Mesoporous silica pellets as bifunctional bone drug delivery system for cefazolin

Mesoporous Silica-Bioglass Composite Pellets as Bone Drug Delivery System with Mineralization Potential

“…The pellets achieved a mean 4.8-log reduction of bacterial growth compared to control, thus excellent bactericidal activity was proved. Similar log reductions were obtained for cefazolin-loaded pellets in our previous study [ 43 ] and for cefazolin/linezolid loaded stainless steel medical grade tubes with potential use as a drug-eluting fixation pin for orthopedic applications [ 44 ]. It might be concluded that obtained pellets fulfill an important criterion of bone drug delivery system, where initial high doses of the drug are required for effective local eradication of bacteria, followed by a sustained release which maintains antibacterial effect.…”

“…In our previous works, we investigated different types of bone drug delivery systems with mineralization potential such as xerogels [ 56 , 57 ], membranes [ 23 , 29 ], powders [ 58 , 59 ], granules [ 55 ], and pellets [ 22 , 43 ]. In the case of previously described pellets, the mineralization potential was provided by either use of MCM-41-calcium phosphate composite [ 22 ] or the addition of hydroxyapatite synthesized via microwave-assisted hydrothermal precipitation method [ 43 ]. The difficulty of such pellets manufacturing is the fact that remineralizing component requires the optimization of its synthesis, composition, and the mineralization potential of such component must be confirmed before its use in the formulation of pellets.…”

“…Herein, the combination of DOX-loaded MCM-41 with bioglass as a remineralizing component seems to overcome the abovementioned difficulties due to the simple synthesis of bioglass and its well-known mineralization potential in vitro and excellent biomineralization in vivo. Moreover, the use of bioglass powder in the pellets formulation allowed to fully replace the microcrystalline cellulose which was used in the previously obtained pellets [ 22 , 43 ]. The elimination of microcrystalline cellulose is another benefit of proposed pellets due to fact that this excipient is characterized by extremely poor mineralization properties.…”

“…Pellets were obtained on a laboratory scale (5 g batch size) in Caleva Multi Lab apparatus using a preoptimized wet granulation, extrusion, and spheronization method [ 43 ]. Silica powders: BG (3.75 g), MCM-41 (0.6 g), and MCM-DOX (0.4 g; equal to 29.3 mg of adsorbed DOX) together with ethyl cellulose (0.25 g, EC, Aqualon N22 Pharm, 20 cP, Warsaw, Poland) were mixed in the mortar and wet-granulated using 4.0 g ethanolic solution (80% ( v / v ) of 5 wt% EC with 2 wt% polydimethylsiloxane (PDMS, hydroxy-terminated, 65 cSt, Sigma-Aldrich, Poznan, Poland) as a binder.…”

“…Cytotoxicity assay was carried out using the already described procedure [ 22 , 43 ]. Human fetal osteoblasts, hFOB 1.19 (ATCC, cat.…”