Controlling the function of bioactive worm micelles by enzyme-cleavable non-covalent inter-assembly cross-linking
| dc.contributor.author | Romanovska, Alina | |
| dc.contributor.author | Schmidt, Martin | |
| dc.contributor.author | Brandt, Volker | |
| dc.contributor.author | Tophoven, Jonas | |
| dc.contributor.author | Tiller, Joerg C. | |
| dc.date.accessioned | 2025-12-17T07:39:57Z | |
| dc.date.available | 2025-12-17T07:39:57Z | |
| dc.date.issued | 2024-02-21 | |
| dc.description.abstract | Drugs that form self-assembled supramolecular structures to be most-active is a promising way of creating new highly specific and active pharmaceuticals. Controlling the activity of bioactive supramolecular structures such as drug-loaded micelles is possible by both core/shell and inter-assembly cross-linking. However, if the flexibility of the assembly is mandatory for the activity cross-linking is not feasible. Thus, such structures cannot be manipulated in their activity. The present study demonstrates a novel concept to control the activity of not drug-releasing, non-cross-linked bioactive superstructures. This is achieved by formation of nanostructured nanoparticles derived by non-covalent inter-assembly cross-linking of the superstructures. This is shown on the example of amphiphilic diblock-copolymers conjugated with the antibiotic ciprofloxacin (CIP). These polymer-antibiotic conjugates form worm micelles, which greatly activate the conjugated antibiotic without releasing it. Non-covalent inter-assembly cross-linking of these CIP-worm-micelles with amphiphilic triblock copolymers terminated with lipase-cleavable esters leads to nanostructured nanoparticles that resemble cross-linked worm micelles and show an up to 135-fold lower activity than the free worm micelles. The activity of the worm-micelles can be fully recovered by cleaving the end groups of the polymeric cross-linker with lipase. | en |
| dc.identifier.uri | http://hdl.handle.net/2003/44560 | |
| dc.language.iso | en | |
| dc.relation.ispartofseries | Journal of controlled release; 368 | |
| dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
| dc.subject | Polymer antibtiotic conjugate | en |
| dc.subject | Ciprofloxacin | en |
| dc.subject | Cross-linked micelles | en |
| dc.subject | Lipase-induced release | en |
| dc.subject | Poly(2-oxazoline) | en |
| dc.subject.ddc | 660 | |
| dc.title | Controlling the function of bioactive worm micelles by enzyme-cleavable non-covalent inter-assembly cross-linking | en |
| dc.type | Text | |
| dc.type.publicationtype | Article | |
| dcterms.accessRights | open access | |
| eldorado.dnb.deposit | true | |
| eldorado.doi.register | false | |
| eldorado.secondarypublication | true | |
| eldorado.secondarypublication.primarycitation | Alina Romanovska, Martin Schmidt, Volker Brandt, Jonas Tophoven, Joerg C. Tiller, Controlling the function of bioactive worm micelles by enzyme-cleavable non-covalent inter-assembly cross-linking, Journal of Controlled Release, Volume 368, 2024, Pages 15-23, https://doi.org/10.1016/j.jconrel.2024.02.013 | |
| eldorado.secondarypublication.primaryidentifier | https://doi.org/10.1016/j.jconrel.2024.02.013 |
