pH-sensitive inulin-based nanomicelles for intestinal site-specific and controlled release of celecoxib

Delia Mandracchia, Adriana Trapani, Sara Perteghella, Milena Sorrenti, Laura Catenacci, Maria Luisa Torre, Giuseppe Trapani, Giuseppe Tripodo

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

Aiming at a site-specific drug release in the lower intestinal tract, this paper deals with the synthesis and physicochemical/biological characterization of pH-sensitive nanomicelles from an inulin (INU) amphiphilic derivative. To allow an intestinal site specific release of the payload, INU-Vitamin E (INVITE) bioconjugates were functionalized with succinic anhydride to provide the system with pH-sensitive groups preventing a premature release of the payload into the stomach. The obtained INVITESA micelles resulted nanosized, with a low critical aggregation concentration and the release studies showed a marked pH-dependent release. The drug loading stabilized the micelles against the acidic hydrolysis. From transport studies on Caco-2 cells, resulted that INVITESA nanomicelles cross the cellular monolayer but are actively re-transported in the secretory (basolateral-apical) direction when loaded in apical side. It suggests that the entrapped drug could not be absorbed before the release from the micelles, enabling so a local release of the active.

Lingua originaleInglese
pagine (da-a)570-578
Numero di pagine9
RivistaCarbohydrate Polymers
Volume181
DOI
Stato di pubblicazionePubblicato - 1 feb 2018
Pubblicato esternamente

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