Trehalosomes: A colon targeting trehalose-based green nanocarriers for the maintenance of remission in inflammatory bowel diseases.

Abstract

The use of non-steroidal anti-inflammatory drugs (NSAIDs) in inflammatory bowel diseases (IBDs) are contradictory between their beneficial effect in alleviating inflammation, and injurious outcome in aggravating the symptoms of colitis. The study aimed to formulate trehalosomes (THs); innovative green trehalose based nanocarriers, to alleviate the inflammation symptoms that might be provoked by NSAIDs in IBDs; as trehalose was proved to lighten the inflammation and the oxidative stress response, besides its resistance to acidic conditions which rises its potentiality as a means for colon targeting. THs were fabricated using L-α-phosphatidylcholine (PL), trehalose and transcutol, in a single step circumventing the incorporation of any organic solvent and loaded with Tenoxicam (TXM) as a model anti-inflammatory medication. A full 23 factorial design, using Design-Expert® software, was established to optimize formulation variables. The optimized formulation composed of trehalose:PL at a weight ratio of 1:1, 377.72 mg transcutol and sonicated for 4 min, possessed a spherical shape with a size of 268.61 nm and EE% of 97.83% and released 70.22 % of its drug content over 24 h. The supreme protective action of TXM loaded THs compared to TXM suspension and drug-free THs was revealed by the suppression of the inflammatory biomarkers and improved histopathology of the colonic tissue in male New Zealand rabbits. IL-1ß, IL-6, and TNF-alpha levels were notably dampened with TXM loaded THs, and oxidative stress markers, measured as GSH and MDA, were significantly reduced. The study indicates the successful role of green THs in colon targeting and its anti-inflammatory characteristics in protecting against possible NSAIDs-driven exacerbation of colitis.