Abstract:

BACKGROUND: Triamcinolone acetonide acetate (TAA) has strong anti-inflammatory effects as a long-acting corticosteroid. TAA has shown good results in the treatment of intraocular diseases in recent years, however, it also brings some side effects, and needs multiple injections to prevent disease recurring. Grafted chitosan, a copolymer, can generate nanoparticles in aqueous solution, and can be used as a drug carrier for extending the duration of drugs, reducing its side effects and improving its bioavailability.
OBJECTIVE: To synthesize the amphiphilic chitosan derivative containing deoxycholic acid groups and to use it as a carrier to encapsulate TAA, to prepare drug-loading nanoparticles of sustained-release function, and to study the load and performance of sustained-release TAA.
METHODS: The amphiphilic chitosan derivative was synthesized through amidation reaction. Morphology and particle size of nanoparticles were observed by transmission electron microscopy, Zeta potential of nanoparticles was measured by Zeta potential analyzer. The entrapment efficiency, drug loading and in vitro drug release properties of TAA-loaded chitosan-deoxycholic acid nanoparticles were determined by in vitro release assay.
RESULTS AND CONCLUSION: The synthesized amphiphilic chitosan derivatives containing TAA could form drug-loaded nanoparticles, of which drug loading content was 82%. With the increasing drug loading content, the particle sizes of drug-loaded nanoparticles increased, while their Zeta potential values decreased. The result of in vitro release assay indicated that the drug-loaded nanoparticles constantly released TAA in a sustained manner within 72 hours. The drug-loaded nanoparticles based on the amphiphilic chitosan derivative exhibited a sustained-release behavior and is potential to increase the therapeutic effect of TAA.