| 1 | An acid-triggered porphyrin-based block copolymer for enhanced photodynamic antibacterial efficacy显示文摘Bacterial infection, especially multidrug-resistant(MDR) bacterial infection has threatened public health drastically. Here, we fabricate an 'acid-triggered' nanoplatform for enhanced photodynamic antibacterial activity by reducing the aggregation of photosensitizers(PSs) in bacterial acidic microenvironment. Specifically, a functional amphiphilic block copolymer was first synthesized by using a pH-sensitive monomer, 2-(diisopropylamino) ethyl methacrylate(DPA) and porphyrin-based methacrylate(TPPC6MA) with poly(oligo(ethylene glycol) methyl ether methacrylate)(POEGMA) as the macromolecular chain transfer agent, and POEGMA-b-[PDPA-co-PTPPC6MA] block copolymer was further self-assembled into spherical nanoparticles(PDPA-TPP). PDPA-TPP nanoparticles possess an effective electrostatic adherence to negatively charged bacterial cell membrane, since they could rapidly achieve positive charge in acidic bacterial media. Meanwhile, the acid-triggered dissociation of PDPA-TPP nanoparticles could reduce the aggregation caused quenching(ACQ) of the photosensitizers, leading to around 5 folds increase of the singlet oxygen(1O2) quantum yield. In vitro results demonstrated that the 'acid-triggered' PDPA-TPP nanoparticles could kill most of MDR S. aureus(Gram-positive) and MDR E. coli(Gram-negative) by enhanced photodynamic therapy, and they could resist wound infection and accelerate wound healing effectively in vivo. Furthermore, PDPA-TPP nanoparticles could well disperse the biofilm and almost kill all the biofilm-containing bacteria. Thus, by making use of the bacterial acidic microenvironment, this 'acid-triggered' nanoplatform in situ will open a new path to solve the aggregation of photosensitizers for combating broad-spectrum drug-resistant bacterial infection. | Fan Yu Chao Chen Guoliang Yang Zhengtong Ren Hongliang Cao Liangshun Zhang Weian Zhang | 2021 | Science China Chemistry2021，64，3： | 2 |
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