Heparin‐Engineered Mesoporous Iron Metal‐Organic Framework Nanoparticles: Toward Stealth Drug Nanocarriers

作者：Elena Bellido, Tania Hidalgo, M.V. Lozano, Mazheva Guillevic, Rosana Simón‐Vázquez, Manuel Jesús Santander-Ortega, África González‐Fernández, Christian Serre, Marı́a José Alonso, Patricia Horcajada · 发表于：Advanced Healthcare Materials · 年份：2015 · DOI：10.1002/adhm.201400755 · 被引用次数：217 · 研究领域：Metal-Organic Frameworks: Synthesis and Applications、Nanoparticle-Based Drug Delivery、Dendrimers and Hyperbranched Polymers

The specific modification of the outer surface of the promising porous metal-organic framework nanocarriers (nanoMOFs) preserving their characteristic porosity is still a major challenge. Here a simple, fast, and biofriendly method for the external functionalization of the benchmarked mesoporous iron(III) trimesate nanoparticles MIL-100(Fe) with heparin, a biopolymer associated with longer-blood circulation times is reported. First, the coated nanoparticles showed intact crystalline structure and porosity with improved colloidal stability under simulated physiological conditions, preserving in addition its encapsulation and controlled release capacities. The effect of the heparin coating on the nanoMOF interactions with the biological environment is evaluated through cell uptake, cytotoxicity, oxidative stress, cytokine production, complement activation, and protein adsorption analysis. These results confirmed that the heparin coating endowed the nanoMOFs with improved biological properties, such as reduced cell recognition, lack of complement activation, and reactive oxygen species production. Overall, the ability to coat the surface of the nanoMOFs using a simple and straight-forward approach could be taken as a way to enhance the versatility and, thus, the potential of porous MOF nanoparticles in biomedicine.