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.
Highlights
Since 2017, the Food and Drug Administration (FDA) has noted a growing trend in the number of new drugs approved
The aim of this study was to analyze the modification of sulindac release profiles from SBA-15-functionalized silicas
We adapted the methodology presented by Zhao with modifications [8]
Summary
Since 2017, the Food and Drug Administration (FDA) has noted a growing trend in the number of new drugs approved. In 2017–2020, 46, 59, 48, and 53 new active substances were approved as medicines each year, respectively [1]. Pharmaceutics 2021, 13, 1693 exhibit poor water solubility and, a low bioavailability. A favorable form of drug delivery is the oral route due to the low cost and simplicity of use for the patient. The oral route ensures the highest rate of patient compliance and, therapy effectiveness. The efficiency of oral therapy is closely related to drug solubility in the gastrointestinal tract and the ability to penetrate the biological membranes. These two parameters determine the classification of medicinal substances into BCS
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
