Preparation and Characterization of pH-Sensitive Capsosomes for Oral Delivery of Therapeutic Proteins

Abstract

Oral administration of therapeutic proteins is very challenging because of gastrointestinal instability and decomposition. In this study, we developed a system for oral delivery of superoxide dismutase (SOD) as one of the therapeutic proteins. SOD-loaded capsosomes (SOD-C) were formed by the assembly of chitosan-coated solid lipid nanoparticles and SOD-loaded liposomes (SOD-L). Unlike raw SOD activity decreases to 19.41% in SGF and 13.70% in SIF, the SOD-C in SGF (89.30%) condition retained its initial catalytic activity and decreased but exhibited a three-fold higher raw SOD activity even after incubation in SIF (41.63%). TEM analysis indicated that after intestinal digestion, the residual amount of intact liposomes affected the higher catalytic activity of SOD-C compared to raw SOD and SOD-L. Based on these results, significantly higher cellular uptake of SOD-C was observed compared to raw SOD. Also, SOD-C remarkably suppressed the cellular malondialdehyde (MDA) concentration by maintaining the antioxidative capacity of SOD to remove MDA produced in the oxidative stress-induced cells, thereby contributing to a significant five-fold difference with SOD-R (p < 0.05). This delivery system can facilitate the oral application of other therapeutic proteins, improving gastrointestinal stability.

Biogenic engineered nanomaterials for enhancing bioavailability via developing nano-iron-fortified smart foods: advances, insight, and prospects of nanobionics in fortification of food

“…Despite being a vital nanocarrier, capsosomes have not been explored for oral iron delivery, but these results demonstrate the potential of smart capsosomes for the oral targeted/controlled delivery of iron. 37 Another important nanocarrier is polymersomes, similar in structure to liposomes, made up of artificial vesicles enclosing an aqueous cavity resulting from the self-assembly of amphiphilic copolymers. 38 They exhibit high physicochemical stability, an increased circulation time, cargo loading capacity, low immune response, decreased cargo degradation, specific response, tunable response, and low toxicity.…”