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Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing
Ágnes Ábrahám1,2, Gergő Gyulai1,2, Judith Mihály3
1MTA-HUN-REN TTK Lendület "Momentum" Peptide-Based Vaccines Research Group, Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences, Budapest, H-1117, Hungary.
Journal of Pharmaceutical Analysis
|January 30, 2025
Summary
Poloxamers enhance lipopeptide drug applicability by forming stable micelles. This formulation improves solubility, antibacterial and anticancer activity, and antigen uptake, while reducing side effects.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biotechnology
Background:
- Lipopeptides show therapeutic promise but face challenges in drug applicability.
- Poloxamers, non-ionic triblock copolymers, offer tunable physico-chemical properties.
- Understanding poloxamer micelle formation and properties is crucial for drug formulation.
Purpose of the Study:
- To investigate the formulation of lipopeptides using poloxamer micelles.
- To evaluate the impact of poloxamers on lipopeptide solubility, stability, and biological activity.
- To optimize lipopeptide drug delivery systems for enhanced therapeutic outcomes.
Main Methods:
- Systematic investigation of poloxamer critical micelle concentration (CMC) at different temperatures and media.
- Cytotoxicity evaluation of poloxamer micelles on various cell lines.
- Formulation of lipopeptide models (antibacterial, anticancer, vaccine antigen) with selected poloxamers, followed by solubility, homogeneity, and particle size analysis using dynamic light scattering (DLS).
Main Results:
- Selected poloxamers (Plur104, Plur123, Plur127) formed stable, reproducible micelles around 20 nm.
- Poloxamer formulation significantly increased lipopeptide solubility and homogeneity, even after freeze-drying.
- Formulated pL1 lipopeptide showed enhanced antibacterial activity and reduced hemolytic effects; pCM15 peptide demonstrated increased tumor cell cytotoxicity; pATIPC peptide exhibited improved cellular uptake.
Conclusions:
- Poloxamers are effective tools for formulating lipopeptides, enhancing their drug applicability.
- Poloxamer micelles improve lipopeptide solubility, stability, and biological efficacy.
- This formulation strategy offers a promising approach for optimizing lipopeptide-based therapeutics and vaccines.
