Abstract
Infection-controlled release of antibacterial agents is of great importance, particularly for the control of peri-implant infections in the postoperative phase. Polymers containing antibiotics bound via enzymatically cleavable linkers could provide access to drug release systems that could accomplish this. Dispersions of nanogels were prepared by ionotropic gelation of alginate with poly-l-lysine, which was conjugated with ciprofloxacin as model drug via a copper-free 1,3-dipolar cycloaddition (click reaction). The nanogels are stable in dispersion and form films which are stable in aqueous environments. However, both the nanogels and the layers are degraded in the presence of an enzyme and the ciprofloxacin is released. The efficacy of the released drug against Staphylococcus aureus is negatively affected by the residues of the linker. Both the acyl modification of the amine nitrogen in ciprofloxacin and the sterically very demanding linker group with three annellated rings could be responsible for this. However the basic feasibility of the principle for enzyme-triggered release of drugs was successfully demonstrated.
Highlights
Drug delivery systems based on hydrogel micro- and nanoparticles are of particular interest because of their good biocompatibility and good compatibility even with sensitive active ingredients such as therapeutic proteins [1,2]
The retention of the model protein interferon β was limited and a strong burst release was observed [32]. Based on these promising results and in an effort to address the main drawback of unspecific burst release, this study presents a new enzyme-responsive alginate/peptide nanogel, in which the model drug ciprofloxacin is conjugated to the Antibiotics 2021, 10, 653
The results clearly demonstrated the intrinsic capabilities of the systems for application as triggered release systems for antibacterial agents
Summary
Drug delivery systems based on hydrogel micro- and nanoparticles are of particular interest because of their good biocompatibility and good compatibility even with sensitive active ingredients such as therapeutic proteins [1,2]. Lipophilic drugs are encapsulated into the polymer matrix, and hydrophilic compounds are adsorbed at the particle’s surface or within the nanogels For both systems, the release in a targeted tissue occurs through the processes of diffusion and degradation. The retention of the model protein interferon β was limited and a strong burst release was observed [32] Based on these promising results and in an effort to address the main drawback of unspecific burst release, this study presents a new enzyme-responsive alginate/peptide nanogel, in which the model drug ciprofloxacin is conjugated to the Antibiotics 2021, 10, 653. Alginate as polyThe aim of the investigation was to find a general synthetic route to conjugate drugs to anion and poly-L-lysine as polycation were chosen as components for the ionotropic gelalinkers suitable for the preparation of nanogels by inotropic gelation. The conjugation was carried out by modification of the piperazine ring
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