Abstract
In recent decades, the versatility of mesoporous silica particles and their relevance to develop controlled release systems have been demonstrated. Within them, gated materials able to modulate payload delivery represent great advantages. However, the role played by the porous matrix in this kind of systems is scarce. In this work, different mesoporous silica materials (MCM-41, MCM-48, SBA-15 and UVM-7) are functionalized with oleic acid as a molecular gate. All systems are fully characterized and their ability to confine the entrapped cargo and release it in the presence of bile salts is validated with release assays and in vitro digestion experiments. The cargo release profile of each synthesized support is studied, paying attention to the inorganic scaffold. Obtained release profiles fit to Korsmeyer–Peppas model, which explains the differences among the studied supports. Based on the results, UVM-7 material was the most appropriate system for duodenal delivery and was tested in an in vivo model of the Wistar rat. Payload confinement and its complete release after gastric emptying is achieved, establishing the possible use of mesoporous silica particles as protection and direct release agents into the duodenum and, hence, demonstrating that these systems could serve as an alternative to the administration methods employed until now.
Highlights
The use of mesoporous silica particles (MSPs) as delivery systems of bioactive molecules has been reinforced during recent years
Within the wide field of MSPs, microparticles present a special interest for the controlled release in the lumen of the gastrointestinal tract (GIT), since their large size makes their internalization in healthy epithelial tissues difficult [24,25,26]
Phosphate Buffer Solution (PBS), Dulbecco’s Modified Eagle’s Medium (DMEM), Fetal Bovine Serum (FBS), penicillin/streptomycin antibiotic (P/S), non-essential amino acids and all the needed mediums for cell culture were provided by Labclinics (Labclinics S.A., Barcelona, Spain)
Summary
The use of mesoporous silica particles (MSPs) as delivery systems of bioactive molecules has been reinforced during recent years. The great loading capacity in their ordered pore matrix, low toxicity levels and high stability in biological conditions, especially when organic moieties are attached to the external surface [1,2,3], make them ideal supports for passive release supports. In these systems, cargo molecules are released from the pores of the particles by diffusion mechanisms [4]. Studies of active release in which the importance of inorganic support is evaluated are rarely found [32,33,34]; the release process can strongly depend on the utilized support
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