Preparation of bifunctional RGD-R8 peptide modified doxorubicin liposome and in vitro evaluation

何笑冬; 舒小镭; 李少林

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Preparation of bifunctional RGD-R8 peptide modified doxorubicin liposome and in vitro evaluation

更新时间：2026-01-09

- Preparation of bifunctional RGD-R8 peptide modified doxorubicin liposome and in vitro evaluation
- Journal of Army Medical University Vol. 36, Issue 20, Pages: 2103-2107(2014)
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  CLC： R914.5;R966;R979.14
- Published：2014
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何笑冬,舒小镭,李少林.双功能RGD/R8修饰阿霉素脂质体的制备及其体外评价[J].陆军军医大学学报(原第三军医大学学报),2014,36(20):2103-2107.

　He Xiaodong,Shu Xiaolei,Li Shaolin.Preparation of bifunctional RGD-R8 peptide modified doxorubicin liposome and in vitro evaluation[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(20):2103-2107.
何笑冬,舒小镭,李少林.双功能RGD/R8修饰阿霉素脂质体的制备及其体外评价[J].陆军军医大学学报(原第三军医大学学报),2014,36(20):2103-2107. DOI：

　He Xiaodong,Shu Xiaolei,Li Shaolin.Preparation of bifunctional RGD-R8 peptide modified doxorubicin liposome and in vitro evaluation[J].J Amry Med Univ (J Third Mil Med Univ),2014,36(20):2103-2107. DOI：

摘要

目的制备串联的RGD-R8肽修饰阿霉素（DOX）脂质体（RGD-R8-LP-DOX），对其理化性质进行表征，并研究脂质体与乳腺癌MCF-7细胞的亲和力和增殖抑制作用。方法采用薄膜分散法制备RGD-R8-LP-DOX，研究脂质体的形态、粒径、电位以及包封率；定量细胞摄取实验研究乳腺癌MCF-7细胞对RGD-R8-LP的摄取效率以及对脂质体摄取的影响因素。定性共聚焦实验观察肿瘤细胞对脂质体的摄取。MTT实验研究RGD-R8-LP-DOX对乳腺癌MCF-7细胞的细胞毒性。结果 RGD-R8-LP-DOX的粒径为（115.8±11.5）nm，电位为（23.45±4.68）mV，阿霉素的包封率为95.6%。细胞摄取实验结果显示，RGD-R8-LP在4 h摄取效率是2 h的1.75倍，差异有统计学意义（P0.05）；MCF-7细胞在与脂质体共同孵育4 h后对RGD-R8-LP的摄取效率分别是R8-LP、RGD -LP和LP的2.1倍、2.9倍和3.8倍，差异有统计学意义（P0.01）；RGD-R8-LP-DOX与乳腺癌MCF-7细胞孵育24 h后的存活率是48 h的1.8倍，差异有统计学意义（P0.05）；在给药48 h后，R8-LP-DOX、RGD -LP-DOX和LP-DOX的细胞存活率分别是RGD-R8-LP-DOX组的1.6倍、1.8倍和2.4倍，差异有统计学意义（P0.01）。结论整合素受体特异性配体RGD和细胞穿膜肽R8串联的RGD-R8肽修饰阿霉素脂质体能够有效穿透肿瘤细胞膜进入肿瘤细胞，是一种潜在高效的乳腺癌给药系统。

Abstract

Objective To prepare RGD-R8 modified doxorubicin liposome (RGD-R8-LP-DOX) and to study its activity on breast cancer MCF-7 cells. Methods RGD-R8-LP-DOX was prepared by film-ultrasonic dispersion method. The appearance

particle size

Zeta potential

and entrapment efficiency were evaluated. The cellular uptake of RGD-R8-LP by MCF-7 cells in vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD-R8-LP-DOX was evaluated by MTT assay. Results The particle diameter of the liposome was 115.8±11.5 nm with the Zeta potential of 23.45±4.68 mV. The entrapment efficiency of DOX was 95.6%. The RGD-R8-LP uptaking rate by MCF-7 cells at 4 h was 1.75 times higher than that at 2 h (P0.05). The RGD-R8-LP uptaking rate by MCF-7 cells was 2.1

2.9 and 3.8 times higher than that of R8-LP

RGD-LP and LP

respectively (P0.01). The cell viability of MCF-7 cells treated by RGD-R8-LP-DOX for 24 h was 1.8 times higher than that for 48 h (P0.05). MTT assay demonstrated that after 48 h treatment

the cell viability of MCF-7 cells treated by R8-LP-DOX

RGD-LP-DOX and LP-DOX were 1.6

1.8 and 2.4 times higher than that of RGD-R8-LP-DOX (P0.01)

respectively. Conclusion RGD-R8-LP-DOX might serve as a promising breast cancer delivery system of antitumor drugs.

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