Self-assembling polymeric nanocarriers to target inflammatory lesions in ulcerative colitis

Abstract We have developed a self-assembling polymeric nanocarrierto deliver the potent immunosuppressive drugCyclosporine A (CsA) to inflammatory lesions in ulcerative colitis(UC) patients. Our nanocarrierhas a high drug loading capacity and efficiently targets its CsA payload to the diseased tissue after local administration. Tissue drug levels were several orders of magnitude higher in animals suffering from a trinitrobenzene-sulfonic acid (TNBS) – induced colitis, compared to healthy control animals; no drug was detectable in the plasma, underlining the localized delivery strategy. An efficient reduction in inflammation score was obtained with a CsA dose of 1 mg/mL. Therapeutic efficacy was comparable to 5- aminosalicylic acid(5-ASA), the positive control treatment in the TNBS - induced colitismodel. Repetitive treatment of healthy animals with CsA nanocarriersfor seven days was well tolerated with no alterations in colon histology.