Tumor-targeting micelles based on folic acid and alpha-tocopherol succinate conjugated hyaluronic acid for paclitaxel delivery

摘要

Tumor-targeting micelles for the delivery of paclitaxel (PTX) were developed based on folic acid and alpha-tocopherol succinate conjugated hyaluronic acid (FA-HA-TOS). The conjugate FA-HA-TOS was synthesized by an esterification reaction and was characterized by proton nuclear magnetic resonance (H-1 NMR) and Fourier transform infrared (FT-IR) analysis. The conjugate self-assembles into nanosized micelles in aqueous medium with a critical micellar concentration (CMC) of 1.12 x 10(-2) mg/mL. The FA-HA-TOS micelles demonstrated high drug loading and entrapment efficiency for PTX, with respective values of 21.37% and 90.48%. The physicochemical properties of the micelles were measured by DIS, TEM and XRD. Moreover, in vitro and in vivo evaluations were performed to demonstrate the superior antitumor activity of the PTX-loaded micelles. It was suggested that the FA-HA-TOS micelle system represents a promising nanocarrier for targeted delivery of PTX.