ABSTRACT

Curcumin, an ayurvedic natural product has many pharmacological properties including liver protection. The objective of this study was to investigate parenteral nanosuspensions of curcumin for enhancing the solubility, Cmax and liver protection and achieve sustained parenteral drug release after intravenous administration. Curcumin nanosuspensions were prepared using solvent-antisolvent precipitation method. The formulations were characterized using techniques such as powder x-ray diffractometry (XRPD), scanning electron microscopy, saturation solubility, in-vitro dissolution, pharmacokinetics and liver protection in rats. Nanosuspensions of curcumin were successfully prepared using solvent-antisolvent precipitation. The size of the particles was below 600 nm. XRPD studies indicated transformation of curcumin from crystalline to amorphous form upon fabrication into nanosuspensions. Saturation solubility and dissolution rate were higher for nanosuspensions when compared to pure drug. The optimum formulation sustained the drug release for 8 days in vivo. Cmax and liver protection of curcumin in the form of intravenous nanosuspensions was significantly higher than that of intravenously administered pure drug in the solution form. Therefore, in this study a parenteral sustained release curcumin nanosuspension formulation intended for sustained systemic release of the drug, enhanced Cmax and enhanced liver protection/targeting was successfully developed. The formulation can be successfully used in liver fibrosis/cirrhosis.