Abstract
Hesperetin is a compound from citrus fruit that has previously been found to exert anticancer activity through a variety of mechanisms. However, the application of hesperetin to cancer therapy has been hampered by its hydrophobicity, necessitating the use of toxic solubilizing agents. Here, we have developed the first liposome-based delivery system for hesperetin. Liposomes were fabricated using the thin-layer evaporation technique and physical and pharmacological parameters were measured. The liposomes remained stable for prolonged periods of time in serum and under storage conditions, and displayed anticancer efficacy in both H441 lung cancer cells and MDA-MB-231 breast cancer cells. Furthermore, the anticancer activity was not impaired in cells expressing the multidrug resistance protein 1 (MDR-1). In conclusion, the encapsulation of hesperetin in liposomes does not interfere with therapeutic efficacy and provides a biocompatible alternative to toxic solubilizing agents, thereby enabling future clinical use of this compound for cancer therapy.
Keywords: Breast cancer, Drug delivery, Flavanone, Lung cancer, MDR-1, Natural products.
Graphical Abstract
Current Drug Delivery
Title:Hesperetin Liposomes for Cancer Therapy
Volume: 13 Issue: 5
Author(s): Joy Wolfram, Bronwyn Scott, Kathryn Boom, Jianliang Shen, Carlotta Borsoi, Krishna Suri, Rossella Grande, Massimo Fresta, Christian Celia, Yuliang Zhao, Haifa Shen and Mauro Ferrari
Affiliation:
Keywords: Breast cancer, Drug delivery, Flavanone, Lung cancer, MDR-1, Natural products.
Abstract: Hesperetin is a compound from citrus fruit that has previously been found to exert anticancer activity through a variety of mechanisms. However, the application of hesperetin to cancer therapy has been hampered by its hydrophobicity, necessitating the use of toxic solubilizing agents. Here, we have developed the first liposome-based delivery system for hesperetin. Liposomes were fabricated using the thin-layer evaporation technique and physical and pharmacological parameters were measured. The liposomes remained stable for prolonged periods of time in serum and under storage conditions, and displayed anticancer efficacy in both H441 lung cancer cells and MDA-MB-231 breast cancer cells. Furthermore, the anticancer activity was not impaired in cells expressing the multidrug resistance protein 1 (MDR-1). In conclusion, the encapsulation of hesperetin in liposomes does not interfere with therapeutic efficacy and provides a biocompatible alternative to toxic solubilizing agents, thereby enabling future clinical use of this compound for cancer therapy.
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Cite this article as:
Wolfram Joy, Scott Bronwyn, Boom Kathryn, Shen Jianliang, Borsoi Carlotta, Suri Krishna, Grande Rossella, Fresta Massimo, Celia Christian, Zhao Yuliang, Shen Haifa and Ferrari Mauro, Hesperetin Liposomes for Cancer Therapy, Current Drug Delivery 2016; 13 (5) . https://dx.doi.org/10.2174/1567201812666151027142412
DOI https://dx.doi.org/10.2174/1567201812666151027142412 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
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