PLGA封装GE11肽偶联锌酞菁纳米光敏剂的制备及体外生物评价OA

Phthalocyanine photosensitizers with high molar extinction coefficients and a biological therapeutic window,exhibit great PDT potential.However,their planar conjugated structure causes hydrophobicity,leading to aggregation in aqueous systems and low tissue-targeting selectivity,limited tumor accumulation and potential healthy tissue damage.To overcome these limitations,this study conjugated 1-sulfonatophenoxy zinc phthalocyanine(ZnPcS)with the GE11 peptide and encapsulated poly(lactic-co-glycolic acid)(PLGA)to form the nanophotosensitizer(PLGA@GE11-ZnPcS).This study used NMR,FT-IR,UV-Vis,etc.to validate the molecular structure,optical properties,nanoparticle size and distribution.Electron paramagnetic resonance(EPR)and 1,3-diphenylisobenzofuran(DPBF)assays evaluated the singlet oxygen generation.PLGA@GE11-ZnPcS showed good water solubility,efficient light activation and outstanding singlet oxygen generation ability.In vitro cell tests indicated good cell compatibility in the dark and remarkable photodynamic anti-tumor activity upon light irradiation.Hemolysis tests verified that the nanophotosensitizer caused no red blood cell hemolysis,indicating in-vivo safety.In conclusion,PLGA@GE11-ZnPcS showed high biosafety and anti-tumor activity,making it a promising candidate for photodynamic tumor therapy and potential drug-resistant bacteria sterilization.However,the high synthesis cost and poor physiological stability of the GE11 peptide currently limit its widespread use in tumor therapy.