Pegylated multifunctional pH-responsive targeted polymeric micelles for ovarian cancer therapy: synthesis, characterization and pharmacokinetic study

Abstract

DTX-loaded folate targeted micelles (DTX/FA-PEG-HEP-CA-TOC) were prepared using a dialysis method and the impact of various processing variables were evaluated on micelle properties. In vitro cytotoxicity and in vivo pharmacokinetics of the optimized formulation were evaluated.DTX/FA-PEG-HEP-CA-TOC exhibited average particle size of 90–185 nm with high entrapment efficiency (53–93%) and pH-dependent drug release behavior. DTX/FA-PEG-HEP-CA-TOC micelles exhibited higher toxicity against SKOV3 cells than DTX/HEP-CA-TOC micelles and free DTX. Significant increase in the T1/2 β, AUC and MRT and decrease in Vd as well as CL values was observed in DTX/FA-PEG-HEP-CA-TOC micelle treated group compared to free DTX treated group.