Journal
JOURNAL OF CONTROLLED RELEASE
Volume 281, Issue -, Pages 58-69Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jconrel.2018.05.007
Keywords
Colon drug delivery systems; Colon targeting; Inflammatory bowel disease; Mesoporous silica microparticles; Gated materials; Smart drug delivery
Funding
- Spanish Government [MAT2015-64139-C4-1-R, AGL2015-70235-C2-2-R]
- Generalitat Valenciana [PROMETEOII/2014/047]
- Spanish MEC
- Electron Microscopy Service at the Universitat Politecnica de Valencia
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Magnetic mesoporous silica microparticles were loaded with safranin O (S1) and with hydrocortisone (S2) and the outer surface functionalized with a bulky azo derivative bearing urea moieties. Aqueous suspensions of both solids at pH 7.4 showed negligible payload release whereas a marked delivery was observed in the presence of sodium dithionite due to the rupture of the azo bonds. Besides, a moderate cargo release was observed at acidic pH due to the hydrolysis of the urea bonds that linked the azo derivative onto the external surface of the inorganic scaffolds. In vitro digestion models showed that S1 and S2 microparticles could be used for the controlled release of payload in the reducing colon environment (in which azoreductase enzymes are present). On the other hand, in vivo pharmacokinetic studies in rats showed that safranine O release from S1 microparticles was concentrated in colon. The performance of S2 microparticles for the treatment of colitis in rats (induced by oral administration of a 2,4,6-trinitrobenzenesulfonic acid solution) was tested. The controlled release of hydrocortisone from S2 in the colon of injured rats induced marked reduction in colon/body weight ratio and in clinical activity score. Also, histological studies showed a marked decrease in inflammation followed by intensive regeneration and almost normal mucosal structure of the individuals treated with S2. Besides, the use of a magnetic belt increased the therapeutic performances of S2 due to an enhanced retention time of the particles in the colon.
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