Influence of molecular weight on oral absorption of water soluble chitosans

Chae, Su Young; Jang, Mi-Kyeong; Nah, Jae‐Woon

doi:10.1016/j.jconrel.2004.10.012

Cited by 339 publications

(155 citation statements)

References 34 publications

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“…Our results showed that the higher concentrations of TM-Bz-CS resulted in higher cytotoxicity. This is in agreement with the findings of a previous study in which the CS showed concentration-dependent cytotoxic effects on Caco-2 cells (16). Therefore, this high concentration (2.5-5 mM) of TM-Bz-CS might damage the cells and result in the lack of recovery in the TEER.…”

Section: Discussionsupporting

confidence: 93%

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Methylated N-(4-N,N-Dimethylaminobenzyl) Chitosan, a Novel Chitosan Derivative, Enhances Paracellular Permeability Across Intestinal Epithelial Cells (Caco-2)

et al. 2008

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Abstract. The aim of this study was to investigate the effect of methylated N-(4-N,N-dimethylaminobenzyl) chitosan, TM-Bz-CS, on the paracellular permeability of Caco-2 cell monolayers and its toxicity towards the cell lines. The factors affecting epithelial permeability, e.g., degree of quaternization (DQ) and extent of dimethylaminobenzyl substitution (ES), were evaluated in intestinal cell monolayers of Caco-2 cells using the transepithelial electrical resistance and permeability of Caco-2 cell monolayers, with fluorescein isothiocyanate dextran 4,400 (FD-4) as a model compound for paracellular tight-junction transport. Cytotoxicity was evaluated with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide viability assay. The results revealed that, at pH 7.4, TM-Bz-CS appeared to increase cell permeability in a concentration-dependent manner, and this effect was relatively reversible at lower doses of 0.05-0.5 mM. Higher DQ and the ES caused the permeability of FD-4 to be higher. The cytotoxicity of TM-Bz-CS depended on concentration, %DQ, and %ES. These studies demonstrated that this novel modified chitosan has potential as an absorption enhancer.

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Section: Discussionsupporting

confidence: 93%

“…The relative viability (%) was calculated based on absorbance at 550 nm using a microplate reader (Universal Microplate Analyzer, Model AOPUS01 and AI53601, Packard BioScience, CT, USA). Viability of nontreated control cells was arbitrarily defined as 100% (16).…”

Section: Evaluation Of Cytotoxicitymentioning

confidence: 99%

Methylated N-(4-N,N-Dimethylaminobenzyl) Chitosan, a Novel Chitosan Derivative, Enhances Paracellular Permeability Across Intestinal Epithelial Cells (Caco-2)

et al. 2008

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“…Chitosan of varying characteristics are generally biocompatible, and induce low cytotoxicity in various type of cell lines (Chae et al, 2005;Kean and Thanou, 2010). We tested the effect on cell viability induced by chitosan and complexes of chitosan with pEGFP or with pEGFPsiRNA in comparison with the corresponding ones formed by Lipofectamine, the commonly used lipotransfection agent.…”

Section: Discussionmentioning

confidence: 99%

Chitosan as a non-viral co-transfection system in a cystic fibrosis cell line

Fernández

Santos-Carballal

Weber

et al. 2016

International Journal of Pharmaceutics

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Successful gene therapy requires the development of suitable vehicles for the selective and efficient delivery of genes to specific target cells at the expense of minimal toxicity. In this work, we investigated a non-viral gene delivery system based on chitosan (CS) to specifically address cystic fibrosis (CF). Thus, electrostatic self-assembled CS-pEGFP and CS-pEGFPsiRNA complexes were prepared from high-pure fully characterized CS (Mw ~20 kDa and degree of acetylation ~30%). The average diameter of positively-charged complexes (i.e.  ~ +25 mV) was ~200 nm. The complexes were found relatively stable over 14 h in OptiMEM. Cell viability study did not show any significant cytotoxic effect of the CS-based complexes in a human bronchial cystic fibrosis cell line (s). We evaluated the transfection efficiency of this cell line with both CS-pEGFP and co-transfected with CS-pEGFP-siRNA complexes at (N/P) charge ratio of 12. We reported an increase in the fluorescence intensity of CS-pEGFP and a reduction in the cells co-transfected with CS-pEGFP-siRNA. This study shows proof-of-principle that co-transfection with chitosan might be an effective delivery system in a human CF cell line. It also offers a potential alternative to further develop therapeutic strategies for inherited disease treatments, such as CF.

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“…Interactions between chitosan, surfactants and insulin resulted in smaller microemulsion sizes [97]. Moreover, low molecular weight chitosans were chosen to prepare the nanoparticles, since their intestinal absorption is known to be significantly better than the high molecular weight candidates and showed a negligible cytotoxic effect on the Caco-2 cells [98].…”

Section: Rationalementioning

confidence: 99%

Oral Delivery of Insulin: Novel Approaches

Elsayed¹

2012

Recent Advances in Novel Drug Carrier Systems

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Influence of molecular weight on oral absorption of water soluble chitosans

Cited by 339 publications

References 34 publications

Methylated N-(4-N,N-Dimethylaminobenzyl) Chitosan, a Novel Chitosan Derivative, Enhances Paracellular Permeability Across Intestinal Epithelial Cells (Caco-2)

Methylated N-(4-N,N-Dimethylaminobenzyl) Chitosan, a Novel Chitosan Derivative, Enhances Paracellular Permeability Across Intestinal Epithelial Cells (Caco-2)

Chitosan as a non-viral co-transfection system in a cystic fibrosis cell line

Oral Delivery of Insulin: Novel Approaches

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