Evaluation of mesoporous carbon aerogels as carriers of the non-steroidal anti-inflammatory drug ibuprofen

Abstract

Towards the development of novel drug carriers for oral delivery of poorly soluble drugs mesoporous aerogel carbons (CAs), namely CA10 and CA20 with different pore sizes (10 and 20nm, respectively), were evaluated. The non-steroidal anti-inflammatory lipophilic compound ibuprofen was incorporated via passive loading. The drug loaded carbon aerogels were systemically investigated by means of High-Resolution Transmission Electron Microscopy (HR-TEM), Nitrogen physisorption studies, X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), X-ray photon electron spectroscopy (XPS) and ζ-potential studies. In vitro release studies were performed in simulated intestinal fluids reflecting both fasted (FaSSIF) and fed (FeSSIF) state conditions. Cytotoxicity studies were conducted with human intestinal cells (Caco-2). Drug was in an amorphous state in the pores of the carbon carrier as shown from the physicochemical characterization studies. The results showed marked differences in the release profiles for ibuprofen from the two aerogels in the media tested whereas in vitro toxicity profiles appear to be compatible with potential therapeutic applications at low concentrations.

Oral Drug Delivery Systems Based on Ordered Mesoporous Silica Nanoparticles for Modulating the Release of Aprepitant

“…Figure 11C) demonstrated a slight inhibition of cell growth (t-test, p > 0.05) for particles concentration of 100 and 500 μg/mL, an indication that these materials might be considered potentially cytotoxic at these concentrations (ISO 10993-5). Importantly, this effect does not seem to be dose-dependent, and could be attributed to mechanical obstruction of the materials to cell proliferation potential [34,35]. The results obtained in the current study are in good agreement with previous studies where ordered mesoporous silica did not exhibit any toxicity when tested in Caco-2 cell lines [36][37][38].…”

“…The in vitro cytotoxicity effects of the MSN particles in Caco-2 cultures was assessed by counting the cell number using the improved Neubauer hemocytometer chamber and an optical microscope [34,[46][47][48]. Prior to each test, the cells were harvested using trypsin (Euroclone)-ethylenediamine tetraacetic acid (EDTA, Sigma-Aldrich)phosphate-buffered saline (PBS) solution (0.25% trypsin-0.05 mM EDTA) and diluted at a density of 10 5 cells/mL.…”

“…After cell attachment (3-4 h), the material suspensions of MCM-41, aprepitant-loaded MCM-41, MCM-48, and aprepitant-loaded MCM-48, with increasing concentration (100, 500, and 2000 μg/mL), were added to the cultures and cells were incubated for 48 h. Subsequently, cells were detached by trypsinization and the number of cells in culture was measured using the Neubauer chamber under the microscope in an attempt to evaluate the effect of the MSN particles on cell proliferation. Simultaneously, the cellular death in Caco-2 cultures was assessed using the trypan-blue dye exclusion method [34,48]. Then cell growth capacity in treated cultures was expressed as a percentage (%) of that observed in the untreated control.…”

Alginate-Based Aerogel Particles as Drug Delivery Systems: Investigation of the Supercritical Adsorption and In Vitro Evaluations

“…In addition, the use of supercritical fluids for the impregnation of active pharmaceutical ingredients, allows to obtain compositions with controlled drug delivery [27,28]. This allows to create a drug with a reduced content of the active substance (compared to already existing drugs), while the therapeutic effect after the use of this tool increases, as well as increases the safety for the patient [29,30].…”

Ανάπτυξη Και Χαρακτηρισμός Φαρμακομορφών Για Παρειακή Χορήγηση Με Τη Χρήση Δισδιάστατης Και Τρισδιάστατης Εκτύπωσης

“…Ο χαρακτηρισμός της στερεάς κατάστασης επέδειξε την επιτυχή πλαστικοποίηση του πολυμερούς, την πλήρη αναμιξιμότητα των ενσωματωμένων υλικών, και την αμορφοποίηση Vis SDP 10-A VP. Οι συνθήκες προσαρμόστηκαν από προηγούμενη βιβλιογραφική αναφορά(Eleftheriadis et al, 2016). Συγκεκριμένα χρησιμοποιήθηκε ως στατική φάση μια στήλη Discovery RP Amide C16 (15 cm, 4.6 mm, 5 μm), ως κινητή φάση τρόπο ώστε να επιτρέπει την πλήρη εμβύθιση των υμενίων και να ικανοποιεί την αξίωση μοριακής διασποράς της αποδεσμευμένης ποσότητας IBU καθ'όλη τη διάρκεια της μελέτης (sink conditions)(Eleftheriadis et al, 2019;Tang et al, 2014).Οι δειγματοληψίες λάβανε χώρα σε προκαθορισμένα χρονικά διαστήματα σε διάρκεια 6 h από το διαμέρισμα του δέκτη, φυγοκεντρήθηκαν σε 4000 rcf και φιλτραρίστηκαν μέσω 0.45 μm PVDF φίλτρων.…”