Hesperetin Liposomes for Cancer Therapy

• Published in: Current drug delivery Vol. 13; no. 5; p. 711
• Main Authors: Wolfram, Joy, Scott, Bronwyn, Boom, Kathryn, Shen, Jianliang, Borsoi, Carlotta, Suri, Krishna, Grande, Rossella, Fresta, Massimo, Celia, Christian, Zhao, Yuliang, Shen, Haifa, Ferrari, Mauro
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01-01-2016
• Subjects: Antineoplastic Agents, Phytogenic - administration & dosage; Antineoplastic Agents, Phytogenic - chemistry; Antineoplastic Agents, Phytogenic - pharmacology; ATP Binding Cassette Transporter, Subfamily B - genetics; ATP Binding Cassette Transporter, Subfamily B - metabolism; Breast Neoplasms - drug therapy; Breast Neoplasms - genetics; Breast Neoplasms - metabolism; Breast Neoplasms - pathology; Cell Line, Tumor; Cell Survival - drug effects; Cholesterol - chemistry; Drug Compounding; Drug Resistance, Neoplasm; Female; Hesperidin - administration & dosage; Hesperidin - chemistry; Hesperidin - pharmacology; Humans; Kinetics; Liposomes; Lung Neoplasms - drug therapy; Lung Neoplasms - pathology; Phosphatidylcholines - chemistry; Polyethylene Glycols - chemistry; Solubility; Transfection
• ISSN: 1875-5704
• DOI: 10.2174/1567201812666151027142412

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.