Mucoadhesive Properties and Interaction with P-Glycoprotein (P-gp) of Thiolated-Chitosans and -Glycol Chitosans and Corresponding Parent Polymers: A Comparative Study

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• 作者：Adriana Trapani ; Claudio Palazzo ; Marialessandra Contino ; Maria Grazia Perrone ; Nicola Cioffi ; Nicoletta Ditaranto ; Nicola Antonio Colabufo ; Massimo Conese ; Giuseppe Trapani ; Giovanni Puglisi
• 刊名：Biomacromolecules
• 出版年：2014
• 出版时间：March 10, 2014
• 年：2014
• 卷：15
• 期：3
• 页码：882-893
• 全文大小：526K
• 年卷期：v.15,no.3(March 10, 2014)
• ISSN：1526-4602

文摘

The aim of the present work was to compare the mucoadhesive and efflux pump P-glycoprotein (P-gp) interacting properties of chitosan (CS)- and glycolchitosan (GCS)-based thiomers and corresponding unmodified parent polymers. For this purpose, the glycol chitosan-N-acetyl-cysteine (GCS-NAC) and glycol chitosan-glutathione (GCS-GSH) thiomers were prepared under simple and mild conditions. Their mucoadhesive characteristics were studied by turbidimetric and zeta potential measurements. The P-gp interacting properties were evaluated measuring the effects of thiolated- and unmodified-polymers on the bidirectional transport (BA/AB) of rhodamine-123 across Caco-2 cells as well as in the calcein-AM and ATPase activity assays. Although all the thiomers and unmodified polymers showed optimal-excellent mucoadhesive properties, the best mucoadhesive performances have been obtained by CS and CS-based thiomers. Moreover, it was found that the pretreatment of Caco-2 cell monolayer with GCS-NAC or GCS restores Rho-123 cell entrance by inhibiting P-gp activity. Hence, GCS-NAC and GCS may constitute new biomaterials useful for improving the bioavailability of P-gp substrates.