Chitosan-TPP nanoparticle as a release system of antisense oligonucleotide in the oral environment.

Abstract Antisense oligonucleotide loaded chitosan nanoparticles were prepared and the release of oligonucleotide from chitosan-TPP/oligonucleotide nanoparticles was investigated. Morphological property, zeta potential and particle size of the prepared chitosan/oligonucleotide nanoparticles were investigated using Field Emission-Scanning Electron Microscope (FE-SEM) and particle size analyzer. The interaction between chitosan and oligonucleotide was confirmed by using capillary zone electrophoresis (CZE), and the released oligonucleotides were determined by spectrophotometric method. Oligonucleotides formed the complexes with chitosan with a unique morphological property. The release of oligonucleotides from nanoparticles was dependent on loading methods and pH conditions. Chitosan/oligomer-TPP nanoparticles, which was prepared by adding TPP after the formation of chitosan/oligonucleotide complex, showed the lowest release percent of oligonucleotides with 41.3% at pH 7.0 among the loading methods. The percent release of oligonucleotide from oligonucleotide loaded chitosan nanoparticle at pH 10 was higher than the one in acidic condition (pH 5.0). The released oligonucleotides from chitosan/oligonucleotide nanoparticles were stable enough for 12 h under the 20% saliva solution. Our results suggest that the sustained release of oligonucleotide from chitosan nanoparticles may be suitable for the local therapeutic application in periodontal diseases.