Theranostic liposomes containing conjugated polymer dots and doxorubicin for bio-imaging and targeted therapeutic delivery
Theranostic liposomes containing conjugated polymer dots and doxorubicin for bio-imaging and targeted therapeutic delivery
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含有共轭聚合物点和阿霉素的治疗诊断脂质体，用于生物成像和靶向治疗递送
DOI：
10.1039/c5ra24485d
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发表时间：
2016-01-01
期刊：
影响因子：
3.9
通讯作者：
Li, Nan
中科院分区：
文献类型：
--
作者：
Ma, Man;Lei, Mingzhu;Li, Nan
这项工作致力于开发一种基于脂质的治疗诊断纳米颗粒，能够同时容纳共轭聚合物点、多柔比星（Dox）和叶酸（FA）。由于聚（9，9-二辛基芴-2，7-二基-co-苯并噻二唑）（PFBT）在体外细胞摄取研究中的高亮度和在体外/体内毒性实验中的良好生物相容性，选择其作为荧光探针。治疗诊断脂质体（PFBT-Dox-Lip-FA）的流体动力学尺寸为127.30 ± 3.20（nm），zeta电位为−25.00 ± 2.00（mV）。最重要的是，与Dox-Lip-FA相比，PFBT-Dox-Lip-FA在24 h时的Dox释放程度在轻度高温条件下显示出令人满意的结果。这种快速释放导致MCF-7细胞中较低的半数最大抑制浓度（IC 50）为16.8 ± 4.5（μg mL−1），而Dox-Lip-FA（37 °C）的IC 50为28.3 ± 3.7（μg mL−1）。细胞摄取研究还显示治疗诊断脂质体在肿瘤细胞中的药物蓄积更高。PFBT-Dox-Lip-FA在荷瘤小鼠模型上的体内研究表明，PFBT可以准确地指示脂质体在肿瘤中的分布。PFBT-Dox-Lip-FA对荷瘤小鼠有明显的抑瘤作用。PFBT-Dox-Lip-FA具有可忽略的体内毒性，是一种用于同时进行癌症诊断和靶向药物递送的有用系统。
This work was devoted to the development of a lipid-based theranostic nanoparticle able to simultaneously host conjugated polymer dots, doxorubicin (Dox) and folate acid (FA). Poly(9,9-dioctylfluorene-2,7-diyl-co-benzothiadiazole) (PFBT) was chosen as the fluorescent probe because of its high brightness in in vitro cellular uptake studies and good biocompatibility in in vitro/in vivo toxicity experiments. The theranostic liposomes (PFBT–Dox–Lip–FA) exhibited a hydrodynamic size of 127.30 ± 3.20 (nm) with a zeta potential of −25.00 ± 2.00 (mV). Mostly importantly, the extent of Dox release at 24 h from PFBT–Dox–Lip–FA showed a satisfactory result under mild hyperthermia conditions compared with Dox–Lip–FA. Such rapid release led to a lower half maximal inhibitory concentration (IC50) in MCF-7 cells at 16.8 ± 4.5 (μg mL−1), whereas the IC50 of Dox–Lip–FA (37 °C) was 28.3 ± 3.7 (μg mL−1). The cellular uptake study also revealed higher drug accumulation in tumor cells for theranostic liposomes. In vivo studies of PFBT–Dox–Lip–FA on tumor-bearing mouse models revealed that the distribution of liposomes in the tumors could be indicated accurately by PFBT. Besides, tumor-bearing mice could be significantly inhibited by PFBT–Dox–Lip–FA. Together with its negligible in vivo toxicity, PFBT–Dox–Lip–FA is a useful system for simultaneous cancer diagnosis and targeted drug delivery.