Modification of the Release of Poorly Soluble Sulindac with the APTES-Modified SBA-15 Mesoporous Silica

Abstract

The effectiveness of oral drug administration is related to the solubility of a drug in the gastrointestinal tract and its ability to penetrate the biological membranes. As most new drugs are poorly soluble in water, there is a need to develop novel drug carriers that improve the dissolution rate and increase bioavailability. The aim of this study was to analyze the modification of sulindac release profiles in various pH levels with two APTES ((3-aminopropyl)triethoxysilane)-modified SBA-15 (Santa Barbara Amorphous-15) silicas differing in 3-aminopropyl group content. Furthermore, we investigated the cytotoxicity of the analyzed molecules. The materials were characterized by differential scanning calorimetry, powder X-ray diffraction, scanning and transmission electron microscopy, proton nuclear magnetic resonance and Fourier transformed infrared spectroscopy. Sulindac loaded on the SBA-15 was released in the hydrochloric acidic medium (pH 1.2) and phosphate buffers (pH 5.8, 6.8, and 7.4). The cytotoxicity studies were performed on Caco-2 cell line. The APTES-modified SBA-15 with a lower adsorption capacity towards sulindac released the drug in a less favorable manner. However, both analyzed materials improved the dissolution rate in acidic pH, as compared to crystalline sulindac. Moreover, the SBA-15, both before and after drug adsorption, exhibited insignificant cytotoxicity towards Caco-2 cells. The presented study evidenced that SBA-15 could serve as a non-toxic drug delivery system that enhances the dissolution rate of sulindac and improves its bioavailability.

APTES-Modified SBA-15 as a Non-Toxic Carrier for Phenylbutazone

“…It was suggested that motion, which is characterized by the relaxation times τ 02 = 5.8 × (s) and the activation energy E a 2 = 3.7 (kJ/mol) can be associated with local motion of the methyl group. The third low temperature motion described by the relaxation time τ 03 = 7.8 × (s) and low activation energy E a 3 = 1.8 (kJ/mol) may be related to the jumps of the hydrogen atom in hydrogen bonds, which arise as a result of the interaction of the NH 2 amine groups of the modified silica with the incorporated drug [ 17 ].…”

“…The SBA-15 mesoporous silica was synthesized in accordance with the protocol described by Zhao et al [ 2 ], with modifications presented in our previous study [ 17 ]. The SBA-15 surface modification process was carried out using the grafting method [ 17 ]. Briefly, we dried the silica for 24 h at 110 °C.…”

“…Solid-state 1 H-NMR measurements were carried out on a pulse spectrometer operating at a frequency of 25 MHz (El-Lab Tel-Atomic, Jackson, MI, USA) [ 17 ]. The samples of PBZ and SBA-15-pr-NH 2 :PBZ were sealed in the glass tubes and degassed.…”

Surface Biofunctionalization of Gadolinium Phosphate Nanobunches for Boosting Osteogenesis/Chondrogenesis Differentiation

“…At this time, the OD values of the GdPO 4 •H 2 O/PLGA, GdPO 4 •H 2 O@SiO 2 /PLGA, GdPO 4 •H 2 O@SiO 2 -APS/PLGA and PBLGg-GdPO 4 •H 2 O/PLGA groups were all higher than those of PLGA, especially the OD values of PBLG-g-GdPO 4 •H 2 O/PLGA cultured cells, which were the highest, with significant differences (p < 0.05). This indicates that the modifiers had good biocompatibility, which may have been the consequence of the positive biocompatibility and biological effects of GdPO 4 •H 2 O, SiO 2 , APS and polyglutamic acid in PBLG [32,[41][42][43][44]. At 7 days of incubation, the OD values of the groups were similar, with only the GdPO 4 •H 2 O@SiO 2 /PLGA and PBLG-g-GdPO 4 •H 2 O/PLGA groups having slightly higher OD values than the glass, GdPO 4 •H 2 O/PLGA and GdPO 4 •H 2 O@SiO 2 -APS/PLGA groups, but there was no significant difference (p > 0.05).…”

Mesoporous Materials as Elements of Modern Drug Delivery Systems for Anti-Inflammatory Agents: A Review of Recent Achievements

“…The most common mesoporous material used as a carrier in drug delivery systems (DDSs) is mesoporous silica and its more advanced forms such as mesoporous silica nanoparticles, mesoporous silica nanorods or bioactive glasses [ 153 , 154 , 155 , 156 ]. Other materials often used for this purpose are mesoporous carbon [ 157 ], mesoporous calcium silicate and mesoporous calcium sulfate [ 150 ].…”