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Related Experiment Videos

Liposomal vasoactive intestinal peptide.

Varun Sethi1, Hayat Onyüksel, Israel Rubinstein

  • 1Department of Pharmaceutics, University of Illinois at Chicago, Chicago, IL 60612, USA.

Methods in Enzymology
|February 22, 2005
PubMed
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Sterically stabilized liposomes (SSL) protect vasoactive intestinal peptide (VIP) from degradation, enhancing its therapeutic potential for various diseases. This formulation strategy prolongs VIP

Area of Science:

  • Drug delivery systems
  • Nanotechnology
  • Biochemistry

Background:

  • Liposomes, particularly sterically stabilized liposomes (SSL), have evolved as advanced drug carriers since the 1960s.
  • SSL offer prolonged circulation and passive targeting to diseased tissues, overcoming limitations of early liposome generations.
  • Vasoactive intestinal peptide (VIP) possesses significant therapeutic potential for unmet medical needs but suffers from rapid degradation in vivo.

Purpose of the Study:

  • To develop and evaluate stable, long-acting formulations of vasoactive intestinal peptide (VIP) using liposome technology.
  • To investigate the conformational changes and protective effects of liposomes on VIP.
  • To optimize the loading of VIP onto sterically stabilized liposomes (SSL).

Main Methods:

Related Experiment Videos

  • Utilized both classic and sterically stabilized liposomes (SSL) as drug delivery platforms for VIP.
  • Employed the film rehydration and extrusion technique for passive loading of VIP onto SSL at room temperature.
  • Analyzed the conformational transition of VIP from random coil to alpha-helix upon association with phospholipid bilayers.

    • Main Results:

    • Spontaneous association of VIP with phospholipid bilayers induced a conformational transition to an alpha-helical structure, enhancing stability.
    • This conformational change protected VIP from enzymatic and spontaneous degradation, prolonging its bioactivity.
    • The film rehydration and extrusion method proved optimal for consistent passive loading of VIP onto SSL.

    Conclusions:

    • VIP formulated with SSL demonstrates enhanced stability and prolonged bioactivity, offering a promising drug delivery strategy.
    • The liposome-induced conformational change is key to protecting VIP and amplifying its therapeutic effects.
    • VIP-loaded SSL represent a viable formulation for preclinical and clinical testing in diseases like pulmonary hypertension, stroke, and Alzheimer's.