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Tumour targeting

Efficient delivery

Nature Reviews Cancer volume 5, page 759 (2005)Cite this article

The authors constructed a targeted drug delivery system comprising polyethylene glycol (PEG) as a carrier, the anticancer agent camptothecin (CPT), and a modified luteinizing hormone-releasing hormone (LHRH) peptide as a targeting moiety. LHRH is overexpressed in ovarian cancer cells and LHRH receptors are only expressed at low levels in healthy ovarian tissue.

When mice bearing human ovarian cancer xenografts were treated with CPT alone, tumours were reduced in size, non-targeted CPT–PEG had increased activity and CPT–PEG–LHRH resulted in the greatest reduction of tumour size. Tumour-cell killing was shown to be by apoptosis, probably due to the increased concentration of CPT entering the cancer cells. To confirm the targeting of the LHRH-conjugate to the ovarian tumours, the authors looked at the distribution of tritium-labelled polymers in the treated mice. Both PEG alone and LHRH–PEG accumulated preferentially in tumour tissue — this is in line with a form of passive targeting known to occur in tumours called the enhanced permeability and retention effect. The level of accumulation of LHRH–PEG was nearly twice that of PEG alone, confirming the active tumour-targeting capacity of this polymer.

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ORIGINAL RESEARCH PAPER

  1. Dharap. S. S. et al. Tumor-specific targeting of an anticancer drug delivery system by LHRH peptide. Proc. Natl Acad. Sci. USA 102, 12962–12967 (2005)

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Authors
  1. Ezzie Hutchinson
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Hutchinson, E. Efficient delivery. Nat Rev Cancer 5, 759 (2005). https://doi.org/10.1038/nrc1721

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