Abstract
The present investigation aimed to develop a tumor-targeting drug delivery system for paclitaxel (PTX). The hydrophobic deoxycholic acid (DA) and active targeting ligand folic acid (FA) were used to modify water-soluble chitosan (CS). As an amphiphilic polymer, the conjugate FA-CS-DA was synthesized and characterized by Proton nuclear magnetic resonance (1H-NMR) and Fourier-transform infrared spectroscopy (FTIR) analysis. The degree of substitutions of DA and FA were calculated as 15.8% and 8.0%, respectively. In aqueous medium, the conjugate could self-assemble into micelles with the critical micelle concentration of 6.6 × 10−3 mg/mL. Under a transmission electron microscope (TEM), the PTX-loaded micelles exhibited a spherical shape. The particle size determined by dynamic light scattering was 126 nm, and the zeta potential was +19.3 mV. The drug loading efficiency and entrapment efficiency were 9.1% and 81.2%, respectively. X-Ray Diffraction (XRD) analysis showed that the PTX was encapsulated in the micelles in a molecular or amorphous state. In vitro and in vivo antitumor evaluations demonstrated the excellent antitumor activity of PTX-loaded micelles. It was suggested that FA-CS-DA was a safe and effective carrier for the intravenous delivery of paclitaxel.
Highlights
Paclitaxel (PTX) is an important clinical chemotherapeutic drug that exhibits strong antitumour activity against a variety of cancer types
The internal core provides a storeroom for poorly water-soluble drugs, and the outer shell allows the retention of the stability of micelles in aqueous medium and provides the opportunity to target the delivery of antitumor drugs to the tumor by further modification [8,9]
The synthesis of folic acid (FA)-CS-Deoxycholic acid (DA) was performed via the amide bond formation between the amino groups of CS and the carboxyl groups of DA and FA
Summary
Paclitaxel (PTX) is an important clinical chemotherapeutic drug that exhibits strong antitumour activity against a variety of cancer types. Polymeric micelles have attracted growing interest due to their attractive characteristics, such as their excellent solubilization ability, small size, high stability, prolonged circulation time, low toxicity, ability to evade scavenging by the mononuclear phagocyte system (MPS), high biocompatibility and efficient accumulation in tumor tissues via an enhanced permeability and retention (EPR) effect [6,7]. The micelles have a unique core–shell structure with hydrophobic segments as the internal core and hydrophilic segments as the outer shell. The internal core provides a storeroom for poorly water-soluble drugs, and the outer shell allows the retention of the stability of micelles in aqueous medium and provides the opportunity to target the delivery of antitumor drugs to the tumor by further modification [8,9]
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