Phthalocyanine-loaded nanostructured lipid carriers functionalized with folic acid for photodynamic therapy

João A Oshiro-Junior, Mariana Rillo Sato, Fernanda Isadora Boni, Karen Loraine Macena Santos, Kleber Thiago de Oliveira, Laura Marise de Freitas, Carla Raquel Fontana, Dean Nicholas, Anthony P. McHale, J Callan, Marlus Chorilli

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Breast cancer is a serious public health problem that causes thousands of deaths annually. Chemotherapy continues to play a central role in the management of breast cancer but is associated with extreme off-target toxicity. Therefore, treatments that directly target the tumor and display reduced susceptibility to resistance could improve the outcome and quality of life for patients suffering from this disease. Photodynamic therapy is a targeted treatment based on the use of light to activate a photosensitizer (PS) that then interacts with molecular oxygen and other biochemical substrates to generate cytotoxic levels of Reactive Oxygen Species. Currently approved PS also tends to have poor aqueous solubility that can cause problems when delivered intravenously. In order to circumvent this limitation, in this manuscript, we evaluate the potential of a phthalocyanine-loaded nanostructured lipid carrier (NLC) functionalized with folic acid (FA). To prepare the FA labelled NLC, the polymer PF127 was first esterified with FA and emulsified with an oil phase containing polyoxyethylene 40 stearate, capric/caprylic acid triglycerides, ethoxylated hydrogenated castor oil 40 and the PS zinc phthalocyanine. The resulting PS loaded FA-NLC had a hydrodynamic diameter of 180 nm and were stable in suspension for >90 days. Interestingly, the amount of singlet oxygen generated upon light activation for the PS loaded FA-NLC was substantially higher than the free PS, yet at a lower PS concentration. The PS was released from the NLC in a sustained manner with 4.13 ± 0.58% and 27.7 ± 3.16% after 30 min and 7 days, respectively. Finally, cytotoxicity assays showed that NLC in the concentrations of 09.1 μM of PS present non-toxic with >80 ± 6.8% viable and after 90 s of the light-exposed the results show a statistically significant decrease in cell viability (57 ± 4%). The results obtained allow us to conclude that the functionalized NLC incorporated with PS associated with the PDT technique have characteristics that make them potential candidates for the alternative treatment of breast cancer.
Original languageEnglish
Number of pages7
JournalMaterials Science and Engineering: C
Issue number110462
Early online date23 Nov 2019
Publication statusPublished (in print/issue) - 31 Mar 2020

Bibliographical note

Funding Information:
This study was financed in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil (CAPES) - Finance Code 001. This study is part of the National Institute of Science and Technology in Pharmaceutical Nanotechnology: a transdisciplinary approach INCT-NANOFARMA, which is supported by São Paulo Research Foundation ( FAPESP , Brazil) Grant # 2014/50928-2 , and by "Conselho Nacional de Desenvolvimento Científico e Tecnológico" ( CNPq , Brazil) Grant # 465687/2014-8 . FAPESP Grant # 2018/17573-7 and 2016/11198-4 and Ulster University .

Publisher Copyright:
© 2019

Copyright 2019 Elsevier B.V., All rights reserved.


  • Nanostructured lipid carriers; Functionalization; Folic acid; Phthalocyanines; Photodynamic therapy; Breast cancer
  • Nanostructured lipid carriers
  • Photodynamic therapy
  • Functionalization
  • Breast cancer
  • Folic acid
  • Phthalocyanines


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