Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers
The effect of N-trimethylchitosan chloride on the intestinal permeability of capreomycin sulfate, a polypeptide antibiotic, using an in vitro model, was evaluated. To improve the mucoadhesivity and permeation enhancer properties of N-trimethylchitosan chloride, it was used a synthetic pathway that s...
Guardado en:
Autores principales: | , , , , , |
---|---|
Formato: | Articulo |
Lenguaje: | Inglés |
Publicado: |
2012
|
Materias: | |
Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/18098 http://www.latamjpharm.org/resumenes/31/2/LAJOP_31_2_1_11.pdf |
Aporte de: |
id |
I19-R120-10915-18098 |
---|---|
record_format |
dspace |
institution |
Universidad Nacional de La Plata |
institution_str |
I-19 |
repository_str |
R-120 |
collection |
SEDICI (UNLP) |
language |
Inglés |
topic |
Farmacia Absorption enhancern CaCo-2; capreomycin sulfate; N-trimethyl chitosan Farmacología |
spellingShingle |
Farmacia Absorption enhancern CaCo-2; capreomycin sulfate; N-trimethyl chitosan Farmacología Plessing, Carlos von Torres, Pablo Rivas, Coralia Guzmán, Paula Núñes, Christian Sepúlveda, Jacqueline Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
topic_facet |
Farmacia Absorption enhancern CaCo-2; capreomycin sulfate; N-trimethyl chitosan Farmacología |
description |
The effect of N-trimethylchitosan chloride on the intestinal permeability of capreomycin sulfate, a polypeptide antibiotic, using an in vitro model, was evaluated. To improve the mucoadhesivity and permeation enhancer properties of N-trimethylchitosan chloride, it was used a synthetic pathway that selectively alkylated the amino groups and not the hydroxyl groups in carbons 3 and 6, which decreases the potency of the polymer, leading to use higher quantities and limit its potential as a functional excipient.
This non-methoxylated derivative of the studied polymer reduced in a reversible way the transepithelial electrical resistance of CaCo-2 monolayers at concentrations not higher than 0.003 % w/v, indicating that the absence of steric hindrance from methoxyl groups improves the effect of N-trimethylchitosan chloride, but at expense of a narrow range of action and higher cytotoxicity. The results of in vitro permeation studies conducted in bicameral Transwell® systems suggested that the permeability of capreomycin sulfate is low, although it was not established if the transport is exclusively paracellular or membrane transporters are involved. By using increasing concentrations of the polymer in the range of 0.001 - 0.003% w/v, it was observed a slight increase in the transport of capreomycin. Therefore, it was concluded that further studies should use N-trimethylchitosan chloride with a lower degree of quaternization or controlled methoxylation, in order to increase the mass to use and obtain a product that is able to remain retained in the intestinal lumen and which in turn interacts with the epithelium. |
format |
Articulo Articulo |
author |
Plessing, Carlos von Torres, Pablo Rivas, Coralia Guzmán, Paula Núñes, Christian Sepúlveda, Jacqueline |
author_facet |
Plessing, Carlos von Torres, Pablo Rivas, Coralia Guzmán, Paula Núñes, Christian Sepúlveda, Jacqueline |
author_sort |
Plessing, Carlos von |
title |
Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
title_short |
Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
title_full |
Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
title_fullStr |
Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
title_full_unstemmed |
Effect of a non-methoxylated N-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in CaCo-2 cell monolayers |
title_sort |
effect of a non-methoxylated n-trimethyl chitosan chloride derivative over capreomycin sulfate permeability in caco-2 cell monolayers |
publishDate |
2012 |
url |
http://sedici.unlp.edu.ar/handle/10915/18098 http://www.latamjpharm.org/resumenes/31/2/LAJOP_31_2_1_11.pdf |
work_keys_str_mv |
AT plessingcarlosvon effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers AT torrespablo effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers AT rivascoralia effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers AT guzmanpaula effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers AT nuneschristian effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers AT sepulvedajacqueline effectofanonmethoxylatedntrimethylchitosanchloridederivativeovercapreomycinsulfatepermeabilityincaco2cellmonolayers |
bdutipo_str |
Repositorios |
_version_ |
1764820463789277184 |