Hesperetin Liposomes for Cancer Therapy.
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.
Joy
J
Wolfram
Bronwyn
B
Scott
Kathryn
K
Boom
Jianliang
J
Shen
Carlotta
C
Borsoi
Krishna
K
Suri
Rossella
R
Grande
Massimo
M
Fresta
Christian
C
Celia
Yuliang
Y
Zhao
Haifa
H
Shen
Department of Nanomedicine, Houston Methodist Research Institute, R8460-9, 6670 Bertner Ave, Houston, TX 77030, USA. mferrari@houstonmethodist.org.
Mauro
M
Ferrari
D018435:ATP Binding Cassette Transporter, Subfamily B / Q000235:genetics / Q000378:metabolism; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry*; D004339:Drug Compounding; D019008:Drug Resistance, Neoplasm; D005260:Female; D006569:Hesperidin / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008081:Liposomes; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010713:Phosphatidylcholines / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D014162:Transfection
C513055:ABCB1 protein, human; D018435:ATP Binding Cassette Transporter, Subfamily B; D000972:Antineoplastic Agents, Phytogenic; D008081:Liposomes; D010713:Phosphatidylcholines; D011092:Polyethylene Glycols; D002784:Cholesterol; D006569:Hesperidin; C013015:hesperetin