by Japan Pharmacopoeia rotating basket method. The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms. RESULTS: The permeability of rebamipide across the jejunal or ileal membranes was higher than the colonic membranes. Both sodium laurate (C12) and labrasol significantly increased permeability across the colon membranes. On the other hand, the release of rebamipide from chitosan capsule was less than 10% totally within 6 h. The area under concentration-time profile of drug in the colon mucosa using chitosan capsules (AUCLI, 1 6011.2 ng · h/g) was 2.5 times and 4.4 times greater than using gelatin capsules and CMC suspension, respectively. Meanwhile, the area under concentration-time profile of drug in the plasma (AUCPL) was 1016.0 ng · h/mL for chitosan capsule, 1887.9 ng · h/mL for CMC suspension p and 2163.5 ng·h/mL for gelatin capsule. Overall, both AUCLI and AUCPL were increased when C12 was coadministrated, but the increase of AUCLI was much greater; the drug delivery index (DDI) was more than 1 compared with simple chitosan capsule group. CONCLUSION: There was a regional difference in the permeability of Rebamipide across the jejunum, ileum and the colon, and passive diffusion seems to be one of the major transport mechanisms of rebamipide. Absorption enhancers can increase the permeability of rebamipide across the colon tissue significantly. In addition, chitosan capsule may be a useful carrier to deliver rebamipide to the colon specifically and the coadministration of C12 with rebamipide may also be very useful in local treatment.© 2008 The WJG Press. All rights reserved.Key words: Rebamipide; Diffusion chamber; Permeability; Sodium laurate; Chitosan capsule; Colon-specific delivery Peer reviewer: Atsushi Nakajima, Professor, Yokohama City University Hospital, 3-9 Fukuura Kanazawaku, Yokohama 236, Japan Huang BB, Li GF, Luo JH, Duan L, Nobuaki K, Akira Y. Permeabilities of rebamipide via the rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier.

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Permeation enhancer effect of chitosan and chitosan derivatives: Comparison of formulations as soluble polymers and nanoparticulate systems on insulin absorption in Caco-2 cells

Cited by 194 publications

References 30 publications

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: Preparation, characterisation and in vitro evaluation

The Role of Intestinal Barrier Function in Early Life in the Development of Colitis

Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

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