Preparation of targeted and phase-shifted nano-scaled contrast agents loaded with drug and detection of the basic performance

LIU Jianxin; LIU Yang; PENG Wanhong

doi:10.16245/j.cnki.issn1008-6978.2021.04.001

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Preparation of targeted and phase-shifted nano-scaled contrast agents loaded with drug and detection of the basic performance

更新时间：2021-10-08

- Preparation of targeted and phase-shifted nano-scaled contrast agents loaded with drug and detection of the basic performance
- Journal of Clinical Ultrasound in Medicine Vol. 23, Issue 4, Pages: 241-245(2021)
- 作者机构：
  
  1. 华中科技大学同济医学院附属武汉中心医院超声诊断科
  2. 湖北省中西医结合医院放射科
- 作者简介：
- 基金信息：
- DOI：10.16245/j.cnki.issn1008-6978.2021.04.001
  CLC： R943
- Published：2021，
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[1]刘建新,柳阳,彭万宏.靶向相变型载药纳米造影剂的制备及其基本性能和显像特性检测[J].临床超声医学杂志,2021,23(04):241-245.

LIU Jianxin, LIU Yang, PENG Wanhong. Preparation of targeted and phase-shifted nano-scaled contrast agents loaded with drug and detection of the basic performance. [J]. Journal of Clinical Ultrasound in Medicine 23(4):241-245(2021)
[1]刘建新,柳阳,彭万宏.靶向相变型载药纳米造影剂的制备及其基本性能和显像特性检测[J].临床超声医学杂志,2021,23(04):241-245. DOI： 10.16245/j.cnki.issn1008-6978.2021.04.001.

LIU Jianxin, LIU Yang, PENG Wanhong. Preparation of targeted and phase-shifted nano-scaled contrast agents loaded with drug and detection of the basic performance. [J]. Journal of Clinical Ultrasound in Medicine 23(4):241-245(2021) DOI： 10.16245/j.cnki.issn1008-6978.2021.04.001.

摘要

目的制备一种叶酸靶向相变型载羟基喜树碱（HCPT）的纳米粒（FA-HCPT-Fe

-PFP NDs）

检测其基本性能和多模态显像特性。方法采用旋转蒸发-超声法制备FA-HCPT-Fe

-PFP NDs。于制备后不同时间点使用电子显微镜测定纳米粒粒径以检测其稳定性;将纳米粒乳液加热后置于显微镜下观察其相变特性

高效液相色谱法检测纳米粒内药物（HCPT）的载药量。检测观察纳米粒对富含叶酸受体的SKOV3肿瘤细胞的寻靶能力。对不同浓度纳米粒制备成的凝胶块进行光声成像及MRI;使用低强度聚焦超声（LIFU）辐照纳米粒乳液后行超声成像

分别验证其增强光声、MRI及超声成像的能力。结果制备的FA-HCPT-Fe

-PFP NDs性质稳定

HCPT载药量为（8.33±0.57）%

包封率为（60.51±2.33）%

加热后可发生液气相变。体外寻靶实验证实该纳米粒对富含叶酸受体的SKOV3肿瘤细胞局部有良好的靶向性。体外多模态显像增强实验结果表明该纳米粒可以明显增强超声、光声及MRI的显影能力。结论本实验所制备的FA-HCPT-Fe

-PFP NDs具备多模态造影剂的功能

是一种极具潜力的分子探针。

Abstract

Objective To prepare phase-shifted folate-modified and HCPT-loaded nanodroplets（FA-HCPT-Fe

-PFP NDs）

and to investigate the properties and multimodality imaging in vitro.Methods were prepared through the rotary evaporation and sonication process.The size and the stability of FA-HCPT-Fe

-PFP NDs were detected at different time point after preparation.The phase transition characteristic of the nanodroplets was detected.Drug loading was determined with reverse-phase high-performance liquid chromatographic system. Targeting efficiency of FA-HCPTFe

-PFP NDs was validated with cell experiment.Photoacoustic and magnetic resonance imaging were performed on the gel blocks prepared by different concentrations of nanoparticles. Ultrasonic imaging was performed after irradiation of the nanoparticle emulsion with LIFU.The above experiments were used to verify the ability of nanoparticles to enhance photoacoustic imaging

MRI and ultrasound imaging.Results and encapsulation efficiency was（60.51±2.33）%.Phase-transition was observed of FA-HCPT-Fe

-PFP NDs with elevated temperature.Targeting experiments in vitro confirmed that the nanoparticles had good targeting ability to SKOV3 tumor cells rich in folate receptors. FA-HCPT-Fe

-PFP NDs nanoemulsions showed obvious photoacoustic signal

MRI signal and ultrasound signal in vitro.Conclusion molecular probe with great potential.

关键词

纳米粒靶向相变载药造影剂

Keywords

NanodropletsTargetingPhase transitionDrug loadingContrast agent

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