DACLATASVIR DIHYDROCHLORIDE MICROSPHERES, PROCESS PARAMETERS FOR ENHANCED PERMEABILITY AND LIVER TARGETING

Objectives: Daclatasavir dihydrochloride (DCLD) is used to treat hepatitis C. DCLD can be used to patients with all stages of compensated liver disease including cirrhosis. The aim of the present study was to develop DCLD microspheres to improve the permeation and maximum accumulation in the liver and in vitro evaluation.
Methods: DCLD microspheres were prepared with chitosan polymer using emulsion crosslinking technique. Twelve formulations were prepared, that is, F1-F12. The microspheres were evaluated for morphology, particle size, encapsulation efficiency, % yield, and permeability. FTIR studies were conducted on optimized formulation to check the drug-excipient compatibility.
Results: The particle size of microspheres was in the range of 11.50±0.08 μm to 98.50±0.05 μm. Encapsulation efficiency of the formulations was observed in the range 47.8–69.2%. The ex vivo permeation studies revealed that 83.3±0.1% of drug was diffused from microspheres in 60 min, whereas from pure drug 49±0.7% of drug was diffused in 60 min.
Conclusion: DCLD microspheres were shown good permeability when compared to pure drug which will improve the absorption.