Poly(Lactic-co-Glycolic Acid Nanoparticles Loaded with Docetaxel and Coated with Chitosan, Carboxymethyl Chitosan, or Glycol Chitosan.

Abstract

Docetaxel (DTX) is a chemotherapeutic drug that has high toxicity and low bioavailability. To solve these problems, PLGA nanoparticles (NPs) were loaded with DTX and coated with mucoadhesive polymers; chitosan (CS), carboxymethyl chitosan (CMCS), or glycol chitosan(GCS). The NPs were characterized for size, charge, and polydispersity. The particles were explored using SEM, FTIR, DSC, and XRD. In vitro studies were performed to evaluate the mucoadhesive properties of the NPs and the drug release. The results validated the successful formation of spherical and monodispersed DTX NPs. The coated NPs exhibited highly positive charges, reaching +44.30±0.21 mV, whereas the uncoated NPs were almost neutral. The formulations demonstrated excellent encapsulation efficiency (>98%) and loading capacity (>45%). All polymers used in the coating process enhanced the mucoadhesive properties of PLGA NPs and sustained DTX release. Both the mucoadhesiveness and release were related to the used coating polymer and its concentration. The formulations were stable for up to three months in the refrigerator. In conclusion, loading DTX in PLGA NPs and coating them with CS, CMCS, or GCS provides a promising strategy to increase the NPs' residence time on mucosal surfaces, which is expected to decrease the required dose of DTX and reduce its side effects.