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Related Concept Videos

Bioavailability Enhancement: Drug Permeability Enhancement01:27

Bioavailability Enhancement: Drug Permeability Enhancement

136
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
136

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Related Experiment Video

Updated: Dec 23, 2025

Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
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A General Approach to Enzyme-Responsive Liposomes.

Jinchao Lou1, Michael D Best1

  • 1Department of Chemistry, University of Tennessee, 1420 Circle Drive, Knoxville, TN, 37996, USA.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|April 18, 2020
PubMed
Summary

Enzyme-responsive liposomes offer improved drug delivery by releasing contents when encountering disease-specific enzymes. This modular approach enhances liposome control for targeted therapeutic applications.

Keywords:
drug deliveryenzymeslipidsliposomesmodular strategy

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Area of Science:

  • Biotechnology
  • Nanomedicine
  • Drug Delivery Systems

Background:

  • Liposomes are efficient nanocarriers for drug delivery to diseased cells.
  • Controlling the release of encapsulated drugs at the target site is crucial for improving liposome efficacy.
  • Enzymes, often overexpressed in diseased cells, present promising targets for triggered liposome release.

Purpose of the Study:

  • To develop a general strategy for enzyme-responsive liposomes.
  • To exploit commonly aberrant enzymes in disease (esterases, phosphatases, β-galactosidases) for liposome cargo release.
  • To design and synthesize novel responsive lipids for enzyme-triggered drug delivery.

Main Methods:

  • Designed and synthesized enzyme-responsive lipids with substrate moieties linked via self-immolating linkers to non-bilayer lipid scaffolds.
  • Utilized liposome dye leakage assays to assess content release upon enzymatic treatment.
  • Employed Dynamic Light Scattering (DLS) analysis to evaluate changes in liposome particle size and membrane properties.

Main Results:

  • Enzyme-responsive liposomes demonstrated significant content release upon exposure to specific enzymes compared to controls.
  • Liposome composition tuning proved critical for controlling the release rate and extent.
  • DLS analysis indicated alterations in membrane properties, evidenced by particle size increases for esterase- and β-galactosidase-responsive liposomes.

Conclusions:

  • A modular and effective strategy for creating enzyme-responsive liposomes has been established.
  • This approach allows for tailored targeting of various disease-associated enzymes.
  • These enzyme-responsive liposomes represent a promising advancement for targeted liposomal drug delivery.