Preparation, characterization, in vitro antibacterial activity and comparative pharmacokinetic study of orally administered curcumin loaded PLGA nanoparticles

Abstract

Curcumin is used as nutraceutical. It is a yellow pigment derived from turmeric (Curcuma longa). It can be used as anti-diabetic, antibacterial, anti-tumor, anti-rheumatic, anti-viral and anti-cancer agent. But poor solubility, rapid degradation and low bioavailability have limited its use in clinical practice. The best way to overcome these problems is to load curcumin in poly lactic co- glycolic acid (PLGA) nanoparticles. Curcumin loaded PLGA nanoparticle increase the bioavailability and absorption of drug. The focus of study was to introduce a method for preparation of nanoparticle with a view to increase the aqueous solubility of curcumin, and to characterize the prepared nanoparticles and access their antibacterial activity and to modify the pharmacokinetic behavior of drug. The nanoparticles were prepared by nanoprecipitation method and it was found that the prepared nanoparticles lies within nanometer range. The evaluation of in-vitro release of curcumin loaded nanoparticle showed that formulation possess high drug loading capacity and entrapment efficiency (89.4%). A minimum inhibitory concentration of curcumin was determined for a variety of bacterial strains and was compared to that of commercially available antibiotic ampicillin. It was found that value of MIC of curcumin was much more pronounced than ampicillin against Staphylococcus aureus and Escherichia coli. The pharmacokinetics parameters were calculated by the pharmacokinetic APO software. The results of comparative pharmacokinetics of these nanoparticles in comparison to the pure standard showed that AUC of Cur NP was 95.38 h.mg/L much greater than pure curcumin (13.6 h.mg/L). The value of Cmax for Cur NP was also increased to 12.50µg/ml as compared to 1.50µg/ml of curcumin alone. Similarly, the value of Tmax was also increased. The increase in Cmax and Tmax values after administering curcumin loaded PLGA nanoparticles can be explained by controlled and sustained release of curcumin from PLGA nanosystem.