Colon drug delivery is aimed at the administration of selected drugs to act locally or even systematically. Corticosteroid drugs are often used exerting even pronounced side effects due to systemic absorption. Here a new drug delivery system (DDS) based on the chemical conjugation of beta-cyclodextrin to inulin to form the INUCD bioconjugate is described. It was designed with the aim to provide this DDS with colon degradable portions (inulin) which degradation products have direct beneficial effects on the well-being of the colon and with a carrier that can solubilize hydrophobic drugs (beta-cyclodextrin). This system was specifically designed to promote a local/topical activity with a significant reduction of the drug systemic absorption. The INUCD bioconjugate was obtained by a simple chemistry binding beta-cyclodextrin to an inulin succinate previously synthesized. The bioconjugate was then characterized in terms of physicochemical properties by ATR-FTIR 1H-NMR DSC and TGA DLS and SEM. Furthermore phase solubility test by using curcumin as a model drug were performed as well as biologic evaluations for cytocompatibility and drug transport across in vitro simulated physiological barriers. Moreover enzymatic degradation studies by inulinase were performed. From the gained results a predictable local drug release of the payload could be attained so allowing a local delivery of e.g. corticosteroids thus avoiding a systemic absorption especially in prolonged therapies.

Combination of inulin and beta-cyclodextrin properties for colon delivery of hydrophobic drugs

Catenacci, Laura;Sorrenti, Milena
;
Perteghella, Sara;Torre, Maria L.;Milanese, Chiara;Tripodo, Giuseppe
2020-01-01

Abstract

Colon drug delivery is aimed at the administration of selected drugs to act locally or even systematically. Corticosteroid drugs are often used exerting even pronounced side effects due to systemic absorption. Here a new drug delivery system (DDS) based on the chemical conjugation of beta-cyclodextrin to inulin to form the INUCD bioconjugate is described. It was designed with the aim to provide this DDS with colon degradable portions (inulin) which degradation products have direct beneficial effects on the well-being of the colon and with a carrier that can solubilize hydrophobic drugs (beta-cyclodextrin). This system was specifically designed to promote a local/topical activity with a significant reduction of the drug systemic absorption. The INUCD bioconjugate was obtained by a simple chemistry binding beta-cyclodextrin to an inulin succinate previously synthesized. The bioconjugate was then characterized in terms of physicochemical properties by ATR-FTIR 1H-NMR DSC and TGA DLS and SEM. Furthermore phase solubility test by using curcumin as a model drug were performed as well as biologic evaluations for cytocompatibility and drug transport across in vitro simulated physiological barriers. Moreover enzymatic degradation studies by inulinase were performed. From the gained results a predictable local drug release of the payload could be attained so allowing a local delivery of e.g. corticosteroids thus avoiding a systemic absorption especially in prolonged therapies.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/1346017
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