Fabrication of Catechin Loaded Bioactive Nanoparticulate Formulation to Improve Cellular Uptake and Gastrointestinal Digestion by In-Vitro Intestinal Co-culture Method

Nanoparticles, specifically polymeric nanoparticles, have been investigated to utilize as drug carriers in recent research. Oral ingestion has been considered a prominent exposure route to nano-based carriers. Hence, the uptake of bioactive NPs by epithelial cells and their interaction with digestive enzymes in the gastrointestinal tract (GIT) would be an effective therapeutic approach to many diseases. The present report aimed to investigate the catechins (CAT) and gelatin (GEL) were blended to fabricate self-assembled gelatin nanoparticles (CAT@GEL NPs) for their improved cellular uptake ability by cell co-culture method, which was developed by Caco-2/HT-29 co-cultured cell prototype. The prepared GEL NPs have a particle size of about ≈ 160 nm and a polydispersity index (PDI) is 0.258, which is suitable for effective cellular uptake. The prepared GEL NPs have prominently improved encapsulation efficiency (EE %) and in-vitro drug release ability about 90.40% and 89.62%, respectively. Importantly, the efficiency of the cellular intake and nanoparticle absorption activity in monoculture was determined by performing flow cytometry and fluorescence spectroscopic analyses on the in-vitro co-culture model. The outcome of the study demonstrated that prepared nanoformulation revealed an outstanding absorption ability, cellular uptake, and suitable cell compatibility (> 90% survival rate). The flow cytometry analysis demonstrated that digested CAT@GEL NPs were significantly higher about 93.98%, confirming that particles are stable without disturbing cell survival rate (%). This study suggests that the developed CAT@GEL nanoformulation could be an effective nanocarrier for the bioactive substances to gastrointestinal oral digestion applications.