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Fluorescent Leakage Assay to Investigate Membrane Destabilization by Cell-Penetrating Peptide
Published on: December 19, 2020
Rapid leakage from PEGylated liposomes triggered by bubbles
Tetsuya Fujie1, Makoto Yoshimoto1
1Department of Applied Chemistry, Yamaguchi University, Tokiwadai 2-16-1, Ube 755-8611, Japan. yosimoto@yamaguchi-u.ac.jp.
Air bubbles significantly accelerate drug leakage from PEGylated liposomes by disrupting lipid bilayers. This bubble-induced release is crucial for controlled drug delivery applications, unlike static conditions or shear flow alone.
Area of Science:
- Colloidal science and materials science
- Biophysical chemistry and drug delivery systems
Background:
- Liposomes serve as effective colloidal carriers for drugs and proteins.
- Physicochemical stimuli-triggered leakage from liposomes has broad biochemical and biomedical applications.
- PEGylated liposomes are utilized to improve drug delivery characteristics.
Purpose of the Study:
- To investigate the effects of air bubbles on the characteristics of PEGylated liposomes.
- To examine the encapsulation and release of 5(6)-carboxyfluorescein from liposomes under varying conditions.
Main Methods:
- Fabrication of PEGylated liposomes using 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) and DSPE-PEG with PEG moieties of 550 or 5000 Da.
- Generation of air bubbles using a bubble column at specific gas velocities.
- Measurement of dye leakage from liposomes in static liquid, gas-liquid flow, and liquid shear flow.
Main Results:
- Leakage from PEGylated liposomes was significantly accelerated by air bubbles at 25 or 40 °C and pH 7.4.
- The dye release rate constant in gas-liquid flow was 168 times higher for liposomes with 1 mol% DSPE-PEG (5000 Da) compared to static conditions.
- Leakage was minimal in non-PEGylated liposomes and less pronounced in liquid shear flow without bubbles, indicating bubble-liposome interaction is key.
Conclusions:
- The interaction between air bubbles and PEGylated liposomes is responsible for the rapid leakage of encapsulated contents.
- Adsorption of PEGylated lipids to bubbles likely induces leaky lipid bilayers, affecting drug release.
- Findings highlight the potential of bubble-mediated processes for controlled release from liposomal drug delivery systems.
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