NIR-labeled perfluoropolyether nanoemulsions for drug delivery and imaging

Theranostic nanoparticle development recently took center stage in the field of drug delivery nanoreagent design. Theranostic nanoparticles combine therapeutic delivery systems (liposomes, micelles, nanoemulsions, etc.) with imaging reagents (MRI, optical, PET, CT). This combination allows for non-invasive in vivo monitoring of therapeutic nanoparticles in diseased organs and tissues. Here, we report a novel perfluoropolyether (PFPE) nanoemulsion with a water-insoluble lipophilic drug. The formulation enables non-invasive monitoring of nanoemulsion biodistribution using two imaging modalities, 19F MRI and near-infrared (NIR) optical imaging. The nanoemulsion is composed of PFPE-tyramide as a 19F MRI tracer, hydrocarbon oil, surfactants, and a NIR dye. Preparation utilizes a combination of self-assembly and high energy emulsification methods, resulting in droplets with average diameter 180 nm and low polydispersity index (PDI less than 0.2). A model nonsteroidal anti-inflammatory drug (NSAID), celecoxib, was incorporated into the formulation at 0.2 mg/mL. The reported nanoemulsion's properties, including small particle size, visibility under 19F NMR and NIR fluorescence spectroscopy, and the ability to carry drugs make it an attractive potential theranostic agent for cancer imaging and treatment.

Graphical abstractFirst perfluoropolyether (PFPE) nanoemulsion formed by combination of self-assembly and high energy emulsification techniques (sonication and microfluidization), incorporates water insoluble COX-2 inhibitor (celecoxib) and can be detected by two imaging modalities: near-infrared (NIR) and 19F MR.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► The first NIR and 19F NMR detectable nanoemulsion for drug delivery of celecoxib. ► The nanoemulsion loads into fetal skin dendritic cells within 24 h. ► Nanoemulsion droplet mean diameter was 180 nm and PDI was less than 0.2. ► Nanoemulsion remains stable for 30 days at 4 °C.