Silibinin is a flavonolignan that is well established for its robust antiviral activity against HCV infection and has undergone several clinical trials for the management of hepatitis C.
Despite its potency, silibinin suffers from poor solubility and bioavailability, restricting its clinical use.
To overcome this limitation, Dr Ching-Hsuan Liu and colleagues prepared silibinin nanoparticles using a nanoemulsification technique, and physicochemically characterized these.
Infectious HCV culture systems were used to evaluate the influence of silibinin nanoparticles on the virus life cycle and examine their antioxidant activity against HCV-induced oxidative stress.
|Silibinin nanoparticles exerted an antioxidant effect via their free radical scavenging function|
The safety profiles of silibinin nanoparticles, in vivo pharmacokinetic studies and antiviral activity against infection of primary human hepatocytes were also assessed.
The research team found that silibinin nanoparticles consisted of nanoscale spherical particles encapsulating amorphous silibinin at more than 97% efficiency and increasing the compound's solubility by more than 75%.
Treatment with silibinin nanoparticles efficiently restricted HCV cell-to-cell transmission, suggesting that they retained silibinin's robust anti-HCV activity.
In addition, silibinin nanoparticles exerted an antioxidant effect via their free radical scavenging function.
Oral administration of silibinin nanoparticles in rodents produced no apparent in vivo toxicity, and pharmacokinetic studies revealed an enhanced serum level and superior biodistribution to the liver compared with non-modified silibinin.
The team found that silibinin nanoparticles efficiently reduced HCV infection of primary human hepatocytes.
Dr Liu's team comments, "Due to silibinin nanoparticles's enhanced bioavailability, effective anti-HCV activity and an overall hepatoprotective effect, we suggest that silibinin nanoparticles may be a cost-effective anti-HCV agent that merits further evaluation for the treatment of hepatitis C."