Bourgat Yannick, Mikolai Carina, Stiesch Meike, Klahn Philipp, Menzel Henning
Institute for Technical Chemistry, Technische Universität Braunschweig, Hagenring 30, 38106 Braunschweig, Germany.
Department of Prosthetic Dentistry and Biomedical Material Science, Hannover Medical School, Carl-Neuberg-Straße 1, 30625 Hanover, Germany.
Antibiotics (Basel). 2021 May 29;10(6):653. doi: 10.3390/antibiotics10060653.
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 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.
抗菌剂的感染控制释放非常重要，特别是对于术后阶段种植体周围感染的控制。含有通过酶可裂解连接子结合抗生素的聚合物可以提供实现这一目标的药物释放系统。通过藻酸盐与聚-L-赖氨酸的离子凝胶化制备纳米凝胶分散体，聚-L-赖氨酸通过无铜的1,3-偶极环加成反应（点击反应）与作为模型药物的环丙沙星共轭。纳米凝胶在分散体中稳定并形成在水性环境中稳定的薄膜。然而，纳米凝胶和层在酶存在下都会降解，环丙沙星会释放出来。释放的药物对……的功效受到连接子残基的负面影响。环丙沙星中胺氮的酰基修饰和具有三个稠合环的空间位阻非常大的连接子基团都可能对此负责。然而，酶触发药物释放原理的基本可行性已得到成功证明。
