Muehlmann Luis Alexandre, Rodrigues Mosar Corrêa, Longo João Paulo Figueiró, Garcia Mônica Pereira, Py-Daniel Karen Rapp, Veloso Aline Bessa, de Souza Paulo Eduardo Narciso, da Silva Sebastião William, Azevedo Ricardo Bentes
Faculty of Ceilandia, University of Brasilia, Federal District, Brazil.
Department of Genetics and Morphology, Institute of Biological Sciences, University of Brasilia, Federal District, Brazil.
J Nanobiotechnology. 2015 May 13;13:36. doi: 10.1186/s12951-015-0095-3.
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.
The nanoemulsion was developed using castor oil and Cremophor ELP®, 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.
Through the use of spontaneous emulsification, a stable AlPc nanoemulsion was developed that exhibits strong in vitro photodynamic activity on cancer cells.
光动力疗法（PDT）结合光、分子氧和光敏剂，在靶细胞中诱导氧化应激。某些疏水性光敏剂，如氯化铝酞菁（AlPc），在抗肿瘤光动力疗法应用中具有巨大潜力。然而，疏水性分子通常需要药物递送系统，如纳米结构，以改善其药代动力学性质并防止聚集，聚集在水性介质中对光发射性质有猝灭作用。因此，本研究旨在开发并测试纳米乳剂形式的AlPc的功效，以便其用于抗癌光动力疗法。
使用蓖麻油和聚氧乙烯蓖麻油（Cremophor ELP®）制备纳米乳剂，获得了水动力学直径约为25 nm的单分散纳米液滴群体。在体外光动力疗法试验中游离AlPc对人乳腺腺癌MCF-7细胞未显示出显著活性，而纳米乳剂中的AlPc表现出强烈的光动力活性。光活化的AlPc应用于MCF-7细胞单层时，50%细胞毒性浓度（CC50）为6.0 nM，并对MCF-7细胞球体产生强大的细胞毒性作用。
通过自发乳化，开发出了一种稳定的AlPc纳米乳剂，其对癌细胞表现出强大的体外光动力活性。
