Lipiodol-based anti-tumour emulsion for treating cancer
Inventors
Guiu, Boris • Boulin, Mathieu • Cercueil, Jean-Pierre
Assignees
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Publication Number
US-10064883-B2
Publication Date
2018-09-04
Expiration Date
Abstract
The present invention relates to a pharmaceutical composition including Lipiodol and a molecule with anti-tumor activity and secondarily a hydroxyethyl starch. The present invention also relates to the use of the compositions according to the invention for treating cancer. According to one embodiment, the pharmaceutical composition according to the invention has between 0.004% and 0.2% by weight of idarubicin, between 0.38% and 2.25% by weight of hydroxyethyl starch and secondarily between 60% and 68% by weight of Lipiodol, and water for injection (or even physiological saline) in a quantity sufficient (q.s.) for 100%.
Core Innovation
The invention relates to a Lipiodol-based water-in-oil pharmaceutical emulsion comprising Lipiodol, a molecule with anti-tumour activity, and hydroxyethyl starch, and provides a formulation intended for cancer therapy. The composition is described as yielding a stable emulsion and advantageous pharmacokinetics, with emphasis on primary liver cancer and hepatic intra-arterial chemoembolisation.
The emulsion is described with particular emphasis on idarubicin as the anti-tumour molecule, including the context that the idarubicin/Lipiodol formulation forms small micelles in the range of about 20–100 μm. Compared to a prior formulation involving Lipiodol and doxorubicin, the document reports improved emulsion stability and reduced systemic exposure, including measured Cmax and AUC in patients.
The document further specifies preferred Lipiodol grades, including Lipiodol Ultra-Fluide and Ethiodol, and hydroxyethyl starch properties, including molecular weight and molar substitution ratio, as part of the formulation design. Example data are described for emulsion stability and micelle size, and non-clinical context is provided using CHC cell lines including HepG2, SNU-398, and SNU-449.
Claims Coverage
The independent claim covers a pharmaceutical composition comprising an emulsion of Lipiodol with a molecule with anti-tumour activity and hydroxyethyl starch. The inventive coverage is further defined by specific concentration ranges, by hydroxyethyl starch properties, by specifying Idarubicin as an example anti-tumour molecule, and by a contacting preparation method.
Lipiodol emulsion with anti-tumour activity and hydroxyethyl starch
A pharmaceutical composition comprising an emulsion of Lipiodol with a molecule with anti-tumour activity and hydroxyethyl starch.
Concentration range for anti-tumour activity molecule
The amount of a molecule with anti-tumour activity is between 0.004% and 0.2% (mass/volume) of the total volume of the preparation.
Hydroxyethyl starch concentration range
Hydroxyethyl starch is present at 0.38% to 2.25% (mass/volume) of the total preparation volume.
Lipiodol concentration range
The Lipiodol content is between 50% and 70% (mass/volume) relative to the total volume of the preparation.
Idarubicin as the anti-tumour molecule
The anti-tumour-active molecule is Idarubicin.
Preparing by contacting components
A method for preparing the composition by contacting Lipiodol, the antitumor-active molecule, and hydroxyethyl starch.
The core inventive subject matter is a Lipiodol emulsion including an anti-tumour-active molecule and hydroxyethyl starch, further constrained by specific concentration ranges and supported by specifying Idarubicin and a contacting preparation method.
Stated Advantages
Provides a stable emulsion with advantageous pharmacokinetics.
Improved emulsion stability compared to a prior Lipiodol/doxorubicin formulation.
Reduced systemic Idarubicin exposure in patients, including reduced measured Cmax and AUC.
Documented Applications
Cancer therapy using a Lipiodol-based emulsion, with emphasis on primary liver cancer.
Hepatic intra-arterial chemoembolisation using the Lipiodol-based pharmaceutical emulsion.
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