Nanoemulsion-based delivery of fluorescent PARP inhibitors in mouse models of small cell lung cancer

Junior Gonzales, Susanne Kossatz, Sheryl Roberts, Giacomo Pirovano, Christian Brand, Carlos Pérez-Medina, Patrick Donabedian, M. Jason de la Cruz, Willem J.M. Mulder, Thomas Reiner

Research output: Contribution to journalArticleAcademicpeer-review

9 Citations (Scopus)
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The preclinical potential of many diagnostic and therapeutic small molecules is limited by their rapid washout kinetics and consequently modest pharmacological performances. In several cases, these could be improved by loading the small molecules into nanoparticulates, improving blood half-life, in vivo uptake and overall pharmacodynamics. In this study, we report a nanoemulsion (NE) encapsulated form of PARPi-FL. As a proof of concept, we used PARPi-FL, which is a fluorescently labeled sensor for olaparib, a FDA-approved small molecule inhibitor of the nuclear enzyme poly(ADP-ribose)polymerase 1 (PARP1). Encapsulated PARPi-FL showed increased blood half-life, and delineated subcutaneous xenografts of small cell lung cancer (SCLC), a fast-progressing disease where efficient treatment options remain an unmet clinical need. Our study demonstrates an effective method for expanding the circulation time of a fluorescent PARP inhibitor, highlighting the pharmacokinetic benefits of nanoemulsions as nanocarriers and confirming the value of PARPi-FL as an imaging agent targeting PARP1 in small cell lung cancer.

Original languageEnglish
Pages (from-to)3776-3782
Number of pages7
JournalBioconjugate Chemistry
Issue number11
Publication statusPublished - 21 Nov 2018


  • Animals
  • Antineoplastic Agents/administration & dosage
  • Cell Line, Tumor
  • Disease Models, Animal
  • Emulsions/chemistry
  • Female
  • Fluorescent Dyes/administration & dosage
  • Humans
  • Lung Neoplasms/drug therapy
  • Mice
  • Mice, Nude
  • Nanostructures/chemistry
  • Pharmaceutical Vehicles/chemistry
  • Phthalazines/administration & dosage
  • Piperazines/administration & dosage
  • Poly (ADP-Ribose) Polymerase-1/antagonists & inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors/administration & dosage
  • Small Cell Lung Carcinoma/drug therapy


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