Docetaxel, an advanced taxoid, has been widely used as an anti-mitotic agent, but further augmentation of its properties is still required, including improvement in low aqueous solubility. Herein, we report the development of bio-eliminable low molecular weight methylcellulose-based surfactant-free injectable formulation for the delivery of docetaxel. Crude methylcellulose, a hydrophobically modified cellulose derivative, was hydrolyzed by an enzymatic degradation method to obtain low molecular weight methylcellulose (LMwMC). Docetaxel was successfully loaded in micelles with small particle sizes high drug loading and sustained release profile. The in vivo anti-cancer effects of intravenously injected nanoparticle systems in B16F10 melanoma xenograft mice were evaluated and demonstrated a significantly enhanced therapeutic effect with the docetaxel-LMwMC micellar aggregates compared to a commercially available docetaxel, Taxotere®. Surfactant-free solubilization of docetaxel could be a promising delivery method for effective insoluble drug delivery for anti-tumor efficacy.

多西他赛是一种先进的紫杉烷，已被广泛用作抗有丝分裂剂，但仍需要进一步增强其性能，包括改善低水溶性。在这里，我们报告了生物可消除的低分子量基于甲基纤维素的无表面活性剂注射剂的开发，以用于多西他赛的递送。通过酶促降解方法水解粗甲基纤维素，疏水改性的纤维素衍生物，以获得低分子量甲基纤维素（LMwMC）。多西他赛已成功地装载在具有小粒径，高载药量和持续释放特性的胶束中。在体内评估了静脉注射纳米颗粒系统在B16F10黑色素瘤异种移植小鼠中的抗癌作用，并证明了与市售的多西他赛相比，多西他赛-LMwMC胶束聚集体的治疗作用显着增强。多西他赛的无表面活性剂增溶可能是有效的不溶性药物递送抗肿瘤功效的一种有前途的递送方法。