广东药科大学学报2025，Vol.41Issue(3)：11-18,8.DOI:10.16809/j.cnki.2096-3653.2025031303
具有信号开关功能的塞来昔布脂质纳米粒荧光探针的制备及评价
Design and functional evaluation of a signal-switchable fluorescent probe for celecoxib-loaded lipid nanoparticles
摘要
Abstract
Objective To develop a signal-switchable fluorescent probe for tracking the in vivo fate of celecoxib-loaded lipid nanoparticles,offering insights for nanomedicine delivery system research.Methods The Aza-Boron Dipyrromethene(Aza-BODIPY)fluorescent dye was synthesized using a literature-based synthetic method.Its structure was characterized by high-resolution mass spectrometry(HRMS)and liquid nuclear magnetic resonance(NMR).The optical properties were evaluated using ultraviolet-visible(UV-Vis)spectrophotometry and fluorescence spectrophotometry.The cytotoxicity and biocompatibility of Aza-BODIPY toward MDCK cells were assessed via the CCK-8 assay and in vitro hemolysis experiments,respectively.Aza-BODIPY-loaded Celecoxib lipid nanoparticles were prepared using a microfluidic jetting process,and their appearance,particle size,zeta potential,drug release profile,and consistency between drug release and fluorescence intensity changes were systematically characterized.Results The target product,Aza-BODIPY dye,was successfully synthesized.It exhibited a maximum excitation wavelength(λex)of 648 nm and a maximum emission wavelength(λem)of 671 nm.Aza-BODIPY was an aggregation-induced quenching(ACQ)-type fluorescent dye with excellent aqueous quenching performance.Fluorescence signal"on-off"switching occured(i.e.,fluorescence quenching)when the water content in the solvent system reached 70%.The Aza-BODIPY dye demonstrated good biocompatibility:at a concentration of 20 μg/mL,cell viability remained above 95%,and the in vitro hemolysis rate was below 5%.The prepared fluorescent probe-loaded Celecoxib lipid nanoparticle system displayed stable properties,presenting as a green milky liquid with a uniform spherical morphology under transmission electron microscopy(TEM).Drug release exhibited high synchronization with the release of the Aza-BODIPY fluorescent dye.Conclusion The Celecoxib lipid nanoparticle fluorescent probe possesses a signal-switching capability,where changes in fluorescence intensity accurately reflect alterations in the structural integrity of the nanoparticles.This property enables its application in studying their in vivo fate.关键词
氮杂硼二吡咯亚甲基/聚集诱导淬灭/塞来昔布脂质纳米粒/荧光探针Key words
Aza-BODIPY/ACQ/CXB-LNP/fluorescent probe分类
药学引用本文复制引用
刘宗明,何桦燊,梁苑雯,巢颖松,彭智轩,班俊峰,李晓芳..具有信号开关功能的塞来昔布脂质纳米粒荧光探针的制备及评价[J].广东药科大学学报,2025,41(3):11-18,8.基金项目
广东省医学科学技术研究基金项目(A2023258) （A2023258）
