Colon-Specific Drug Delivery Behavior of pH-Responsive PMAA/Perlite Composite

• Main Authors: Mehrdad Mahkam, Laleh Vakhshouri
• Format: Article
• Language: English
• Published: MDPI AG 2010-04-01
• Series: International Journal of Molecular Sciences
• Subjects: methacrylic acid; perlite; silylation; polymerization; polymer grafting
• Online Access: http://www.mdpi.com/1422-0067/11/4/1546/

The preparation, characterization, and in vitro release of 5-aminosalicylic acid (5-ASA)from methacrylic acid (MAA)/perlite composites (APC) prepared via a sol–gel route are reported. The free-radical graft polymerization of methacrylic acid (MAA) onto perlite particles was studied experimentally. The grafting procedure consisted of surface activation with 3-(trimethoxysilyl) propyl methacrylate (TSPA), followed by free-radical graft polymerization of methacrylic acid (MAA) in ethyl acetate with 2,2΄-azobis-isobutyronitrile (AIBN) initiator. The composition of the composites hybrid materials was determined by FTIR spectroscopy. Equilibrium swelling studies were carried out in enzyme-free simulated gastric and intestinal fluids (SGF and SIF, respectively). The dried composites were immersed in a saturated solution of 5-ASA in water overnight and dried over a period of three days at room temperature and the in vitro release profiles were established separately in both (SGF, pH 1) and (SIF, pH 7.4). The 5-ASA concentration of the solution was measured using a UV-Vis spectrophotometer (205 nm) at different time intervals. The in vitro drug release test revealed that the release rate of 5-ASA in buffer solutions increased with the silica content in the composites; on the contrary, the increase of the content of 3-(trimethoxysilyl)propyl methacrylate (TSPA), a coupling agent, decreased the drug release rate.