Abstract
Amphiphilic polymer of α-tocopherol succinate modified glycol chitosan (TS-GC) was successfully constructed by conjugating α-tocopherol succinate to the skeleton of glycol chitosan and characterized by Fourier-transform infrared (FT-IR) and proton nuclear magnetic resonance (1H-NMR). In aqueous milieu, the conjugates self-assembled to micelles with the critical aggregation concentration of 7.2 × 10−3 mg/mL. Transmission electron microscope (TEM) observation and dynamic light scattering (DLS) measurements were carried out to determine the physicochemical properties of the micelles. The results revealed that paclitaxel (PTX)-loaded TS-GC micelles were spherical in shape. Moreover, the PTX-loaded micelles showed increased particle sizes (35 nm vs. 142 nm) and a little reduced zeta potential (+19 mV vs. +16 mV) compared with blank micelles. The X-ray diffraction (XRD) spectra demonstrated that PTX existed inside the micelles in amorphous or molecular state. In vitro and in vivo tests showed that the PTX-loaded TS-GC micelles had advantages over the Cremophor EL-based formulation in terms of low toxicity level and increased dose, which suggested the potential of the polymer as carriers for PTX to improve their delivery properties.
Highlights
Paclitaxel (PTX), as a powerful anti-tumor drug, has been extensively used in the clinical treatment of several solid tumors, such as refractory ovarian cancer, metastasis breast cancer, non-small cell lung cancer, Acquired Immune Deficiency Syndrome-related Kaposi’s sarcoma and other cancers [1,2]
The polymer tocopherol succinate modified glycol chitosan (TS-glycol chitosan (GC)) was synthesized via the coupling reaction between carboxyl group of TS and amine group of GC in the presence of water-soluble 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC)
The findings suggested that PTX-loaded TS-GC micelles could be used as a potential PTX carrier
Summary
Paclitaxel (PTX), as a powerful anti-tumor drug, has been extensively used in the clinical treatment of several solid tumors, such as refractory ovarian cancer, metastasis breast cancer, non-small cell lung cancer, Acquired Immune Deficiency Syndrome-related Kaposi’s sarcoma and other cancers [1,2]. Several studies reported that Cremophor EL induced serious side effects such as hypersensitivity, nephrotoxicity, neurotoxicity, and the extraction of plasticizer from the infusion tubes [3] In light of these drawbacks, a number of alternative preparations were investigated, including liposomes, nanocrystals, micelles, cyclodextrin complexes and PTX conjugates [4,5,6,7,8]. Among these formulations, polymeric micelles have been proven as promising drug delivery systems for PTX administration [9,10], because of their attractive characteristics, such as biocompatibility, high drug-loading content, small size (
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