Successful in vivo hyperthermal therapy toward breast cancer by Chinese medicine shikonin-loaded thermosensitive micelle

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

6 Scopus Citations
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Author(s)

  • Yonghua Su
  • Nian Huang
  • Di Chen
  • Li Zhang
  • Xia Dong
  • Yun Sun
  • Xiandi Zhu
  • Fulei Zhang
  • Jie Gao
  • Ying Wang
  • Kexing Fan
  • Wei Li
  • Changquan Ling

Related Research Unit(s)

Detail(s)

Original languageEnglish
Pages (from-to)4019-4035
Journal / PublicationInternational Journal of Nanomedicine
Volume12
Publication statusPublished - 29 May 2017

Link(s)

Abstract

The Chinese traditional medicine Shikonin is an ideal drug due to its multiple targets to tumor cells. But in clinics, improving its aqueous solubility and tumor accumulation is still a challenge. Herein, a copolymer with tunable poly(N-isopropylacrymaide) and polylactic acid block lengths is designed, synthesized, and characterized in nuclear magnetic resonance. The corresponding thermosensitive nanomicelle (TN) with well-defined core-shell structure is then assembled in an aqueous solution. For promoting the therapeutic index, the physical-chemistry properties of TNs including narrow size, low critical micellar concentration, high serum stability, tunable volume phase transition temperature (VPTT), high drug-loading capacity, and temperature-controlled drug release are systematically investigated and regulated through the fine self-assembly. The shikonin is then entrapped in a degradable inner core resulting in a shikonin-loaded thermosensitive nanomicelle (STN) with a VPTT of similar to 40 degrees C. Compared with small-molecular shikonin, the in vitro cellular internalization and cytotoxicity of STN against breast cancer cells (Michigan Cancer Foundation-7) are obviously enhanced. In addition, the therapeutic effect is further enhanced by the programmed cell death (PCD) specifically evoked by shikonin. Interestingly, both the proliferation inhibition and PCD are synergistically promoted as T. VPTT, namely the temperature-regulated passive targeting. Consequently, as intravenous injection is administered to the BALB/c nude mice bearing breast cancer, the intratumor accumulation of STNs is significantly increased as T. VPTT, which is regulated by the in-house developed heating device. The in vivo antitumor assays against breast cancer further confirm the synergistically enhanced therapeutic efficiency. The findings of this study indicate that STN is a potential effective nanoformulation in clinical cancer therapy.

Research Area(s)

  • thermosensitive micelle, shikonin, breast cancer, intra-tumor accumulation, critical micelle concentration, hyperthermal therapy, in vivo, THERMORESPONSIVE POLYMERIC MICELLES, BLOCK-COPOLYMER MICELLES, DRUG-DELIVERY, SOLID TUMORS, TARGETED CHEMOTHERAPY, INTRACELLULAR UPTAKE, RELEASE, CELLS, NANOPARTICLES, STABILITY

Citation Format(s)

Successful in vivo hyperthermal therapy toward breast cancer by Chinese medicine shikonin-loaded thermosensitive micelle. / Su, Yonghua; Huang, Nian; Chen, Di; Zhang, Li; Dong, Xia; Sun, Yun; Zhu, Xiandi; Zhang, Fulei; Gao, Jie; Wang, Ying; Fan, Kexing; Lo, Puichi; Li, Wei; Ling, Changquan.

In: International Journal of Nanomedicine, Vol. 12, 29.05.2017, p. 4019-4035.

Research output: Journal Publications and Reviews (RGC: 21, 22, 62)21_Publication in refereed journal

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