Biodegradable Nanoparticles for Targeted Delivery in Treatment of Ulcerative Colitis

Nanoparticles (NPs) are proposed for targeted drug delivery to the inflammation site in severe cases of inflammatory bowel disease (IBD) where state-of-the-art delivery devices fail. Meselamine (5-Aminosalicylic acid), entrapped into nanoparticles was administered either orally or rectally to male Wistar rats suffering from a preexisting experimental colitis induced by acetic acid. Meselamine, a front line drug in the treatment of ulcerative colitis, was incorporated within poly(lactic-co-glycolic acid) i.e., PLGA nanoparticles, which were administered once a day orally and rectally for five consecutive days. Clinical activity score, colon/body weight ratio, ulcer index and myeloperoxidase activity were determined to assess the inflammation. All nanoparticulate formulations proved to be efficient as compared to the free drug in suspension in mitigating the experimental colitis. The clinical activity score, myeloperoxidase activity and ulcer index decreased significantly (p<0.05*), after the oral administration of meselamine nanoparticles suspension. The free drug, meselamine, suspension does not found effective in terms of clinical activity, myeloperoxidase activity and ulcer index, as is evident from the nonsignificant decrease in clinical parameters. The meselamine nanoparticles proved their potential to retain the drug from systemic absorption as evident by a significantly reduced clinical activity, myeloperoxidase activity and ulcer index. The nanoparticles potential in reducing the inflammation was further proved by the histopathology of the resected colon from every group of animals. The use of drug loaded nanoparticles offers several advantages compared to standard therapeutic strategies such as a higher selectivity in adhesion to and enhanced drug penetration into the inflamed tissue.