PEGylated Chitosan Nanoparticles as Oral Delivery Vehicles for Protein Drugs

• Published in: Russian journal of general chemistry 2023-12, Vol.93 (Suppl 4), p.S965-S977
• Main Authors: Liang, F., Zen, W. H., Huang, S., Liang, J. Q., Deng, X. Y.
• Format: Article
• Language: English
• Subjects: Albumin; Analysis; Biocompatibility; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Chitosan; Drugs; Nanoparticles; Polyelectrolytes; Polyethylene glycol; Polyols; Proteins; Serum albumin; Zeta potential
• ISSN: 1070-3632; 1608-3350
• DOI: 10.1134/S1070363223170139

PEGylated chitosan nanoparticles as oral delivery system for protein drugs were constructed by polyelectrolyte composite method. BSA-loaded nanoparticles were prepared by optimizing the conditions using bovine serum albumin (BSA) as protein drug model. The average particle size was 205.74±1.96 nm with PDI of 0.090 and the zeta potential was –36.76±9.4 mV, when the molar ratio was 0.20, the concentration was 0.6 mg/mL and polyethylene glycol grafting degree was 16%. The system showed high loading capacity and encapsulation efficiency for BSA which was up to 22.8±5.8% and 82.3±6.2% respectively. The cumulative release rate decreased with increasing initial amount and BSA was released slower in strong acid environment, such as simulated gastric pH 1.4, with cumulative release rate of 45% after 180 h, indicating that the nanoparticles can protect BSA from degradation. The Korsmeyer-Peppas and first-order kinetic models were used to fit well, dominated by the diffusion of BSA adsorbed on the surface, the dissolution of nanoparticles and the diffusion of BSA from the nanoparticles. The results suggested that PEGylated chitosan nanoparticles show excellent biocompatibility, with the potential as promising nanocarriers for oral delivery of protein drugs.