One-Step Self-Assembling Method to Prepare Dual-Functional Transferrin Nanoparticles for Antitumor Drug Delivery.
One-Step Self-Assembling Method to Prepare Dual-Functional Transferrin Nanoparticles for Antitumor Drug Delivery.
复制标题
DOI：
10.1016/j.xphs.2015.12.007
复制
发表时间：
2016-03
影响因子：
3.8
通讯作者：
Kaikai Wang;A. Yuan;Jiaqian Yu;Jinhui Wu;Yiqiao Hu
中科院分区：
文献类型：
--
作者：
Kaikai Wang;A. Yuan;Jiaqian Yu;Jinhui Wu;Yiqiao Hu
基于蛋白质的纳米颗粒由于其高生物相容性和生物可降解性，在临床前和临床实践中都有很大的前景。然而，复杂的制剂往往使蛋白质变性，从而降低其生物活性。为了克服这些缺点，我们开发了一种一步自组装的方法来制备蛋白质基纳米颗粒。转铁蛋白（Tf）是一种靶向蛋白，与2-巯基乙醇混合以破坏二硫键。利用这种方法，可以很容易地获得Tf- ptx - nps（紫杉醇负载Tf纳米粒子）。Tf-PTX-NPs呈圆形，直径可控制在5 ~ 200 nm范围内。Tf在体外形成纳米颗粒后对其受体的生物活性也得到了证实。Tf-PTX-NPs在小鼠异种肿瘤移植模型中也能一定程度地抑制肿瘤生长。因此，我们利用这种自组装方法，制备了以Tf为基础的抗肿瘤纳米颗粒，其中Tf既作为靶向片段，又作为药物载体。
Protein-based nanoparticles hold great promise in both preclinical and clinical practices due to their high biocompatibility and biodegradability. However, the complicated preparations often denature proteins, which subsequently diminish their bioactivity. To overcome these drawbacks, we developed a one-step self-assembling method for preparing protein-based nanoparticles. Transferrin (Tf), a targeting protein, was mixed with 2-mercaptoethanol to break disulfide bonds. Using this method, Tf-PTX-NPs (paclitaxel-loaded Tf nanoparticles) could be readily obtained. Tf-PTX-NPs were round and their diameter could be controlled in the range of 5-200 nm. The bioactivity of Tf to its receptor after forming nanoparticles was also confirmedin vitro. Tf-PTX-NPs also could inhibit the tumor growth to some extent in a mice tumor xenograft model. Therefore, using this self-assembling method, we fabricated this antitumor Tf-based nanoparticle, in which Tf acted as both the targeting moiety and drug carrier.