Weakly acidic pH-responsive liposomal content release induced by histidine-modified agents
Ayumi Kashiwada1,2, Narumi Taoka1, Yukiha Chijimi1
1Department of Applied Molecular Chemistry, College of Industrial Technology, Nihon University, 1-2-1, Izumi-cho, Narashino, Chiba, 275-8575, Japan. kashiwada.ayumi@nihon-u.ac.jp.
Organic & Biomolecular Chemistry
|March 22, 2024
Summary
Histidine-modified liposomes offer controlled drug release triggered by internal pH changes. C12-His liposomes demonstrated significant pH-dependent release, paving the way for targeted therapeutic delivery systems.
Area of Science:
- Biomedical Engineering
- Drug Delivery
- Nanotechnology
Background:
- Liposomal vesicles are innovative for site-specific drug delivery.
- Internal stimuli-responsive release enhances therapeutic efficacy.
- Controlling liposomal release within endosomes is a key challenge.
Purpose of the Study:
- To design histidine-modified agents (Cn-His) for endosomal pH-controlled liposomal drug release.
- To investigate the pH-dependent properties and content release of Cn-His-incorporated liposomes.
- To establish a platform for clinically applicable triggered release formulations.
Main Methods:
- Synthesis and incorporation of histidine-modified agents (Cn-His) into liposomes.
- Characterization of liposome properties (size, ζ-potential) using dynamic light scattering and ζ-potential measurements.
- Assessment of pH-dependent content release (carboxyfluorescein, Nile red) via fluorescence spectroscopy.
Main Results:
- Liposomes maintained uniform size across tested pH conditions.
- ζ-potential shifted from neutral/negative at physiological pH to positive at acidic endosomal pH.
- Acidic pH triggered significant release of both polar and nonpolar contents, with C12-His showing notable pH sensitivity.
Conclusions:
- Cn-His agents effectively render liposomes sensitive to endosomal pH changes.
- The developed liposomes enable triggered content release in response to acidic endosomal environments.
- This research provides a foundation for developing advanced, pH-controllable liposomal drug delivery systems.
