Abstract A successful oral protein nanocarrier needs to exhibit the following characteristics: stability in the gastrointestinal (GI) tract, drug release at specific site, overcoming high mucus turnover, mucoadhesive properties and… Click to show full abstract
Abstract A successful oral protein nanocarrier needs to exhibit the following characteristics: stability in the gastrointestinal (GI) tract, drug release at specific site, overcoming high mucus turnover, mucoadhesive properties and enhanced epithelial absorption. The purpose of this research was to examine the potential of complex coacervation technique for manufacturing of insulin-loaded chitosan-Dz13Scr nanoparticles. The nanoparticles were characterized for size, polydispersity index, entrapment efficiency, drug loading capacity, zeta potential, morphology, stability and consistency of physiochemical properties. Additionally, toxicity, GI permeation, endocytosis absorption pathway, and glucose consumption capacity, were examined in cellular assays. The optimized formulation variables [0.5% of natural polymer (chitosan) and 10 μg of an oligonucleotide (Dz13Scr)] could control the physiochemical properties of nanoparticles. The complex coacervation technique used in the study could tighten the size uniformity and generate nanoparticles with high encapsulation efficiency (88%). In vitro drug release model also confirmed that the nanoparticles could withstand the acidic environment with only 13% of insulin released. The formulation could maintain its stability upon storage, promote the permeation of encapsulated insulin via paracellular absorption and endocytic pathway, and induced glucose uptake in the skeletal muscle cells. Therefore, this insulin-loaded chitosan-Dz13Scr nanoparticle is a potential drug delivery system for management of diabetes mellitus.
               
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