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

Abstract

Two different types of ordered mesoporous nanoparticles, namely MCM-41 and MCM-48, with similar pore sizes but different pore connectivity, were loaded with aprepitant via a passive diffusion method. The percentage of the loaded active agent, along with the encapsulation efficiency, was evaluated using High-performance Liquid Chromatography (HPLC) analysis complemented by Thermogravimetric Analysis (TGA). The determination of the pore properties of the mesoporous particles before and after the drug loading revealed the presence of confined aprepitant in the pore structure of the particles, while Powder X-ray Diffractometry(pXRD), Differential Scanning Calorimetry (DSC), and FTIR experiments indicated that the drug is in an amorphous state. The release profiles of the drug from the two different mesoporous materials were studied in various release media and revealed an aprepitant release up to 45% when sink conditions are applied. The cytocompatibility of the silica nanoparticles was assessed in Caco-2 cell monolayers, in the presence and absence of the active agent, suggesting that they can be used as carriers of aprepitant without presenting any toxicity in vitro.

Mesoporous Silica Particles as Drug Delivery Systems—The State of the Art in Loading Methods and the Recent Progress in Analytical Techniques for Monitoring These Processes

“…High performance liquid chromatography (HPLC) is used to separate, identify, and quantify different mixture components, and it is applied to confirm the chemical stability of the molecules loaded into nanoparticles [237,238], entrapment efficiency [239,240], and to obtain the drug release curves, as demonstrated in the release studies of naproxen [15], paclitaxel [87], resveratrol [241], felodipine and furosemide [17], and many others. For the determination of drug loading efficiency, after the completion of the loading process, samples undergo centrifugation and the unloaded molecules present in the supernatant are analyzed by HPLC, as was shown in the case of rifampin [242].…”

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

“…They have claimed that the absence of the melting peak of doxycycline hyclate in the DSC curve resulted from the formation of an inclusion complex between drug molecules and β-cyclodextrin. Moreover, the disappearance of DSC peaks characteristic for melting points of other drugs such as aprepitant [ 33 ], ketoprofen [ 34 ], ticagrelor [ 35 ] have been reported for various mesoporous silicas and suggested both the successful encapsulation of drug molecules and their amorphous or semi-crystalline nature inside the pores.…”

The Physical Chemistry and Chemical Physics (PCCP) Section of the International Journal of Molecular Sciences in Its Publications: The First 300 Thematic Articles in the First 3 Years

“…This thematic area is associated with articles [ 12 , 15 , 20 , 21 , 26 , 50 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 , 101 ], of which there are a total of 50. In contrast to the areas already discussed above, articles of all four types are presented here ( Table 5 ), although, here, too, the Original constitutes a clear majority over the other 3 types of articles.…”

“…Since all of the above articles were included in two special issues, “Ion and Molecule Transport in Membrane Systems” and “Ion and Molecule Transport in Membrane Systems 2.0”, it is quite understandable that there are two editorials among them, namely [ 99 , 100 ]. Only less than 10 articles belong to the surface sciences proper, namely [ 12 , 15 , 20 , 21 , 83 , 91 , 96 , 97 , 98 ], and the topics and objects of research are also very diverse. For example, in [ 12 ], the synthesis of Mobil Composition of Matter 41 (MCM-41) mesoporous silica nanoparticles of controlled sizes and porous structure has been performed.…”

“…For example, in [ 12 ], the synthesis of Mobil Composition of Matter 41 (MCM-41) mesoporous silica nanoparticles of controlled sizes and porous structure has been performed. Three articles were related to the study of mesoporous silica nanoparticles; so, in the first of them [ 20 ], it was shown how, after coating mesoporous silica particles with various polyelectrolytes or proteins, it is possible to produce completely individualized hollow shells for encapsulating various drugs; in the second [ 96 ], mesoporous silica with large pores were developed for the transfer of large biomolecules and their release from these pores by changing the acidity of the medium; and, in the third [ 97 ], two different types of ordered mesoporous nanoparticles, using the passive diffusion method. It should be noted that among these publications, there is also a specialized review [ 21 ], which is also devoted to such mesoporous silica nanoparticles, which are functionalized to target them to subcellular compartments, with an emphasis on the cytoplasm, mitochondria, and the nucleus.…”