中国组织工程研究

中国组织工程研究 ›› 2010, Vol. 14 ›› Issue (47): 8800-8804.doi: 10.3969/j.issn.1673-8225.2010.47.015

• 药物控释材料 drug delivery materials • 上一篇    下一篇

整合素αvβ3受体靶向载药脂质体的制备及体外靶向性

解旭品，周兆熊，胡亚立，张柏根，张纪蔚   

  1. 上海交通大学医学院附属仁济医院血管外科，上海市  200001
  • 出版日期:2010-11-19 发布日期:2010-11-19
  • 通讯作者: 张纪蔚，教授，主任医师，上海交通大学医学院附属仁济医院血管外科，上海市 200001 zhangjiwei001@sina.com
  • 作者简介:解旭品★，男，1984年生，山东省临沂市人，汉族，上海交通大学医学院附属仁济医院在读硕士，主要从事下肢动脉硬化的机制及防治研究。 xiexupin@163.com
  • 基金资助:

    上海市科学技术委员会科研计划项目(0852nm05100)。

Preparation of integrin αvβ3 targeted liposome and its targeted ability in vitro

Xie Xu-pin, Zhou Zhao-xiong, Hu Ya-li, Zhang Bai-gen, Zhang Ji-wei   

  1. Department of Vascular Surgery, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai   200001, China
  • Online:2010-11-19 Published:2010-11-19
  • Contact: Zhang Ji-wei, Professor, Chief physician, Department of Vascular Surgery, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200001, China zhangjiwei001@sina.com
  • About author:Xie Xu-pin★, Studying for master’s degree, Department of Vascular Surgery, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200001, China xiexupin@163.com
  • Supported by:

    Scientific Research Plan of Science and Technology Commission of Shanghai, No. 0852nm05100*

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摘要：

背景：含RGD序列的多肽是多种整合素的识别位点，以其相对分子质量小、稳定、易于制备，且无免疫原性等优点被广泛用于纳米靶向药物传递系统的设计。
目的：制备以RGD环五肽为配基的整合素αvβ3载药脂质体，通过体外细胞学实验证实其受体靶向性。
方法：使用人工合成的RGD环五肽作为靶向分子探针，通过高压均质法制备靶向整合素αvβ3载药脂质体，采用扫描电镜和激光粒度分析仪检测纳米颗粒形态和粒径；以流式细胞分析观察其对血管平滑肌细胞的特异性标记，并考察荷载药物的离体缓释能力以及体外靶向能力。
结果与结论：合成的靶向载药脂质体粒径为(175±6) nm，包封率为(96.33±1.02)%，体外溶出时间超过5 d。靶向载药脂质体对整合素αvβ3具有较高的特异性亲和力，可通过受体介导的内吞作用进入细胞内。提示制备的靶向整合素αvβ3载药脂质体，具有较高的药物包封率及缓释性，能与整合素αvβ3受体特异性结合，是一种新型的受体介导靶向制剂。

关键词: 整合素&alpha, v&beta, 3, RGD(精氨酸-甘氨酸-天冬氨酸), 醋酸地塞米松, 靶向载药脂质体, 生物材料与药物控释

Abstract:

BACKGROUND: RGD-containing peptides are recognition sites of a variety of integrin and are widely used in the design of targeting nanoparticles for drug delivery system due to its small molecular weight, stability, easy preparation, and no immunogenicity.
OBJECTIVE: To synthesize the integrin αvβ3 targeted liposome, loading drugs and with RGD oligopeptide as main binding components, and to assess its receptor targeted ability through in vitro cytology experiment.
METHODS: The synthetic RGD oligopeptide served as targeted molecular probe, the liposomes conjugated with Arg-Gly-Asp (RGD) peptides were made by high pressure homogeneous processing methods. The morphology and size were examined by scanning electron microscope and laser particle size analyzer. The specific mark of vascular smooth muscle cells was analyzed with flow cytometry, as well as the ex vivo release and in vitro targeting ability of loaded drugs.
RESULTS AND CONCLUSION: The particle size of targeted liposome was (175±6) nm, and the encapsulation efficiency was (96.33±1.02)%.The targeted liposome loading drugs could release persisted over 5 days in vitro. The targeted liposome had specific affinity for αvβ3 integrin and could enter cells with receptor-mediated endocytosis. The integrin αvβ3 targeted liposomes have relatively high encapsulation efficiency and sustained release pattern, it can bind particularly with αvβ3 integrin and may become a new type receptor-mediated targeting agent.

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