Tumor regression and modulation of gene expression via tumor-targeted tocotrienol niosomes

Tan DM 1 , Fu JY 1 , Wong FS 1 , Er HM 2 , Chen YS 3 , Nesaretnam K 1

Affiliations 

  • 1 Product Development & Advisory Services Division, Malaysian Palm Oil Board, No 6, Persiaran Institusi, Bandar Baru Bangi, 43000 Kajang, Selangor Darul Ehsan, Malaysia
  • 2 Department of Pharmaceutical Chemistry, School of Pharmacy, International Medical University, No 126, Jalan 19/155B, Bukit Jalil, 57000 Kuala Lumpur, Malaysia
  • 3 Department of Human Biology, School of Medicine, International Medical University, No 126, Jalan 19/155B, Bukit Jalil, 57000 Kuala Lumpur, Malaysia
Nanomedicine (Lond), 2017 Oct;12(20):2487-2502.
PMID: 28972460 DOI: 10.2217/nnm-2017-0182

Abstract

AIM: To develop 6-O-palmitoyl-ascorbic acid-based niosomes targeted to transferrin receptor for intravenous administration of tocotrienols (T3) in breast cancer.

MATERIALS & METHODS: Niosomes were prepared using film hydration and ultrasonication methods. Transferrin was coupled to the surface of niosomes via chemical linker. Nanovesicles were characterized for size, zeta potential, morphology, stability and biological efficacy.

RESULTS: When evaluated in MDA-MB-231 cells, entrapment of T3 in niosomes caused 1.5-fold reduction in IC50 value compared with nonformulated T3. In vivo, the average tumor volume of mice treated with tumor-targeted niosomes was 12-fold lower than that of untreated group, accompanied by marked downregulation of three genes involved in metastasis.

CONCLUSION: Findings suggested that tumor-targeted niosomes served as promising delivery system for T3 in cancer therapy.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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