Abstract: AIM: To evaluate the pharmacokinetics and pharmacodynamics of acetylcysteine nanospheres. METHODS: Two groups of NAC nanoparticles and free drug groups were injected into mouse tail vein. NAC was detected in plasma and different organs at different time. Chronic liver injury model was established by subcutaneous injection of carbon tetrachloride in rats. Different doses of NAC nanoparticles were administrated.Treatment of NAC nanospheres efficacy was evaluated on serum markers and indicators of liver tissue.RESULTS: Acetylcysteine nanospheres changed the distribution of drugs in the body.The results showed that drug concentration significantly increased in the liver tissue,half-life increased obviously. Pharmacodynamics result showed that the nanospheres can reduce serum markers and improve hepatic antioxidant function.Liver biopsy showed that the nanosphere treatment groups ameliorated hepatic steatosis, inflammatory and necrosis.CONCLUSION: The acetylcysteine nanosphere had obvious liver targeting, improving therapy for liver injure. Nanospheres are an ideal new formulations for acetylcysteine.

Key words: Acetylcysteine, Nanospheres, Pharmacokinetics, Pharmacodynamics