Nanosuspension encapsulated chitosan-pectin microbeads as a novel delivery platform for enhancing oral bioavailability

Abstract

The current study aimed to overcome the poor solubility and colon-specific delivery of curcumin (CUR) by formulating a curcumin nanosuspension (CUR-NS) using the antisolvent precipitation method. Freeze-dried CUR-NS was encapsulated into microbeads (CUR-NS-MB) by the ionotropic gelation method using zinc chloride (as a cross-linking agent) with the help of rate-controlling polymers, pectin, and chitosan. Furthermore, cellulose acetate phthalate (CAP) is incorporated as an enteric polymer to protect against acidic medium degradation. Particle size, surface morphology, interaction studies, and entrapment studies were performed to optimize CUR-NSs. Nanosuspensions stabilized with hydroxypropyl methylcellulose (HPMC E-15; 1 % w/v) showed an average particle size of 193.5 ± 4.31 nm and a polydispersity index (PDI) of 0.261 ± 0.020. The optimized microbeads (CUR-NS-MB) showed 89.45 ± 3.11 % entrapment efficiency with a drug loading of 14.54 ± 1.02 %. The optimized formulation (CUR-NS-MB) showed colon-specific in vitro drug release bypassing acid pH degradation. In animal studies, a 2.5-fold increase in Cmax and a 4.4-fold increase in AUC048h were observed with CUR-NS-MB, which was more significant than that of plain CUR. Therefore, the developed CUR-NS-MB has the potential to be used as a colon-specific delivery system.