New Biodegradable Hydrogels Based on Inulin and α,β-Polyaspartylhydrazide Designed for Colonic Drug Delivery: In Vitro Release of Glutathione and Oxytocin.
Succinic derivatives of inulin (INU-SA) with two different degrees of derivatization (20% and 30%, mol/mol) were cross-linked with α,β-polyaspartylhydrazide (PAHy) to obtain INUPAHy hydrogels. Cross-linking was performed using N-ethyl-N-(3-dimethylaminopropyl)-carbodiimide hydrochloride (EDC) and N-hydroxysulfosuccinimide (NHSS) as coupling agents and by varying the reaction time (4 h, 8 h and 24 h). All samples prepared were characterized by FT-IR analysis and swelling measurements in different media. In vitro assays, performed in the presence of inulinase, demonstrated the degradability of the prepared hydrogels. Cell compatibility was evaluated using Caco-2 cells through both direct and indirect assay. Glutathione (GSH) and oxytocin (OT), both potential agents for the treatment of colonic inflammation, were entrapped into a INUPAHy hydrogel and their release was evaluated in simulated gastrointestinal fluids. The obtained results suggest that GSH- and OT-loaded INUPAHy hydrogels are potentially useful for the oral treatment of inflammatory bowel disease.
Mandracchia
Delia
D
a Dipartimento Farmaco-Chimico, Università di Bari, Via Orabona 4, 70125 Bari, Italy.
Denora
Nunzio
N
Franco
Massimo
M
Pitarresi
Giovanna
G
Giammona
Gaetano
G
Trapani
Giuseppe
G
D018938:Caco-2 Cells; D002234:Carbodiimides / Q000737:chemistry; D002470:Cell Survival; D002851:Chromatography, High Pressure Liquid; D003106:Colon; D004123:Dimethylamines / Q000737:chemistry; D016503:Drug Delivery Systems; D005978:Glutathione / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D020100:Hydrogels / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy; D007444:Inulin / Q000031:analogs & derivatives / Q000737:chemistry; D008422:Materials Testing; D015394:Molecular Structure; D009077:Mucins / Q000737:chemistry; D010121:Oxytocin / Q000008:administration & dosage / Q000493:pharmacokinetics; D010455:Peptides / Q000737:chemistry; D011108:Polymers; D017550:Spectroscopy, Fourier Transform Infrared; D013388:Succinimides / Q000737:chemistry; D013997:Time Factors
D002234:Carbodiimides; D004123:Dimethylamines; D020100:Hydrogels; D009077:Mucins; C569266:N-ethyl-N'-(3-(dimethylamino)-propyl)carbodiimide; D010455:Peptides; D011108:Polymers; D013388:Succinimides; C442699:poly(aspartylhydrazide); D010121:Oxytocin; C035761:N-hydroxysulfosuccinimide; D007444:Inulin; D005978:Glutathione