Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing
The aim of the research is to increase the applicability of lipopeptides as drugs. To this end, non-ionic triblock copolymers, namely poloxamers, were applied. The physico-chemical properties of poloxamers vary depending on the length of the blocks. In our study, we experimented with different types...
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| Format: | Article |
| Language: | English |
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Elsevier
2024-12-01
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| Series: | Journal of Pharmaceutical Analysis |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2095177924001175 |
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| author | Ágnes Ábrahám Gergő Gyulai Judith Mihály Andrea Horváth Orsolya Dobay Zoltán Varga Éva Kiss Kata Horváti |
| author_facet | Ágnes Ábrahám Gergő Gyulai Judith Mihály Andrea Horváth Orsolya Dobay Zoltán Varga Éva Kiss Kata Horváti |
| author_sort | Ágnes Ábrahám |
| collection | DOAJ |
| description | The aim of the research is to increase the applicability of lipopeptides as drugs. To this end, non-ionic triblock copolymers, namely poloxamers, were applied. The physico-chemical properties of poloxamers vary depending on the length of the blocks. In our study, we experimented with different types and systematically investigated the variation of the critical micelle concentration (CMC) of poloxamers at 25 and 37 °C in different media. In addition, the cytotoxicity of the different poloxamer micelles on three different cell lines was evaluated, and based on the results, Plur104, Plur123, and Plur127 were selected. Fatty acid elongated derivatives of a short antibacterial peptide (pL1), a medium-sized anticancer peptide (pCM15), and a branched-chain vaccine antigen (pATIPC) were used as lipopeptide models, and their formulations with the selected poloxamers were investigated. The solubility and homogeneity of the lipopeptides were significantly increased, and dynamic light scattering (DLS) measurements showed the formation of small particles of around 20 nm, which were well reproducible and storable. Similar homogenous micelle formation was observed after freeze-drying and reconstitution with water. The pL1 lipopeptide, formulated with the selected poloxamers, exhibited enhanced antibacterial activity with significantly reduced haemolytic side effects. The pCM15 peptide, when incorporated into poloxamer micelles, showed significantly enhanced cytotoxicity against tumor cells. Additionally, the internalization rate of poloxamer-formulated pATIPC peptide by antigen-presenting model cells exceeded that of the unformulated peptide. Our results demonstrate the potential of poloxamers as promising tools for the formulation of lipopeptides and for the optimization of their selectivity. |
| format | Article |
| id | doaj-art-947aba583b3b45528818054456b0e38a |
| institution | Kabale University |
| issn | 2095-1779 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmaceutical Analysis |
| spelling | doaj-art-947aba583b3b45528818054456b0e38a2025-01-30T05:13:58ZengElsevierJournal of Pharmaceutical Analysis2095-17792024-12-011412101020Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressingÁgnes Ábrahám0Gergő Gyulai1Judith Mihály2Andrea Horváth3Orsolya Dobay4Zoltán Varga5Éva Kiss6Kata Horváti7MTA-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; Laboratory of Interfaces and Nanostructures, Institute of Chemistry, Eötvös Loránd University, Budapest, H-1117, HungaryMTA-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; Laboratory of Interfaces and Nanostructures, Institute of Chemistry, Eötvös Loránd University, Budapest, H-1117, HungaryHUN-REN TTK Biological Nanochemistry Research Group, Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences, Budapest, H-1117, HungaryInstitute of Medical Microbiology, Semmelweis University, Budapest, H-1085, HungaryInstitute of Medical Microbiology, Semmelweis University, Budapest, H-1085, HungaryHUN-REN TTK Biological Nanochemistry Research Group, Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences, Budapest, H-1117, Hungary; Department of Physical Chemistry and Materials Science, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Budapest, H-1111, HungaryLaboratory of Interfaces and Nanostructures, Institute of Chemistry, Eötvös Loránd University, Budapest, H-1117, HungaryMTA-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; Corresponding author.The aim of the research is to increase the applicability of lipopeptides as drugs. To this end, non-ionic triblock copolymers, namely poloxamers, were applied. The physico-chemical properties of poloxamers vary depending on the length of the blocks. In our study, we experimented with different types and systematically investigated the variation of the critical micelle concentration (CMC) of poloxamers at 25 and 37 °C in different media. In addition, the cytotoxicity of the different poloxamer micelles on three different cell lines was evaluated, and based on the results, Plur104, Plur123, and Plur127 were selected. Fatty acid elongated derivatives of a short antibacterial peptide (pL1), a medium-sized anticancer peptide (pCM15), and a branched-chain vaccine antigen (pATIPC) were used as lipopeptide models, and their formulations with the selected poloxamers were investigated. The solubility and homogeneity of the lipopeptides were significantly increased, and dynamic light scattering (DLS) measurements showed the formation of small particles of around 20 nm, which were well reproducible and storable. Similar homogenous micelle formation was observed after freeze-drying and reconstitution with water. The pL1 lipopeptide, formulated with the selected poloxamers, exhibited enhanced antibacterial activity with significantly reduced haemolytic side effects. The pCM15 peptide, when incorporated into poloxamer micelles, showed significantly enhanced cytotoxicity against tumor cells. Additionally, the internalization rate of poloxamer-formulated pATIPC peptide by antigen-presenting model cells exceeded that of the unformulated peptide. Our results demonstrate the potential of poloxamers as promising tools for the formulation of lipopeptides and for the optimization of their selectivity.http://www.sciencedirect.com/science/article/pii/S2095177924001175LipopeptidePluronicPoloxamerMulti-epitope vaccineAntimicrobial peptide |
| spellingShingle | Ágnes Ábrahám Gergő Gyulai Judith Mihály Andrea Horváth Orsolya Dobay Zoltán Varga Éva Kiss Kata Horváti Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing Journal of Pharmaceutical Analysis Lipopeptide Pluronic Poloxamer Multi-epitope vaccine Antimicrobial peptide |
| title | Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing |
| title_full | Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing |
| title_fullStr | Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing |
| title_full_unstemmed | Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing |
| title_short | Optimizing lipopeptide bioactivity: The impact of non-ionic surfactant dressing |
| title_sort | optimizing lipopeptide bioactivity the impact of non ionic surfactant dressing |
| topic | Lipopeptide Pluronic Poloxamer Multi-epitope vaccine Antimicrobial peptide |
| url | http://www.sciencedirect.com/science/article/pii/S2095177924001175 |
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