Hydrophobically modified PEGylated glycol chitosan nanoparticles: synthesis, characterisation and anticancer properties

A novel palmitoylated glycol chitosan polymer grafted with PEG (PGC-PEG) was successfully developed to form amphiphilic micelles in aqueous solution. The incorporation of hydrophobic itraconazole (ITZ) with PGC-PEG polymer produced PGC-PEG-ITZ nanoparticles in the form of homogenous polymeric micelles (PMs) and nanoemulsions (NEs). The NEs showed higher drug entrapment than that of PMs while maintaining the nanometre particle size range. Both NEs and PMs demonstrated sustained and high cumulative drug release of 93% and 89%, respectively, as well as no significant changes in drug entrapment, particle size, and size polydispersity at room temperature. The nanoparticles also exhibited stability in biological fluid by protecting the drug load from degradation. The nanoparticles exhibited anticancer activity against human breast cancer cells with a superior effect by the NEs. The PEGylated GC-based nanoparticles are a promising nanocarrier for improvement of the delivery and therapeutic activity of hydrophobic drugs.

Automated summary

A novel palmitoylated glycol chitosan polymer grafted with PEG (PGC-PEG) was developed to form amphiphilic micelles, incorporating hydrophobic itraconazole (ITZ) to produce PGC-PEG-ITZ nanoparticles in the form of homogenous polymeric micelles (PMs) and nanoemulsions (NEs). NEs showed higher drug entrapment and superior anticancer activity against human breast cancer cells compared to PMs. These PEGylated GC-based nanoparticles are promising nanocarriers for improving the delivery and therapeutic activity of hydrophobic drugs.