Effect of RGD-modified paclitaxel and microRNA-34a co-loaded liposome on inhibiting tumor growth in A549-bearing nude mice

赵欣; 张健

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Effect of RGD-modified paclitaxel and microRNA-34a co-loaded liposome on inhibiting tumor growth in A549-bearing nude mice

更新时间：2026-01-09

- Effect of RGD-modified paclitaxel and microRNA-34a co-loaded liposome on inhibiting tumor growth in A549-bearing nude mice
- Journal of Army Medical University Vol. 37, Issue 12, Pages: 1243-1247(2015)
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  CLC： R734.2;R969;R979.1
- Published：2015
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赵欣,张健.RGD修饰共载紫杉醇与microRNA-34a脂质体对肺癌裸鼠移植瘤的生长抑制作用[J].陆军军医大学学报(原第三军医大学学报),2015,37(12):1243-1247.

　Zhao Xin,Zhang Jian.Effect of RGD-modified paclitaxel and microRNA-34a co-loaded liposome on inhibiting tumor growth in A549-bearing nude mice[J].J Amry Med Univ (J Third Mil Med Univ),2015,37(12):1243-1247.
赵欣,张健.RGD修饰共载紫杉醇与microRNA-34a脂质体对肺癌裸鼠移植瘤的生长抑制作用[J].陆军军医大学学报(原第三军医大学学报),2015,37(12):1243-1247. DOI：

　Zhao Xin,Zhang Jian.Effect of RGD-modified paclitaxel and microRNA-34a co-loaded liposome on inhibiting tumor growth in A549-bearing nude mice[J].J Amry Med Univ (J Third Mil Med Univ),2015,37(12):1243-1247. DOI：

摘要

目的探讨精氨酸-甘氨酸-天冬氨酸（Arg-Gly-Asp，RGD）修饰共载紫杉醇与microRNA-34a脂质体（RGD miLPs-34a/PTX）的体内药代动力学以及体内对肺癌裸鼠移植瘤的生长抑制作用。方法采用荧光分光光度法检测RGD miLPs-34a/PTX的体外血清稳定性和体内药代动力学。构建肺癌裸鼠移植瘤模型，近红外活体成像研究RGD miLPs-34a/PTX在荷瘤裸鼠的体内分布。荷瘤裸鼠治疗实验检测RGD miLPs-34a/PTX对肿瘤的生长抑制作用。结果 RGD miLPs-34a/PTX在50%血清中具有良好的稳定性。药代动力学实验表明，在荷瘤小鼠血液中的microRNA-34a的消除速率明显快于miLPs-34a/PTX和RGD miLPs-34a/PTX组，差异有统计学意义（P0.05）；活体成像实验结果显示，RGD miLPs-34a/PTX在肿瘤组织的荧光分布显著强于miLPs-34a/PTX。肿瘤生长抑制实验结果显示，RGD miLPs-34a/PTX对肿瘤生长的抑制作用显著强于其他脂质体组，差异有统计学意义（P0.01）。各给药组对肿瘤生长抑制能力显著强于生理盐水组，差异有统计学意义（P0.01）。结论体内研究证实RGD修饰的共载紫杉醇和miRNA脂质体能够延长药物体内循环时间，达到长循环效果，具有良好的体内肿瘤靶向性和体内肿瘤治疗效果。

Abstract

Objective To research the pharmacokinetics and antitumor effect of arginine-glycine-aspartic acid (RGD)-modified paclitaxel and microRNA-34a co-loaded liposome (RGD miLPs-34a/PTX) in A549-bearing nude mice. Methods Fluorescence spectrophotometry was used to evaluate in vitro stability of RGD miLPs-34a/PTX in 50% fetal bovine serum (FBS) and in vivo pharmacokinetics. Near infrared imaging was adopted to evaluate the targeting efficiency of the liposome. A549 cells were xenografted into athymic mice to establish lung cancer mouse models

which were used to evaluate the antitumor effect of the liposome. Results RGD miLPs-34a/PTX could be stable in 50% FBS for 24 h. The elimination of microRNA-34a was much quicker than that of miLPs-34a/PTX and RGD miLPs-34a/PTX (P0.05). Near infrared imaging demonstrated that the accumulation of RGD miLPs-34a/PTX was much higher than that of miLPs-34a/PTX. The antitumor effect of RGD miLPs-34a/PTX was much better than that of other liposomes (P0.05). Conclusion RGD miLPs-34a/PTX shows high targeting efficiency and antitumor effect

and is a promising drug delivery system targeting lung cancer.

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