Aluminium-phthalocyanine chloride nanoemulsions for anticancer photodynamic therapy: Development and in vitro activity against monolayers and spheroids of human mammary adenocarcinoma MCF-7 cells

作者：Muehlmann Luis Alexandre; Rodrigues Mosar Correa; Figueiro Longo Joao Paulo; Garcia Monica Pereira; Py Daniel Karen Rapp; Veloso Aline Bessa; Narciso de Souza Paulo Eduardo; da Silva Sebastiao William; Azevedo Ricardo Bentes^*

来源：Journal of Nanobiotechnology, 2015, 13(1): 36.

DOI：10.1186/s12951-015-0095-3

• Spontaneous emulsification
• Cancer
• Drug delivery systems
• Third-generation photosensitizers
• Human breast adenocarcinoma MCF-7 cells
• Spheroids

Background: Photodynamic therapy (PDT) combines light, molecular oxygen and a photosensitizer to induce oxidative stress in target cells. Certain hydrophobic photosensitizers, such as aluminium-phthalocyanine chloride (AlPc), have significant potential for antitumor PDT applications. However, hydrophobic molecules often require drug-delivery systems, such as nanostructures, to improve their pharmacokinetic properties and to prevent aggregation, which has a quenching effect on the photoemission properties in aqueous media. As a result, this work aims to develop and test the efficacy of an AlPc in the form of a nanoemulsion to enable its use in anticancer PDT.
Results: The nanoemulsion was developed using castor oil and Cremophor ELP (R), and a monodisperse population of nanodroplets with a hydrodynamic diameter of approximately 25 nm was obtained. While free AlPc failed to show significant activity against human breast adenocarcinoma MCF-7 cells in an in vitro PDT assay, the AlPc in the nanoemulsion showed intense photodynamic activity. Photoactivated AlPc exhibited a 50 % cytotoxicity concentration (CC50) of 6.0 nM when applied to MCF-7 cell monolayers and exerted a powerful cytotoxic effect on MCF-7 cell spheroids.
Conclusion: Through the use of spontaneous emulsification, a stable AlPc nanoemulsion was developed that exhibits strong in vitro photodynamic activity on cancer cells.

• 出版日期2015-5-13