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Liposomes Loaded with Histone Deacetylase Inhibitors for Breast Cancer Therapy by Giorgia Urbinati; Véronique Marsaud; Vincent Plassat; Elias Fattal; Sylviane Lesieur; Jack-Michel Renoir is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

What is Liposomes Loaded with Histone Deacetylase Inhibitors for Breast Cancer Therapy about?

Histone deacetylase (HDAC) inhibitors (HDACi) of the class I trichostatin A (TSA), CG1521 (CG), and PXD101 (PXD) were incorporated at a high rate (∼1 mM) in liposomes made of egg phosphatidylcholine/cholesterol/distearoylphosphoethanolamine-polyethylenglycol 2000 (64:30:6). Physicochemical parameters (size, zeta potential, loading, stability, release kinetics) of these HDACiloaded pegylated liposomes were optimized and their cytotoxicity (MTT test) was measured in MCF-7, T47-D, MDA-MB-231 and SkBr3 breast cancer cell lines. In MCF-7 cells, TSA and PXD were efficient inducers of proteasome-mediated estradiol receptor ␣ degradation and they both affected estradiol-induced transcription (TSA > PXD) contrary to CG. Moreover, TSA most efficiently altered breast cancer cell viability as compared to the free drug, CG-liposomes being the weakest, while unloaded liposomes had nearly no cytotoxicity. Pegylated liposomes loaded with TSA or PXD remained stable in size, charge and biological activity for one month when stored at 4 • C. All HDACi-loaded liposomes released slowly the encapsulated drug in vitro, CG-loaded liposomes showed the slowest release kinetic. These formulations could impro

Who reads Liposomes Loaded with Histone Deacetylase Inhibitors for Breast Cancer Therapy?

Author

Giorgia Urbinati; Véronique Marsaud; Vincent Plassat; Elias Fattal; Sylviane Lesieur; Jack-Michel Renoir

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

2010

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)