Optimization and characterization of hepatoprotective andrographolide microspheres in the necrotic rat model

Abstract

This study aimed to develop controlled release drug delivery of oral andrographolide encapsulated in microspheres, targeted against degenerative hepatic disorder. Ionotropic gelation technique was used to prepare andrographolide loaded Chitosan/Na-Alginate microspheres. The final drug formulation was optimized based on the statistical modeling used in the study. SEM, DSC, and XRD studies revealed a spherical formulation with a smooth surface morphology and increased thermal stability. Mean particle size, drug entrapment efficiency, and cumulative drug release from the optimized formulation were observed to be 37.46 ± 2.3 μm, 88.13 ± 3.6%, and 93.04 ± 5.1%, respectively, and manifesting steady-state release profile up to 12 h with zero-order kinetics and Non-Fickian diffusional release. In-vivo studies show a remarkable effect in elevated liver enzyme levels, and hepatocellular necrosis in CCl4 intoxicated Wistar Rats. Findings from this study suggest that andrographolide microspheres could be a potential delivery system with high oral bioavailability and sustained drug release profile against hepatic necrosis.