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.
Casadei
Maria Antonietta
MA
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università La Sapienza, Piazzale Aldo Moro 5, 00185 Roma, Italy.
Pitarresi
Giovanna
G
Calabrese
Rossella
R
Paolicelli
Patrizia
P
Giammona
Gaetano
G
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