Chitosan-functionalized poly(lactide-co-glycolide) nanoparticles: breaking through the brain’s tight security gateway

Despite the development of several progressive treatments, many effective anticancer drugs have failed in clinical examinations due to the inability to penetrate across the blood–brain barrier. For this reason, the local and controlled delivery of anticancer drugs using biodegradable polymeric nanoparticles is attracting increasing attention as a viable therapy for treating brain tumors. In the present study, poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) with high emulsifying effects were prepared in conjunction with vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (TGPS) and chitosan, which imparted the desired surface morphology and particle size. The particle sizes, the surface morphology and the phase composition were correlated with the loaded amount of chitosan and operating pH. The laboratory cytotoxicity of the particles was investigated using the PC12 cell line. An increase in the chitosan content decreased the particle sizes of the NPs in a semilinear pattern and increased the potential therapeutic effects as indicated by high cell viability. These chitosan surface-modified PLGA NPs could be used for local drug delivery, thereby greatly expanding the spectrum of drugs available for the treatment of brain tumors.