紫杉醇修饰的氧化铁纳米颗粒用于肿瘤成像与治疗

本文利用我们前期工作中制备的聚乙二醇修饰的氧化铁纳米颗粒作为药物载体，共价负载抗肿瘤药物紫杉醇，体外实验表明，该载药体系具有与市售紫杉醇注射液相当的肿瘤细胞毒性，体内实验表明，该载药体系能够有效的聚集在肿瘤组织，且其肿瘤抑制效果优于市售紫杉醇注射液。

Dongfang Liu,Wei Wu,Xi Chen,Song Wen,Xizhi Zhang,Qi Ding,Gaojun Teng，Ning Gu*.Conjugation of paclitaxel to iron oxide nanoparticles for tumor imaging and therapy,Nanoscale, 2012, 4, 2306-2310.

Fig.1 Invitro cytotoxicity of clinical PTX injection (a, black), SPIONPTX (a, white), and SPION-PEG (b, contains the same amount of iron as the SPION-PTX) against Hela cells.

Figure 2T2*-weighted images (TR/TE of 408 ms/3.5 ms) at pre-injection (a) and 4 h post-injection (b) of 8 mg kg_1 of SPION-PTX at the level of the tumor on the proximal thigh of the mice. The white arrow indicates the tumor region. (c) In vivo antitumor effect obtained from each treated group, expressed as the average values of the relative tumor volume v/v0 (where v denotes the tumor volume at test time points and v0 denotes the corresponding initial tumor volume at the beginning of treatment). *P < 0.05 (versus ptx injection group at the equivalent dose from the 5th day). inset shows the typical photographs of excised tumors from mice on the 7th day after treatments with spion-ptx (5 mg kg_1 equiv), ptx (taxol) injection (5 mg kg_1 equiv), spion-peg and saline. (d) evolution of body weight of each group during the experiments. data in (c) and (d) are presented as mean±sd (n="3–5).

Scheme 1Schematic chemical structures of PTX-COOH, SPION-PEG, SPION-PTX and their synthetic routes.