Modulation of Pharmaceutical and Pharmacokinetic Attributes of Curcumin Encapsulated in Chitosan Using Spray Drying Technique

Abstract

The present study is designed to formulate and characterize Curcumin (CUR) loaded Chitosan nanoparticles by ionic cross linking using TPP by employing spray drying technique to enhance the aqueous solubility, hence oral bio availability of Curcumin. Curcumin is very sparingly aqueous soluble, unstable in alkaline conditions and gets eliminated faster, resulting in poor bio availability. Curcumin in alcohol was used as drug loading solution. Tween 80 served as nano emulsifier and stabilizer. EE of optimized formulation F6 was found to be 98.5 ± 0.16 %. This formulation has an average particle size of 25 ± 0.1 nm. The Zeta potential of the formulation is -200 mV.  FTIR results revealed the absence of characteristic CUR peak in Curcumin Chitosan nanoparticles implying the successful incorporation of CUR into the Chitosan matrix. DSC thermograms witnessed that the crystalline form of CUR is transformed into amorphous form, having better dissolution and stability profile. SEM imaging of the nanosuspension formulation showed the topological features of the prepared nanoparticles. The nanoparticles were more spherical, discrete and homogeneous. % cumulative drug release studies exhibited very less drug release in Simulated Gastric Fluid (SGF- 3.97 %) and Simulated Intestinal Fluid (SIF - 4.2 %) exhibiting sustained release. Pure Curcumin showed burst release of approximately 95 % in 2 h in SGF with a decline in the concentration after 2 h in SIF due to significantly increased degradation in the alkaline conditions. The oral bioavailability (AUC) of Curcumin in female wistar rats increased 11-times following ingestion of Curcumin nanosuspension in comparison with conventional Curcumin suspension. The maximum concentration C_max of 1034 ± 96 ng / ml for nanosuspension and 94 ± 9.4 ng / ml for Curcumin suspension and was observed at t_max of 2 h for both nanosuspension and suspension.