Abstract
This study is aimed at the preparation and evaluation of atorvastatin (AN)-loaded chitosan (CS) nanoparticles to achieve improved bioavailability of atorvastatin as its bioavailability is very poor. Chitosan is a popular choice in the application as a drug delivery carrier due to its biocompatibility, chemical versatility, aqueous solubility and low cost. Hence, a total of nine formulations (AN1–AN9) were prepared to study the effects of CS:tripolyphosphate (TPP) ratio and the amount of drug. The best formulation was selected by calculating the overall desirability (OD) factor. Among all, AN9 was found to possess the maximum percentage yield, loading efficiency and percentage (%) drug release compared to other formulations due to the incorporation of more amount of polymer compared to other formulations. SEM microphotographs and zeta-sizer reports indicated that atorvastatin-loaded chitosan nanoparticles were in the nanometric range and were spherical, discrete and uniform in size. The selected polymer chitosan was found to possess good compatibility with atorvastatin, without any mutual interaction, based on the results of DSC and FTIR analyses. The nanoparticles were found to have good flow properties. The in vivo results proved that the best formulation has shown significant difference in the reduction of triglycerides (TG), total cholesterol (TC) and no significant change in high density lipids (HDL) cholesterol levels in blood when compared with the marketed formulation. Better regenerative changes were observed during histopathological evaluation of liver in a group treated with atorvastatin nanoparticles than those of other groups, that confirmed the improved hypolipidemic action. Thus, from all the above observations, it was concluded that AN9 formulation has shown the highest in vitro drug release and loading efficiency than other formulations, which might be due to increased entrapment of drug and the surface area through decreased particle size which further confirmed the improved in vitro bioavailability and in vivo performance than those of marketed atorvastatin tablet. This study strongly suggests the use of chitosan nanoparticles as drug delivery system to improve the bioavailability of atorvastatin.
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