Biodegradable and pH-sensitive hydrogels for potential colon-specific drug delivery: characterization and in vitro release studies.
A novel pH-sensitive and biodegradable composite hydrogel, based on a methacrylated and succinic derivative of dextran, named Dex-MA-SA, and a methacrylated and succinic derivative of alpha,beta-poly( N-2-hydroxyethyl)- DL-aspartamide (PHEA), named PHM-SA, was produced by photocross-linking. The goal was to obtain a colon-specific drug delivery system, exploiting both the pH-sensitive behavior and the colon-specific degradability. The hydrogel prepared with a suitable ratio between the polysaccharide and the polyaminoacid was characterized regarding its swelling behavior in gastrointestinal simulated conditions, chemical and enzymatic degradability, interaction with mucin, and cell compatibility on CaCo-2 cells. Moreover, 2-methoxyestradiol was chosen as a model of anticancer drug and release studies, were performed in the absence or in the presence of dextranase and esterase. The obtained hydrogel, due to its pH-sensitive swelling and enzymatic degradability, together with mucoadhesion and cell compatibility, could be potentially useful as system for the oral treatment of colonic cancer.
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.
Maria Antonietta
MA
Casadei
Giovanna
G
Pitarresi
Rossella
R
Calabrese
Patrizia
P
Paolicelli
Gaetano
G
Giammona
D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D003106:Colon / Q000378:metabolism*; D016503:Drug Delivery Systems; D006801:Humans; D020100:Hydrogels / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D009077:Mucins / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared
D020100:Hydrogels; D009077:Mucins