Abstract
The use of ordered mesoporous matrices, and in particular carbon-based mesoporous nanoparticles has shown great potential towards enhancing the bioavailability of orally administered drugs. Nevertheless, elucidation of the in vivo absorption, distribution, and excretion of such carriers is essential for understanding their behaviour, and radiolabelling provides a very useful way to track their occurrence inside the body. In this work, uniform spherical CMK-1-type ordered mesoporous carbon nanoparticles have been radiolabelled with Technetium-99m (99mTc) and traced after oral administration to mice. Ex vivo biodistribution studies showed that the radiolabelled nanoparticles accumulated almost exclusively in the gastrointestinal tract; complete elimination of the radiotracer was observed within 24 h after administration, with practically no uptake into other main organs. These findings along with the results from in vitro stability studies indicate that the spherical carbon nanoparticles examined could be safely used as drug carriers with minimal side effects, but also support the great value of radiolabelling methods for monitoring the particles’ behaviour in vivo.
Highlights
Oral drug delivery [1] constitutes the most widely used, cost-effective, non-invasive administration strategy for treating patients with comfort and simplicity [2]
When developing the chromatogram in sodium citrate, [99m Tc]Tc-CMK-1 and free [99m Tc]TcO4 - are expected to move with the solvent front (Rf = 0.8–1.0), whereas [99m Tc]TcO2 remained at the origin (Rf = 0.0–0.2) [56,59,66]
By combining the results derived from the two developing systems, radiochemical purity (RCP) of [99m Tc]Tc-CMK-1 was calculated according to the following formula:
Summary
Oral drug delivery [1] constitutes the most widely used, cost-effective, non-invasive administration strategy for treating patients with comfort and simplicity [2]. Over the past few years, a number of reports [30] have confirmed that mesoporous carbon materials can effectively encapsulate various poorly water-soluble drugs (e.g., ibuprofen [11,31,32], indomethacin [24], fenofibrate [33], simvastatin [34], carvedilol [35,36], itraconazole [37] etc.) and enhance their dissolution and bioavailability In addition to their great efficiency in terms of drug loading and controlled release, some MCNs exhibit significant optoelectronic, photothermal-conversion and photoacoustic-generation properties, due to sp hybridization, while their surface can carry stimuli-responsive, fluorescent or targeting agents through π-π stacking [38,39,40,41,42,43,44,45]. The obtained results combined with the in vitro stability studies are of high importance for the validation of the respective drug delivery systems, helping showcase their suitability for real therapeutic applications
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