Tissue fibrosis results from uncontrolled healing responses that results in excessive mesenchymal cell activation, collagen and other extracellular matrix (ECM) deposition. In the gastrointestinal (GI) tract, fibrosis leads to narrowing of the lumen and stricture formation. A drug treatment to prevent fibrosis and strictures in the GI tract would be transformational for patient care. Here, we aimed to develop a stricture treatment with following characteristics and components: (1) a small molecule with strong antifibrotic effects; (2) that is delivered locally at the site of the stricture to ensure correct lesional targeting while protecting the systemic circulation and that is (3) formulated with sustained release properties to act throughout the wound healing processes.