Stimuli-responsive α-helical peptide gatekeepers for mesoporous silica nanocarriersElectronic supplementary information (ESI) available: Experimental details. See DOI: 10.1039/c7nj00124j

• Main Authors: Lee, Jeonghun, Han, Seungjong, Lee, Jinyoung, Choi, Minhyuek, Kim, Chulhee
• Format: Article
• Language: English
• ISSN: 1144-0546; 1369-9261
• DOI: 10.1039/c7nj00124j

Among the numerous gatekeepers, peptides have attracted much interest due to their specific targeting, cell penetrating, endo-/lysosomal escaping, and enzymatic degrading capabilities. Recently, we developed peptide gatekeepers with turn structures that were triggered to release via stimuli-responsive conformational conversion. In this report, to extend the utilization of stimuli-responsive peptide gatekeepers on the surface of MSNs, we prepared α-helical peptide gatekeepers with a capability for stimuli-responsive conformational conversion on the surface of mesoporous silica nanoparticles. The stimuli-responsive α-helical peptide gatekeepers controlled the release of entrapped drugs triggered by GSH addition and consequential conformational conversion. Furthermore, the nanoparticles efficiently disrupted the liposome membranes. Therefore, stimuli-responsive α-helical peptide gatekeepers would be useful for the construction of mesoporous delivery vehicles with enhanced therapeutic efficacy via membrane disruption. A stimuli-responsive α-helical peptide, as a gatekeeper on the surface of mesoporous silica nanoparticles, efficiently controlled the release of entrapped drugs through triggered conformational conversion and effectively disrupted lipid membranes.