Development of mucoadhesive biloniosome nanoparticles for enhanced gastrointestinal absorption of cordycepin

Abstract

Cordycepin, an adenosine analogue, has displayed numerous pharmacological and therapeutic implications including enhanced apoptosis and inhibition of proliferation of cancer cells, antioxidant property and improving sexual activity. However, oral administration of cordycepin has limited practical use due to its poor bioavailability in the intestine. Here, we developed a novel hybrid nanoparticle system for effective delivery of cordycepin in the gastrointestinal tract by using the bile salt-based liposome/niosome hybrid system (designated as biloniosome). In addition, mucoadhesive chitosan biopolymer was coated on the biloniosome nanoparticles to improve the mucoadhesive properties thereby enhancing the drug efficiency. Cordycepin-encapsulated biloniosome nanoparticles were synthesized by solvent (ethanol) injection technique followed by coating with chitosan. The physicochemical characteristics of the prepared nanoparticles were investigated. Their biological activities, such as in vitro anticancer activity and in vitro permeation across the human intestinal barrier were evaluated. We successfully produced hybrid nanoparticles with ~150 nm in diameter and over 60% loading efficiency of cordycepin. The evaluation of hydrodynamic size and zeta-potential indicated that chitosan successfully modified the biloniosome. Interestingly, the hybrid nanoparticles showed potent cytotoxic activity against HT29 cell lines. Our results demonstrated that the chitosan-coated biloniosome, exhibits 3-fold increase in mucoadhesive property and improved permeation through the human intestinal barrier as compared to uncoated nanoparticles. In conclusion, the nanovation (nanotechnology + innovation) presented here is an improved version of cordycepin encapsulated in the hybrid nanoparticle system which serves as a promising candidate for oral colorectal cancer chemotherapy.