Light controlled drug-based supramolecular polymer self-assemblies for efficient antibacterial manipulation

Chengfei Liu , Zuoting Yang , Xin Song, Yongchao Qian, Hongbin Huo, Jia He, JuAn Zhang, Zhelin Zhang, Menghan Shi, Jun Pang, Baoliang Zhang, Wei Tian
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Abstract

The infections and diseases caused by harmful bacteria are regarded as the worldwide health-threatening issue. The most antibiotics-based delivery systems restricted the controlled drug release at specific infection sites due to the stable chemical conjugation, thus largely compromising the treatment effectiveness. Herein, we report the construction of light controlled drug-based supramolecular polymer (LDSP), which is endowed the “switch on” function for realizing the controllable antibiotics released in specific sites. LDSP was first formed based on the host-guest interaction between β-cyclodextrin units grafted hyaluronic acid chain (HA-CD) and azobenzene moiety linked by two enoxacin units (Azo-(Eno)2), and could further self-assemble into light controlled drug-based supramolecular polymer self-assemblies (LDSPSAs). Under the UV light irradiation, the “switch on” function of LDSPSAs could be effectively turned on at the specific infected tissues due to the smartly dissociated host-guest interaction, facilitating the controlled release of the hydrophobic Azo-(Eno)2 to interact with bacteria for efficient antibacterial effect. The biological evaluation demonstrated that LDSPSAs achieved good antibacterial efficiency and well biosafety.

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用于高效抗菌操作的光控药物基超分子聚合物自组装
有害细菌引起的感染和疾病被认为是世界性的健康威胁问题。大多数基于抗生素的给药系统由于其稳定的化学偶联而限制了药物在特定感染部位的受控释放,从而在很大程度上影响了治疗效果。本文报道了光控药物基超分子聚合物(LDSP)的构建,该聚合物具有“开关”功能,可实现抗生素在特定位点的可控释放。LDSP最初是基于接枝透明质酸链(HA-CD)的β-环糊精单元和由两个依诺沙星单元(Azo-(Eno)2)连接的偶氮苯段之间的主客体相互作用而形成的,并且可以进一步自组装成光控药物基超分子聚合物自组装体(LDSPSAs)。在紫外光照射下,LDSPSAs的“开关”功能可在特定感染组织上有效开启,通过巧妙解离主客体相互作用,促进疏水偶氮-(Eno)2的可控释放,与细菌相互作用,达到有效的抗菌效果。生物学评价表明,ldspsa具有良好的抗菌效果和生物安全性。
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