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pH-sensitive pHLIP® coated niosomes.

Mohan C Pereira1, Monica Pianella2, Da Wei1

  • 1a Physics Department , University of Rhode Island , Kingston , RI , USA.

Molecular Membrane Biology
|August 10, 2017
PubMed
Summary

Novel pH-sensitive niosomes coated with pH (Low) insertion peptide (pHLIP) target cancer sites effectively. These targeted nanocarriers show enhanced tumor uptake and improved biodistribution for potential cancer theranostics.

Keywords:
Drug deliveryfluorescence imagingtargeting tumor acidity

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Area of Science:

  • Nanomedicine
  • Biotechnology
  • Materials Science

Background:

  • Nanomedicine offers advantages over conventional therapies by enabling tunable properties of nanocarriers for drug encapsulation.
  • Efficient and specific targeting of nanocarriers to pathological sites is crucial for minimizing side effects and maximizing therapeutic efficacy.

Purpose of the Study:

  • To develop a novel targeted nano drug delivery system for cancer theranostics.
  • To create pH-sensitive niosomes utilizing pH (Low) insertion peptide (pHLIP) as an acidity-sensitive targeting moiety.

Main Methods:

  • Formulation of pH-sensitive niosomes (80-90 nm) using nonionic surfactants, cholesterol, and DSPE-lipid or pyrene-conjugated pHLIP.
  • Evaluation of pHLIP-coated niosomes' ability to sense extracellular acidity in cancer cells.
  • In vivo studies involving intravenous injection of fluorescently labeled pHLIP-coated niosomes into tumor-bearing mice.

Main Results:

  • pHLIP-coated niosomes demonstrated significant accumulation in tumors.
  • Targeted niosomes showed 2-3 times higher tumor uptake compared to non-targeted PEGylated niosomes.
  • Minimal targeting of non-cancerous tissues like kidney, liver, and muscles was observed.

Conclusions:

  • pHLIP-coated niosomes effectively target tumor sites by sensing extracellular acidity.
  • These niosomes exhibit prolonged circulation time and uniform biodistribution within tumors.
  • pHLIP-coated niosomes represent a promising novel delivery system for cancer theranostics.