The clinical application of paclitaxel (PTX) is limited due to its low solubility and severe side effects. In this study, an amphiphilic graft copolymer based on mPEG, deoxycholic acid and N-acetyl-L-cysteine modified hyaluronic acid (mPEG-HA(DCA)-NAC) was synthesized and used as a redox-sensitive nano-sized drug delivery system. The polymer was characterized by Fourier transform infrared (FT-IR) and Proton nuclear magnetic resonance (¹H NMR) analysis. As an amphiphilic polymer, mPEG-HA(DCA)-NAC could self-assemble into micelles in aqueous milieu and encapsulate PTX in the hydrophobic core with high drug loading of 15.6% and high encapsulation efficiency of 73.8%. The PTX-loaded micelles had an average size of 147 nm and zeta potential of −38.3 mV. Physicochemical properties of the micelles were measured by TEM and XRD analysis. XRD analysis confirmed the successful encapsulation of PTX in an amorphous state. In vitro drug release study demonstrated the redox-sensitivity of the micelles. In vitro and in vivo antitumor efficacy study indicated that the PTX-loaded mPEG-HA(DCA)-NAC micelles had excellent antitumor effect but with low toxicity to the body. It can be concluded that the mPEG-HA(DCA)-NAC micellar system represents a promising nanocarrier for delivery of PTX.

紫杉醇（PTX）的临床应用由于其低溶解度和严重的副作用而受到限制。在这项研究中，基于mPEG，脱氧胆酸和N-乙酰-L-半胱氨酸修饰的透明质酸（mPEG-HA（DCA）-NAC）的两亲性接枝共聚物被合成并用作氧化还原敏感的纳米级药物递送系统。该聚合物的特征在于傅立叶红外光谱（FT-IR）和质子核磁共振（¹1 H NMR）分析。作为一种两亲聚合物，mPEG-HA（DCA）-NAC可以在水性环境中自组装成胶束，将PTX包埋在疏水核中，载药量高达15.6％，包封率高达73.8％。载有PTX的胶束的平均大小为147 nm，ζ电位为-38.3 mV。通过TEM和XRD分析来测量胶束的理化性质。XRD分析证实了无定形状态下PTX的成功封装。体外药物释放研究证明了胶束的氧化还原敏感性。体外和体内抗肿瘤功效研究表明，载有PTX的mPEG-HA（DCA）-NAC胶束具有优异的抗肿瘤作用，但对机体的毒性低。可以得出结论，mPEG-HA（DCA）-NAC胶束系统代表了有前途的纳米载体用于PTX的交付。