Toxicity and Pharmacokinetic Studies of Aerosolized Clinical Grade Azacitidine.

ABSTRACT:

Background

Azacitidine as an effective epigenetic therapeutic agent has not been used as an aerosol form to treat lung cancer patients. We aerosolized clinical grade azacitidine (Aza), optimized the formulation, and studied its pharmacokinetics and toxicity in mice.

Methods

Extrusion-precipitation method and DNA methyltransferase inhibition rate were used to measure the aerodynamic size and aerosolized Aza activity. In the single dose pharmacokinetic study, Aza concentrations in peripheral blood and lungs were measured by LC-MS method. In the multiple-dose toxicity studies, histo-pathological evaluation was used to determine the organ and bone marrow toxicities.

Results

In pharmacokinetic study, aerosolized Aza was found to deposit mainly into the lung with very littl

SUBMITTER: Qiu X 

PROVIDER: S-EPMC6050589 | biostudies-literature | 2016 May

REPOSITORIES: biostudies-literature