Preparation, characterization, and in vitro drug release behavior of thiolated alginate nanoparticles loaded budesonide as a potential drug delivery system toward inflammatory bowel diseases

Abstract

For site-specific drug delivery in inflammatory bowel disease, reducible sodium alginate nanoparticles cross-linked with disulfide linkage were developed. Nanoparticles were synthesized in deionized water through self-assembly of amphiphilic thiolated sodium alginate Alg-Cys and subsequently produced cross-linking of disulfide bonds. TEM image showed a spherical core-shell configuration with a size of about 430 nm for the nanoparticles. Dynamic light scattering (DLS) showed high stability, narrow size distribution, and pH-dependent swelling transition for the nanoparticles. Cytotoxicity study showed that there was no evident cell inhibition among the nanoparticles. Also, the size of the nanoparticles increased in 10 mM glutathione (GSH) solution due to the cleavage of disulfides within their network structures. Compared to that in GSH-free buffer, there was a remarkable increase in drug release in pH 7.4 buffer with GSH from drug-loaded nanoparticles, indicating that the nanoparticles could be used for colon-specific drug delivery.

Keywords:

• Sodium alginate derivative
• disulfide cross-linked nanoparticles
• pH-sensitivity
• reduction-response
• colon-specific drug delivery

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This study is supported by the Key R&D project of Shandong Province (2019GSF107031).