Matrix mediated fluorescence enhancement — why nanoparticles and PPIX make a friendly couple

Abstract

The hexyl ester of 5-aminolevulinic acid (HAL) is an efficient inducer of the endogenous photosensitizer protoporphyrin IX (PPIX) in neoplastic tissue and approved for the fluorescence photodetection of bladder cancer. It is, however, limited to topical application due to unsuitable pharmacokinetic and pharmacodynamic properties following systemic administration. In this study we sought to prepare HAL laden polymeric nanoparticles made from polylactic acid (PLA) as possible means to improve the systemic bioavailability of HAL. Nanoparticles were prepared by nanoprecipitation. Particle size and morphology of freshly prepared and dehydrated nanoparticles were assessed and the ability to generate PPIX fluorescence was tested on a T24 human bladder carcinoma cell line. Fluorescence intensities of cells incubated with nanoencapsulated HAL were significantly higher than in presence of free HAL. Interestingly, the effect was — at least partly — provoked by the direct interaction of exogenously induced PPIX with the nanoparticles.