叶酸受体靶向量子点脂质体作为荧光探针

Folate receptor-targeted quantum dot liposomes as fluorescence probes.

作者信息

Yang Chang, Ding Nan, Xu Yibing, Qu Xiaolan, Zhang Jing, Zhao Chaoyang, Hong Liang, Lu Yao, Xiang Guangya

机构信息

School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

出版信息

J Drug Target. 2009 Aug;17(7):502-11. doi: 10.1080/10611860903013248.

Abstract

In this study, the preparation of the novel imaging agents, folate receptor (FR)-targeted liposomes encapsulating hydrophilic CdTe quantum dots (QDs), and their use as luminescence probes for live cell imaging are reported. Hydrophilic CdTe QDs were directly synthesized in the water phase, and FR-targeted QD liposomes were prepared by hydrating the lipid thin film with CdTe suspension. Formulations were characterized by UV-visible and fluorescent measurements, liposomal particle size, and zeta potential. The targeting and imaging ability of FR-targeted liposomes were investigated against the human uterine cervix cancer cell line (HeLa). Furthermore, the cytotoxicity of QD liposomes was evaluated by HeLa cells incubated with FR-targeted QD liposomes, nontargeted QD liposomes, and free QDs. The results showed that FR-targeted QD liposomes were spherically shaped with high fluorescence yield, excellent photochemical stability, good cancer targeting, and minimal cytotoxicity. The average size of FR-targeted fluorescence liposomes was ~105 nm, and their size distribution was rather narrow. After storage at 4 degrees C for 11 months, QD liposomes maintained similar size and did not show any leakage of QDs. FR-targeted CdTe QD liposomes, which can target tumor cells via FR-mediated endocytosis, would become an attractive probe for tumor cell or tissue imaging for a long-time monitoring.

摘要

在本研究中,报道了新型成像剂——包裹亲水性碲化镉量子点(QDs)的叶酸受体(FR)靶向脂质体的制备及其作为活细胞成像发光探针的应用。亲水性碲化镉量子点在水相中直接合成,通过用碲化镉悬浮液水合脂质薄膜制备FR靶向量子点脂质体。通过紫外可见光谱和荧光测量、脂质体粒径和zeta电位对制剂进行表征。研究了FR靶向脂质体对人子宫颈癌细胞系(HeLa)的靶向和成像能力。此外,通过用FR靶向量子点脂质体、非靶向量子点脂质体和游离量子点孵育HeLa细胞来评估量子点脂质体的细胞毒性。结果表明,FR靶向量子点脂质体呈球形,具有高荧光产率、优异的光化学稳定性、良好的癌症靶向性和最小的细胞毒性。FR靶向荧光脂质体的平均尺寸约为105nm,其尺寸分布相当窄。在4℃储存11个月后,量子点脂质体保持相似的尺寸,并且未显示出任何量子点泄漏。FR靶向碲化镉量子点脂质体可通过FR介导的内吞作用靶向肿瘤细胞,将成为用于肿瘤细胞或组织成像以进行长期监测的有吸引力的探针。

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