中国科学院大学刘勇团队报道了清除葡萄球菌生物膜的三氯生共轭脂肪酶反应聚合物胶束。相关研究成果发表在2024年3月4日出版的《中国高分子科学杂志》。

细菌生物膜在治疗耐药感染方面提出了重大挑战，需要开发创新的纳米药物。

该文中，研究人员介绍了三氯生偶联的脂肪酶响应性聚合物胶束，该胶束旨在利用生物膜特性并作为响应性药物递送平台。使用通过ε-己内酯（CL）和含三氯生的环状碳酸三甲烯酯（MTC-Tri）的开环聚合，合成的两亲性嵌段聚合物制备胶束。聚乙二醇（PEG-OH）作为宏观引发剂，形成具有PEG外壳的胶束，促进其渗透到细菌生物膜中。该胶束的一个重要优势在于它们与生物膜内的局部细菌脂肪酶的相互作用。这些脂肪酶触发了胶束的快速降解，以可控的方式释放出三氯生。这种释放的三氯生有效地消除了嵌入生物膜中的细菌。

值得注意的是，三氯生偶联胶束对小鼠成纤维细胞的毒性最小，表明其生物相容性和安全性。这一发现强调了这些胶束在对抗细菌生物膜中观察到的耐药性方面的潜在应用。三氯生偶联的脂肪酶响应聚合物胶束在解决细菌生物膜中的耐药性方面，表现出了很有前途的特性。通过利用生物膜特性和实施响应性药物递送系统，研究人员寻求为对抗耐药细菌提供了有效的解决方案。

附：原文原文

Title: Triclosan-conjugated, Lipase-responsive Polymeric Micelles for Eradication of Staphylococcal Biofilms

Author: Yan-Qiang Huang, Yuan-Feng Li, Yong Liu, Lin-Qi Shi

Issue&Volume: 2024-03-04

Abstract: Bacterial biofilms present a significant challenge in treating drug-resistant infections, necessitating the development of innovative nanomedicines. In this study, we introduce triclosan-conjugated, lipase-responsive polymeric micelles designed to exploit biofilm properties and serve as a responsive drug delivery platform. The micelles were created using an amphiphilic block polymer synthesized via ring-opening polymerization of ε-caprolactone (CL) and triclosan-containing cyclic trimethylene carbonate (MTC-Tri). Poly(ethylene glycol) (PEG-OH) acted as the macro-initiator, resulting in micelles with a PEG shell that facilitated their penetration into bacterial biofilms. An important advantage of our micelles lies in their interaction with local bacterial lipases within biofilms. These lipases triggered rapid micelle degradation, releasing triclosan in a controlled manner. This liberated triclosan effectively eliminated bacteria embedded in the biofilms. Notably, the triclosan-conjugated micelles displayed minimal toxicity to murine fibroblasts, indicating their biocompatibility and safety. This finding emphasizes the potential application of these micelles in combatting drug resistance observed in bacterial biofilms. Our triclosan-conjugated, lipase-responsive polymeric micelles exhibit promising characteristics for addressing drug resistance in bacterial biofilms. By harnessing biofilm properties and implementing a responsive drug delivery system, we seek to provide an effective solution in the fight against drug-resistant bacteria.

DOI: 10.1007/s10118-024-3094-8

Source: https://www.cjps.org/en/article/doi/10.1007/s10118-024-3094-8/