Formulation and Optimization of Colon-Specific Nanoparticles Containing A Herbal Anticancer Agent

Abstract

Colon cancer is one of the major ailments associated with increased death rate globally. This study aimed to design and optimize a nanoparticulate system for delivering sulforaphane (SFN), a dietary phytochemical with anticancer properties, to the colon. Eudragit S100, a pH-sensitive polymer was utilized to fabricate polymeric nanoparticles for delivering the drug specifically to the colon. The nanoparticles were formulated by nanoprecipitation technique and applied design of experiments (DoE) for optimization and validation. The optimized formulation was characterized for its physicochemical properties, such as particle size, shape, surface morphology, encapsulation efficiency, zeta potential, polydispersity index, in-vitro drug release, and stability at refrigerated conditions. The prepared NPs revealed spherical and smooth surfaces and value of polydispersity index, particle size, zeta potential and encapsulation efficiency were found to be 0.255, 119.46 ± 0.09 nm and -35.68 ± 0.75 mV and 64.17 ± 0.56%, respectively. The in-vitro drug release study showed that the optimized nanoparticles exhibited minimal drug release at pH 1.2 and pH 6.8, but significant and sustained drug release at pH 7.4 corresponded to the colon’s pH. The stability study indicated that the prepared formulation was stable at refrigerated condition for six months. These findings suggest that the developed delivery system could be a promising strategy for effectively encapsulating and delivering the phytochemical anticancer agent to the colon.