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International Journal of Molecular Medicine
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Article

Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody

  • Authors:
    • Haitao Li
    • Yunfei Teng
    • Xia Xu
    • Jianyong Liu
  • View Affiliations / Copyright

    Affiliations: Department of Vascular Surgery, Wuhan Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei 430022, P.R. China, Department of Pathology, Wuhan Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, Hubei 430022, P.R. China
  • Pages: 3586-3596
    |
    Published online on: February 28, 2018
       https://doi.org/10.3892/ijmm.2018.3518
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Abstract

The most common tumors in children are infantile hemangiomas which could cause morbidity and severe complications. The development of novel alternative drugs to treat infantile hemangiomas is necessary, since Hemangeol is the only US Food and Drug Administration-approved drug for infantile hemangiomas. However, Hemangeol has several disadvantages, including a high frequency of administration and adverse effects. Rapamycin is a well‑established antiangiogenic drug, and we have previously developed rapamycin lipid polymer nanoparticles (R‑PLNPs) as a local sustained‑release drug delivery system to achieve controlled rapamycin release and to decrease the frequency of administration and side effects of rapamycin. To improve the targeting of R‑PLNPs to infantile hemangiomas in the present study, R‑PLNPs were modified to include an antibody against vascular endothelial growth factor receptor (VEGF). The characteristics, and the anti‑hemangioma activity of the resulting R‑PLNPs coupled with the anti‑VEGFR2 antibody (named R‑PLNPs‑V) were examined in vitro and in vivo. R‑PLNPs‑V possessed a small size (115 nm) and sustained drug release for 6 days. The anti‑VEGFR2 antibody promoted the targeting and cytotoxic effect of R‑PLNPs‑V to human hemangioma endothelial cells and human umbilical vein endothelial cells. Using a subcutaneous infantile hemangioma xenograft in mice, the in vivo therapeutic effect (evaluated with hemangioma weight, volume, and microvessel density) of R‑PLNPs‑V was demonstrated to be superior compared with rapamycin alone and other non‑targeted nanoparticles, without any total body weight loss. In summary, R‑PLNPs‑V could facilitate targeted delivery and sustained release of rapamycin to infantile hemangiomas, and thus may represent a promising candidate treatment for infantile hemangiomas.
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Copy and paste a formatted citation
Spandidos Publications style
Li H, Teng Y, Xu X and Liu J: Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody. Int J Mol Med 41: 3586-3596, 2018.
APA
Li, H., Teng, Y., Xu, X., & Liu, J. (2018). Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody. International Journal of Molecular Medicine, 41, 3586-3596. https://doi.org/10.3892/ijmm.2018.3518
MLA
Li, H., Teng, Y., Xu, X., Liu, J."Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody". International Journal of Molecular Medicine 41.6 (2018): 3586-3596.
Chicago
Li, H., Teng, Y., Xu, X., Liu, J."Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody". International Journal of Molecular Medicine 41, no. 6 (2018): 3586-3596. https://doi.org/10.3892/ijmm.2018.3518
Copy and paste a formatted citation
x
Spandidos Publications style
Li H, Teng Y, Xu X and Liu J: Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody. Int J Mol Med 41: 3586-3596, 2018.
APA
Li, H., Teng, Y., Xu, X., & Liu, J. (2018). Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody. International Journal of Molecular Medicine, 41, 3586-3596. https://doi.org/10.3892/ijmm.2018.3518
MLA
Li, H., Teng, Y., Xu, X., Liu, J."Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody". International Journal of Molecular Medicine 41.6 (2018): 3586-3596.
Chicago
Li, H., Teng, Y., Xu, X., Liu, J."Enhanced rapamycin delivery to hemangiomas by lipid polymer nanoparticles coupled with anti-VEGFR antibody". International Journal of Molecular Medicine 41, no. 6 (2018): 3586-3596. https://doi.org/10.3892/ijmm.2018.3518
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