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Liposomal glucocorticoids

A technology of glucocorticoids and liposomes, which is applied in liposome delivery, endocrine system diseases, bone diseases, etc., can solve the problems of low stability of preparations, unpopularity, and reduced half-life of circulation, etc. Chemicals and pharmaceuticals, the effect of reducing side effects

Inactive Publication Date: 2006-02-08
NOVOSOM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the disadvantages of the above-mentioned preparations are: the hydrophobic active substance derivatives are exchanged with plasma components, and the preparations have low stability in vivo
Conjugation of antibody to liposomes results in reduced circulating half-life upon repeated use, which is pharmacologically undesirable

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0127] Preparation of liposomes filled with dexamethasone phosphate

[0128] A mixture of 50 mol% DPPC, 10 mol% DPPG and 40 mol% Chol was dissolved in chloroform and then completely dried in a rotary evaporator under vacuum.

[0129] Add dexamethasone phosphate solution (25 mg / ml dexamethasone phosphate in 10 mM HEPES and 150 mM NaCl, pH 7.5) into the liquid film in an amount capable of forming a 100 mM suspension. Next, the suspension was hydrated in a water bath at 50° C. for 45 minutes with shaking, and then treated in an ultrasonic bath for 5 minutes. Thereafter, the solution was frozen.

[0130] After thawing, the liposomes were repeatedly extruded through a membrane with a pore width of 400 nm. Uncoated dexamethasone phosphate was removed by gel filtration.

Embodiment 2

[0132] Determination of Dexamethasone Phosphate Release

[0133]Liposomes were prepared as in Example 1, and diluted with buffer (10 mM HEPES, 150 mM NaCl, pH 7.5) to a concentration of 12 mM lipid. Next, incubate at 37°C. Aliquots of this incubation solution were promptly removed at defined time points (see table below). The content of dexamethasone phosphate in aliquots was determined using RP-HPLC.

[0134] Table 1

[0135] The release of dexamethasone phosphate as a percentage of the coated amount at different times after incubation in buffer at 37°C

[0136] Preparation Lipid mol% 0 hours 24 hours 120 hours

[0137] A DPPC / DPPG / Chol 50:10:40 1.1 6.0 7.3

[0138] Liposomes showed sufficient stability during the assay. In 5 days, less than 8% of the coated active substance was released.

Embodiment 3

[0140] Uses of liposomal dexamethasone phosphate

[0141] According to Buchner method ("Behandlung der antigeninduzierten Arthritisder Ratte mit Anti-Makrophagenprinzipien und monoklonalen Anti-CD4Antikrpern", Ph.D.thesis 1996, Friedrich-Alexander University Erlangen-Nuremberg, Germany, p.129), in test animals (rats ) to produce antigen-induced arthritis.

[0142] Antigen was injected into the synovial fluid of the right knee by intra-articular injection according to the Buchner method, and arthritis was induced on day 0. Arthritic animals were treated with intravenous injection of liposomal dexamethasone phosphate (Formulation A, 3.75 mg / kg) at 6, 24 and 48 hours after arthritis induction. Free dexamethasone phosphate (formulation K, also 3.75 mg / kg) and saline solution (saline) served as controls. The following parameters were used to establish the effect of sample administration.

[0143] - Determination of joint swelling (cf., figure 1 )

[0144] - parameters of hist...

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Abstract

The invention relates to a liposomal formulation comprising water-soluble glucocorticoids, the use of said formulation for treating inflammatory diseases, and a kit containing the liposomal formulation, e.g. as a pharmaceutical agent.

Description

technical field [0001] The present invention relates to a liposome preparation comprising a water-soluble glucocorticoid, the invention also relates to the use of the preparation in the treatment of inflammatory diseases, and also relates to a kit comprising the liposome preparation in the form of a medicament. Background technique [0002] Glucocorticoids are a class of substances that have long been used to treat inflammatory diseases. The formulation of active substances of this class into liposomal formulations is known in principle and mentioned several times. Preparation of unmodified pharmaceutical dosage forms is very difficult because the encapsulated material in liposomes is re-released within a few hours. A brief discussion of well-known strategies and examples are given below: [0003] Lipophilic derivatives encapsulated by liposome membranes: DE 27 120 30 (ICI 1977) is an early example of lipophilic substituted glucocorticoids, for example dexamethasone palmit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
CPCA61K9/1271A61K9/127A61K9/1272A61P19/02A61P29/00A61P5/44
Inventor 斯特芬·潘茨纳罗尔夫·布罗伊尔雷蒙德·W.·金内乌纳·劳赫豪斯
Owner NOVOSOM
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