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Formulation and Optimization of Idarubicin Thermosensitive Liposomes Provides Ultrafast Triggered Release at Mild Hyperthermia and Improves Tumor Response by Tao Lu; Wouter J.M. Lokerse; Ann L.B. Seynhaeve; Gerben A. Koning; Timo L.M. ten Hagen is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Formulation and Optimization of Idarubicin Thermosensitive Liposomes Provides Ultrafast Triggered Release at Mild Hyperthermia and Improves Tumor Response about?
Drug delivery through thermosensitive liposomes (TSL) in combination with hyperthermia (HT) has shown great potential. HT can be applied locally forcing TSL to release their content in the heated tumor resulting in high peak concentrations. To perform optimally the drug is ideally released fast (seconds) and taken up rapidly by tumor cells. The aim of this study was to develop a novel thermosensitive liposome formulation of the anthracycline idarubicin (IDA-TSL). The hydrophobicity of idarubicin may improve its release from liposomes and subsequently rapid cellular uptake when combined mild hyperthermia. Here, we investigated a series of parameters to optimize IDA-TSL formulation. The results show that the optimal formulation for IDA-TSL is DPPC/DSPC/DSPE-PEG (6/3.5/0.5 mol%), with ammonium EDTA of 6.5 pH as loading buffer and a size of ~85 nm. In vitro studies demonstrated minimal leakage of ~20% in FCS at 37 °C for 1h, while an ultrafast and complete triggered release of IDA was observed at 42 °C. On tumor cells IDA-TSL showed comparable cytotoxicity to free IDA at 42 °C, but low cytotoxicity at 37 °C. Intravital microscopy imaging demonstrated an efficient in vivo intravascular
Who reads Formulation and Optimization of Idarubicin Thermosensitive Liposomes Provides Ultrafast Triggered Release at Mild Hyperthermia and Improves Tumor Response?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Tao Lu; Wouter J.M. Lokerse; Ann L.B. Seynhaeve; Gerben A. Koning; Timo L.M. ten Hagen
- Publisher
- Elsevier BV
- Published
- 2015
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)