Novel folate-targeted paclitaxel nanoparticles for tumor targeting: preparation, characterization, and efficacy

Abstract

To improve tumor targeting of anticancer drugs has recently been the focus of a great deal of research. In this study, firstly, a cholesterol–PEG₁₀₀₀–NH₂ (Chol–PEG₁₀₀₀–NH₂) -conjugated folate (FA) was synthesized, and then paclitaxel (PTX) was loaded to prepare nanoparticles using solvent precipitation combined with a high pressure homogenization method, followed by characterization by dynamic light scattering (DLS), transmission electron microscopy (TEM) and differential scanning calorimetry (DSC). Secondly, in vitro cytotoxicity was also studied, which showed that PTX/Chol–PEG₁₀₀₀–FA nanoparticles exhibited comparable cytotoxicity against 4T1 compared with Taxol. Thirdly, the targeting ability of PTX/Chol–PEG₁₀₀₀–FA nanoparticles was demonstrated by ex vivo and in vivo anti-tumor activity against 4T1 cells. Ex vivo optical imaging revealed that Dir loaded PTX/Chol–PEG₁₀₀₀–FA nanoparticles were distributed more in tumors than PTX/mPEG₁₀₀₀–Chol nanoparticles and Taxol at 30 mg kg⁻¹. An in vivo imaging study also revealed that the target function of PTX/Chol–PEG₁₀₀₀–FA nanoparticles was better than PTX/mPEG₁₀₀₀–Chol nanoparticles. In other words, the constructed PTX/nanoparticles in this study can successfully target tumors and exhibit good antitumor activity, which can be considered to be a promising targeted delivery system for breast therapy.