Ebpay生命医药出版社

Ebpay生命

100530

论文已发表

提 交 论 文


注册即可获取Ebpay生命的最新动态

注 册



IF 收录期刊



  • 3.3 Breast Cancer (Dove Med Press)
  • 3.4 Clin Epidemiol
  • 2.5 Cancer Manag Res
  • 2.9 Infect Drug Resist
  • 3.5 Clin Interv Aging
  • 4.7 Drug Des Dev Ther
  • 2.7 Int J Chronic Obstr
  • 6.6 Int J Nanomed
  • 2.5 Int J Women's Health
  • 2.5 Neuropsych Dis Treat
  • 2.7 OncoTargets Ther
  • 2.0 Patient Prefer Adher
  • 2.3 Ther Clin Risk Manag
  • 2.5 J Pain Res
  • 2.8 Diabet Metab Synd Ob
  • 2.8 Psychol Res Behav Ma
  • 3.0 Nat Sci Sleep
  • 1.8 Pharmgenomics Pers Med
  • 2.7 Risk Manag Healthc Policy
  • 4.2 J Inflamm Res
  • 2.1 Int J Gen Med
  • 4.2 J Hepatocell Carcinoma
  • 3.7 J Asthma Allergy
  • 1.9 Clin Cosmet Investig Dermatol
  • 2.7 J Multidiscip Healthc



更多详情 >>





已发表论文

含共轭亚油酸紫杉醇（CLA-PTX）的 iRGD 修饰脂质体，对 B16-F10 黑色素瘤的抗肿瘤效果影响

 

Authors Du R, Zhong T, Zhang WQ, Song P, Song WD, Zhao Y, Wang C, Tang YQ, Zhang X, Zhang Q

Published Date June 2014 Volume 2014:9(1) Pages 3091—3105

DOI http://dx.doi.org/10.2147/IJN.S65664

Received 7 April 2014, Accepted 6 May 2014, Published 24 June 2014

 
Abstract: In the present study, we prepared a novel delivery system of iRGD (CRGDK/RGPD/EC)-modified sterically stabilized liposomes (SSLs) containing conjugated linoleic acid–paclitaxel (CLA-PTX). The anti-tumor effect of iRGD-SSL-CLA-PTX was investigated on B16-F10 melanoma in vitro and in vivo. The in vitro targeting effect of iRGD-modified SSLs was investigated in a real-time confocal microscopic analysis experiment. An endocytosis-inhibition assay was used to evaluate the endocytosis pathways of the iRGD-modified SSLs. In addition, the in vitro cellular uptake and in vitro cytotoxicity of iRGD-SSL-CLA-PTX were evaluated in B16-F10 melanoma cells. In vivo biodistribution and in vivo antitumor effects of iRGD-SSL-CLA-PTX were investigated in B16-F10 tumor-bearing mice. The induction of apoptosis by iRGD-SSL-CLA-PTX was evaluated in tumor-tissue sections. Real-time confocal microscopic analysis results indicated that the iRGD-modified SSLs internalized into B16-F10 cells faster than SSLs. The identified endocytosis pathway of iRGD-modified SSLs indicated that energy- and lipid raft-mediated endocytosis played a key role in the liposomes’ cellular uptake. The results of the cellular uptake experiment indicated that the increased cellular uptake of CLA-PTX in the iRGD-SSL-CLA-PTX-treated group was 1.9-, 2.4-, or 2.1-fold compared with that in the CLA-PTX group after a 2-, 4-, or 6-hour incubation, respectively. In the biodistribution test, the CLA-PTX level in tumor tissues from iRGD-SSL-CLA-PTX-treated mice at 1 hour (1.84±0.17 µg/g) and 4 hours (1.17±0.28 µg/g) was 2.3- and 2.0-fold higher than that of CLA-PTX solution at 1 hour (0.79±0.06 µg/g) and 4 hours (0.58±0.04 µg/g). The value of the area under the curve for the first 24 hours in the tumors of iRGD-SSL-CLA-PTX-treated mice was significantly higher than that in the SSL-CLA-PTX and CLA-PTX solution-treated groups (P <0.01). The in vivo antitumor results indicated that iRGD-SSL-CLA-PTX significantly inhibited the growth of B16-F10 tumors compared with the SSL-CLA-PTX or CLA-PTX solution-treatment groups (P <0.01). The results of tumor-cell apoptosis showed that tumors from the iRGD-SSL-CLA-PTX-treated group exhibited more advanced cell apoptosis compared with the control, CLA-PTX solution-, and SSL-CLA-PTX-treated groups. In conclusion, the antitumor effect of iRGD-SSL-CLA-PTX was confirmed on B16-F10 melanoma in vitro and in vivo.
Keywords: peptide-modified liposome, iRGD, CLA-PTX, antitumor effect, in vitro, in vivo






Download Article[PDF]