In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition

Gaetano Giammona, Nicola Antonio Colabufo, Adriana Trapani, Giuseppe Trapani, Maria Grazia Perrone, Delia Mandracchia, Giuseppe Tripodo

Risultato della ricerca: Article

12 Citazioni (Scopus)

Abstract

Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor. Pre-treatment of Caco-2 cell monolayer with a GCS solution or GCS-based nanoparticles increased the absorptive transport of Rho-123 across the monolayer of 1.43-fold. The modification of GCS with 2-iminothiolane led to GCS-TBA conjugate which did not show any P-gp inhibitory activity. Therefore, GCS polymer and corresponding dosage forms may contribute to increase the oral bioavailability of Pgp-substrate drugs, while GCS-TBA cannot be used for the same purpose.
Lingua originaleEnglish
pagine (da-a)73-82
Numero di pagine10
RivistaCarbohydrate Polymers
Volume166
Stato di pubblicazionePublished - 2017

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Glycols
Chitosan
Pumps
Glycoproteins
P-Glycoprotein
Dosage Forms
Monolayers
Nanoparticles
glycol-chitosan
Substrates
Suspensions
Polymers
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Organic Chemistry
  • Polymers and Plastics
  • Materials Chemistry

Cita questo

Giammona, G., Colabufo, N. A., Trapani, A., Trapani, G., Perrone, M. G., Mandracchia, D., & Tripodo, G. (2017). In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition. Carbohydrate Polymers, 166, 73-82.

In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition. / Giammona, Gaetano; Colabufo, Nicola Antonio; Trapani, Adriana; Trapani, Giuseppe; Perrone, Maria Grazia; Mandracchia, Delia; Tripodo, Giuseppe.

In: Carbohydrate Polymers, Vol. 166, 2017, pag. 73-82.

Risultato della ricerca: Article

Giammona, G, Colabufo, NA, Trapani, A, Trapani, G, Perrone, MG, Mandracchia, D & Tripodo, G 2017, 'In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition', Carbohydrate Polymers, vol. 166, pagg. 73-82.
Giammona, Gaetano ; Colabufo, Nicola Antonio ; Trapani, Adriana ; Trapani, Giuseppe ; Perrone, Maria Grazia ; Mandracchia, Delia ; Tripodo, Giuseppe. / In vitro evaluation of glycol chitosan based formulations as oral delivery systems for efflux pump inhibition. In: Carbohydrate Polymers. 2017 ; Vol. 166. pagg. 73-82.
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AU - Giammona, Gaetano

AU - Colabufo, Nicola Antonio

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AU - Perrone, Maria Grazia

AU - Mandracchia, Delia

AU - Tripodo, Giuseppe

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AB - Recently, we have reported that glycol chitosan (GCS) was able to reverse the P- glycoprotein (P-gp) efflux pump. The objective of the present study was to evaluate the potential of two GCS-based dosage forms (aqueous solution or nanoparticle suspension) for oral administration of the P-gp substrate Rho-123. A further aim of the present study was to assess the effect of the glycol chitosan-4-thiobutylamidine thiomer (GCS-TBA) on P-gp activity considering that the corresponding thiomer of chitosan series is a well-known P-gp inhibitor. Pre-treatment of Caco-2 cell monolayer with a GCS solution or GCS-based nanoparticles increased the absorptive transport of Rho-123 across the monolayer of 1.43-fold. The modification of GCS with 2-iminothiolane led to GCS-TBA conjugate which did not show any P-gp inhibitory activity. Therefore, GCS polymer and corresponding dosage forms may contribute to increase the oral bioavailability of Pgp-substrate drugs, while GCS-TBA cannot be used for the same purpose.

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