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靶向舌癌的多功能纳米颗粒的制备及体外研究

[Preparation of multifunctional nanoparticles targeting tongue cancer and in vitro study].

作者信息

Ren Wei, Qiu Li-Hua, Gao Zhi, Li Pan, Zhao Xin, Hu Cheng-Chen

机构信息

Dep. of Oral and Maxillofacial Surgery, Stomatological Hospital of Chongqing Medical University, Chongqing Key Laboratory of Oral Diseases and Biomedical Science, Chongqing 401147, China.

Dep. of Oral and Maxillofacial Surgery, Stomatological Hospital of Chongqing Medical University, Chongqing Key Laboratory of Oral Diseases and Biomedical Science, Chongqing 401147, China;Chongqing Municipal Key Laboratory of Oral Biomedical Engineering of Higher Education, Chongqing 401147, China.

出版信息

Hua Xi Kou Qiang Yi Xue Za Zhi. 2018 Jun 1;36(3):240-246. doi: 10.7518/hxkq.2018.03.002.

Abstract

OBJECTIVE

This study aims to prepare docetaxel (DOC)-loaded multifunctional nanoparticles containing indocyanine green (ICG) and perfluorohexane (PFH) as targeted drug delivery system, which is supplemented with stromal cellderived factor-1 (SDF-1), and characterize their properties.

METHODS

Multifunctional nanoparticles were prepared by using the double emulsion method. SDF-1 was covalently conjugated to the surface of the nanoparticles through thioether bonding. Their particle size, distribution, and surface potential were determined with the Malvern measuring instrument. The conjugation of SDF-1 was evaluated by confocal laser scanning microscope. Encapsulation efficiency (ELC), drug loading capacity (DLC), and release regularity of the nanoparticles were determined by high-performance liquid chromatography (HPLC). In vitro photothermal property was recorded by a thermal imager. The in vitro imaging capacity was observed by a photoacoustic instrument and an ultrasonic diagnostic apparatus. Targeting capability was assessed by flow cytometry. The cell activity on SCC-15 cells was checked by CCK-8 method.

RESULTS: The targeted multifunctional nanoparticles showed regularly sphericity. The diameter was (502.88±17.92) nm. The zeta potential was (-11.5±3.15) mV. ELC was 54.12%±1.74%. DLC was 1.08 mg·mL-1. In vitro drug release was initially fast and subsequently slow. The photothermal characteristics were related to the concentration; the higher the concentration, the higher the temperature. Nanoparticles could detect significant photoacoustic and ultrasound signals. The in vitro targeting rate was 89.99%. No significant differences of cell viability in the SINPs groups were observed at each concentration (P>0.05). The inhibition effect of DOC-SINPs was stronger than that of SINPs whether or not in the presence of laser irradiation among the groups of 150 and 200 μg·mL-1 (P<
0.05).

CONCLUSIONS

Multifunctional nanoparticles for diagnosis and treatment were successfully prepared and displayed dualmode ultrasound/photoacoustic imaging and antitumor effects of chemotherapy and photothermal therapy.

摘要

目的

本研究旨在制备负载多西他赛(DOC)的多功能纳米颗粒,其包含吲哚菁绿(ICG)和全氟己烷(PFH)作为靶向给药系统,并补充基质细胞衍生因子-1(SDF-1),并对其性质进行表征。

方法

采用双乳化法制备多功能纳米颗粒。通过硫醚键将SDF-1共价偶联到纳米颗粒表面。用马尔文测量仪测定其粒径、分布和表面电位。通过共聚焦激光扫描显微镜评估SDF-1的偶联情况。通过高效液相色谱(HPLC)测定纳米颗粒的包封率(ELC)、载药量(DLC)和释放规律。用热成像仪记录体外光热性能。用光声仪器和超声诊断仪观察体外成像能力。通过流式细胞术评估靶向能力。用CCK-8法检测对SCC-15细胞的细胞活性。

结果

靶向多功能纳米颗粒呈规则球形。直径为(502.88±17.92)nm。zeta电位为(-11.5±3.15)mV。ELC为54.12%±1.74%。DLC为1.08 mg·mL-1。体外药物释放最初较快,随后较慢。光热特性与浓度有关;浓度越高,温度越高。纳米颗粒能检测到显著的光声和超声信号。体外靶向率为89.99%。在各浓度下,SINPs组的细胞活力无显著差异(P>0.05)。在150和200 μg·mL-1组中,无论是否存在激光照射,DOC-SINPs的抑制作用均强于SINPs(P<0.05)。

结论

成功制备了用于诊断和治疗的多功能纳米颗粒,其显示出双模式超声/光声成像以及化疗和光热疗法的抗肿瘤作用。

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