Modifying release of poorly soluble active pharmaceutical ingredients with the amine functionalized SBA-16 type mesoporous materials

Abstract

SBA-16 and two modified SBA-16 type ordered mesoporous silica were used as the carriers for ibuprofen (anti-inflammatory drug) and furosemide (loop diuretic drug). Modification of the solid carrier was prepared with chitosan or N-3[(amino(poly-propylenoxy)]aminopropyltrimethoxysilane. The samples of carriers and carrier-drug loaded materials were characterized by X-ray diffraction, N2 adsorption, Fourier-transform infrared spectroscopy, thermogravimetry, and differential scanning calorimetry. The release profiles of active pharmaceutical ingredients were performed in media with different pH in the USP 2 apparatus as well as in two biorelevant media (fasted state simulated gastric fluid and fasted state small intestinal fluid) in USP 4 apparatus. The loading of active substances into mesoporous materials was performed with modified immersion method. The maximum content of deposited drug in mesoporous material was close to 12.0 and 2.2 wt.% for ibuprofen and furosemide, respectively. After drug adsorption, the reduction of BET surface area, pore volume and pore diameter of non-modified and modified SBA-16 was observed, while the cubic arrays of siliceous matrix were well preserved. The release profiles of ibuprofen and furosemide loaded in mesoporous materials in media with different pH and biorelevant fasted state simulated gastric fluid and fasted state small intestinal fluid showed that the new SBA-16 type materials modify the release profiles of furosemide, increasing the dissolution rate of these substances in the medium at pH 1.2. The cytotoxicity of the materials and permeability of drugs after their loading on SBA-16 materials were evaluated on Caco-2 model. The results of our study showed that mesoporous materials did not exert cytotoxic effects and did not influence on the permeability of both active pharmaceutical ingredients in relation to pure substances.

Synthesis and Characterization of Hierarchical Zeolites Modified with Polysaccharides and Its Potential Role as a Platform for Drug Delivery

“…Based on the results of the release of ibuprofen from hierarchical zeolites ( Figure 4 ), it can be concluded that all polysaccharide-modified materials showed higher release rates compared to unmodified materials. Previously, the same tendency was observed after the modification of the surface with amine groups, i.e., the structure of mesoporous molecular sieve of SBA-16-type modified with chitosan significantly affects the release rate of furosemide [ 55 ]. A correlation was observed between the release rate of ibuprofen and the type of polysaccharide used during the synthesis of hierarchical zeolites.…”

Recent Advances in the Preparation and Applications of Organo‐functionalized Porous Materials

“…In addition, the high hydrophobic nature and the rich basic sites on the surface of the functionalized KIT‐6 helped to achieve much better adsorption and release profile of ibuprofen than pure KIT‐6 materials, revealing the importance of the functionalized moieties in the DDS. Similarly, ibuprofen (anti‐inflammatory) and furosemide (loop diuretic) were adsorbed onto the pure and chitosan and amino‐functionalized SBA‐16 with 3D porous structure and studied the release profiles of these drugs at different pH in simulating gastrointestinal tract . The authors reported no change in the bioavailability of ibuprofen for different carriers, and the functionalized materials did not show any cytotoxic effects and showed excellent releasing profile.…”