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Issue 21, 2013
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Hypericin-loaded lipid nanocapsules for photodynamic cancer therapy in vitro

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Hypericin (Hy), a naturally occurring photosensitizer (PS), is extracted from Hypericum perforatum plants, commonly known as St. John's wort. The discovery of the in vitro and in vivo photodynamic activities of hypericin as a photosensitizer generated great interest, mainly to induce a very potent antitumoral effect. However, this compound belongs to the family of naphthodianthrones which are known to be poorly soluble in physiological solutions and produce non-fluorescent aggregates (A. Wirz et al., Pharmazie, 2002, 57, 543; A. Kubin et al., Pharmazie, 2008, 63, 263). These phenomena can reduce its efficiency as a photosensitizer for the clinical application. In the present contribution, we have prepared, characterized, and studied the photochemical properties of Hy-loaded lipid nanocapsule (LNC) formulations. The amount of singlet oxygen (1O2) generated was measured by the use of p-nitroso-dimethylaniline (RNO) as a selective scavenger under visible light irradiation. Our results showed that Hy-loaded LNCs suppressed aggregation of Hy in aqueous media, increased its apparent solubility, and enhanced the production of singlet oxygen in comparison with free drug. Indeed, encapsulation of Hy in LNCs led to an increase of 1O2 quantum yield to 0.29–0.44, as compared to 0.02 reported for free Hy in water. Additionally, we studied the photodynamic activity of Hy-loaded LNCs on human cervical carcinoma (HeLa) and Human Embryonic Kidney (HEK) cells. The cell viability decreased radically to 10–20% at 1 μM, reflecting Hy-loaded LNC25 phototoxicity.

Graphical abstract: Hypericin-loaded lipid nanocapsules for photodynamic cancer therapy in vitro

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The article was received on 25 May 2013, accepted on 20 Aug 2013 and first published on 23 Aug 2013

Article type: Paper
DOI: 10.1039/C3NR02724D
Citation: Nanoscale, 2013,5, 10562-10572
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    Hypericin-loaded lipid nanocapsules for photodynamic cancer therapy in vitro

    A. Barras, L. Boussekey, E. Courtade and R. Boukherroub, Nanoscale, 2013, 5, 10562
    DOI: 10.1039/C3NR02724D

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