Matrix metalloproteinase-assisted triggered release of liposomal contents

Bioconjug Chem. 2008 Jan;19(1):57-64. doi: 10.1021/bc070081p. Epub 2007 Dec 14.

Abstract

We offer a novel methodology for formulating liposomes by incorporating sequence-specific collagen-mimetic peptides such that they are specifically "uncorked" by a matrix metalloproteinase, MMP-9. By encapsulating carboxyfluorescein (as a self-quenching fluorescent dye), we demonstrate that the time-dependent release of the dye from liposomes is due to the specific enzymatic cleavage of the surface-exposed collagen-mimetic peptides. The specificity of such cleavage is attested by the fact that the liposomal "uncorking" and their content release occur only by MMP-9 and not by a general proteolytic enzyme, trypsin, despite the fact that the collagen mimetic peptides contain the trypsin cleavage site. The mechanistic details underlying the formulations of liposomes and their enzyme-selective "uncorking" and content release are discussed. Arguments are presented that such liposomes can be fine-tuned to serve as the drug delivery vehicles for the detection and treatment of various human diseases, which occur due to the overexpression of a variety of pathogenic matrix metalloproteinases.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Biomimetics
  • Collagen / chemistry
  • Collagen / metabolism
  • Fluorescent Dyes / metabolism
  • Humans
  • Lipoproteins / chemistry
  • Lipoproteins / metabolism
  • Liposomes / chemistry*
  • Liposomes / metabolism*
  • Matrix Metalloproteinase 9 / metabolism*
  • Peptides / chemistry
  • Peptides / metabolism
  • Substrate Specificity
  • Time Factors
  • Transition Temperature
  • Trypsin / metabolism

Substances

  • Fluorescent Dyes
  • Lipoproteins
  • Liposomes
  • Peptides
  • Collagen
  • Trypsin
  • Matrix Metalloproteinase 9