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Chinese Journal of Medical Ultrasound (Electronic Edition) ›› 2018, Vol. 15 ›› Issue (06): 473-478. doi: 10.3877/cma.j.issn.1672-6448.2018.06.016

Special Issue:

• Basic Science Research • Previous Articles     Next Articles

Preparation of paclitaxel loaded and human epidermal growth factor receptor-2-targeted macromolecular contrast agent and targeting research in vitro

Qing Wen1, Guozhen Yan1,(), Junfeng He1, Yang Liu1   

  1. 1. Department of Ultrasound, The First Affiliated Hospital of Baotou Medical College, Baotou 014010, China
  • Received:2017-09-16 Online:2018-06-01 Published:2018-06-01
  • Contact: Guozhen Yan
  • About author:
    Corresponding author: Yan Guozhen, Email:

Abstract:

Objective

To prepare a high molecular contrast agent carrying paclitaxel and anti human epidermal growth factor receptor-2 (HER-2) antibody, and to investigate the target ability in vitro and its effects on ultrasonography in vitro.

Methods

The paclitaxel-loaded and anti HER-2 antibodies polymer contrast agents were prepared by the double emulsion technique and carbodiimide technique, and its general properties were by tested. The combination of drug-loading targeted contrast agent and SKBR-3 breast cancer cells was observed with laser confocal microscope. The effect of imaging in vitro was observed by the high frequency ultrasonography.

Results

The average diameter of drug-loaded targeting carboxyl terminal lactic acid (PLGA) nanoparticle was (318.07±12.51) nm, the surface potential was (-2.16±0.31) mV, the drug encapsulation efficiency was (60.00±3.40)%, the drug loading amounts was (6.00±0.34)%, and the contrast agent was spherical particles with uniform size and good dispersion. Laser confocal microscope found significant combination of anti HER-2 antibody and carboxyl terminal lactic acid/hydroxyacetic acid copolymer (PLGA-COOH) polymer contrast agent. Flow cytometry observed the combination rate was (99.59±0.42)%. Search target experiment in vitro observed drug targeting macromolecular contrast agent and SBKR-3 breast cancer cells had a high binding rate. In vitro imaging experiments showed that drug targeting macromclecular imgaging agent appeared uniform and fine dotted dense hyper-echogenicity.

Conclusions

A kind of her-2-targeted and paclitaxel loaded high molecular contrast agent was successfully prepared. It had good performance, high drug loading amounts and entrapment efficiency. It and SKBR-3 breast cancer cells had a high binding rate. The external imaging was better.

Key words: Polymer contrast agent, Anti human epidermalgrowth factor receptor-2 antibody, Paclitaxel

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