Non-polar photosensitizer formulations for photodynamic therapy

a non-polar, photodynamic therapy technology, applied in the direction of dermatological disorders, sexual disorders, drug compositions, etc., can solve the problems of lack of specificity, limited liposomes, patient gaining a new set of maladies from the therapy, etc., to improve the transport of non-polar photosensitizers, improve pharmacokinetic properties, and preserve the structure and size of liposomes

Inactive Publication Date: 2005-03-03
BIOLITEC PHARMA MARKETING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

It is another object of the present invention to incorporate non-polar photosensitizers into a liposomal membrane thus allowing non-polar and polar substances to be transported using the same vehicle.
It is a further object of the present invention to preserve the structure and size of liposomal constructs with incorporated non-polar photosensitizer during freeze-drying processes by adding monosaccharides or polyalcohols as cryoprotectants.
It is yet another object of the present invention to provide a photosensitizer formulation with improved pharmacokinetic properties.
It is still another object of the present invention to improve the transport of non-polar photosensitizers through the cell membrane and thus increasing the efficacy of PDT.
The present invention involves a pharmaceutical liposomal formulation for photodynamic therapy comprising a non-polar porphyrin photosensitizer and one or more phospholipids, which are stable in storage without

Problems solved by technology

Although sometimes successful, liposomes have limitations.
A constant problem in the treatment of infectious disease is the lack of specificity of the agents used for the treatment of disease, which results in the patient gaining a new set of maladies from the therapy.
The use of PDT for the treatment of various types of disease is limited due to the inherent features of photosensitizers.
These include their high cost, extended retention in the host organism, substantial ski

Method used

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  • Non-polar photosensitizer formulations for photodynamic therapy
  • Non-polar photosensitizer formulations for photodynamic therapy

Examples

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example 1

Preparation of Liposomes containing m-THPC

mTHPC (Temoporfin) was synthesized as described in U.S. Pat. Nos. 4,992,257 and 5,162,519, incorporated herein by reference.

Liposomes were prepared according to the following general procedure:

Non-polar photosensitizer, ascorbic palmitate and the phospholipids are dissolved in chloroform / methanol. The solution is then dried under vacuum using a rotary evaporator until the chloroform / methanol mixture is not detectable by gas chromatography anymore. Water for injection is added to rehydrate the lipid film at a temperature of 50° C. for at least 2 hours. The mixture is then passed through a homogenizer filter system using a final pore size of 100 nanometer. Optionally, the rehydration water is supplemented with monosaccharides or polyalcohols. The filtrate is collected, filled into vials and optionally freeze dried. The freeze dried composition is reconstituted with water for injection prior to administration.

Using the foregoing procedu...

example 1a

IngredientAmount % w / vmTHPC 0.05 to 0.15Dipalmitoyl Phosphatidyl Choline 0.5 to 2.0Dipalmitoyl Phosphatidyl Glycerol 0.05 to 0.2pegylated Distearoyl Phosphatidyl 0.05 to 0.2EthanolamineAscorbic Palmitate0.002 to 0.004Water for Injectionas required to achievedesired concentrations above

example 1b

IngredientAmount % w / vmTHPC 0.05 to 0.15Dipalmitoyl Phosphatidyl Choline 0.5 to 2.0Dipalmitoyl Phosphatidyl Glycerol 0.05 to 0.2Ascorbic Palmitate0.002 to 0.004Water for Injectionas required to achievedesired concentrations above

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Abstract

A pharmaceutical liposomal formulation for photodynamic therapy comprising a non-polar porphyrin photosensitizer and one or more phospholipids, which are stable in storage without requiring freeze-drying is described. The liposomal formulation provides therapeutically effective amounts of the photosensitizer for intravenous administration. The phospholipids may be modified by pegylation, i.e. they contain poly ethylene glycol as an integral part of the phospholipids. The formed liposomes contain the non-polar photosensitizer within the membrane and are useful for the combined targeting of a non-polar photosensitizer and a second polar substance. When a formulation includes the presence of monosaccharides or polyalcohols, it can be efficiently freeze-dried preserving the size of the liposomal vehicles and the content of a therapeutically effective amount of the photosensitizing agent. The invention also relates to the liposome composition formed upon reconstitution with an aqueous vehicle. The freeze-dried formulation upon reconstitution with a suitable aqueous vehicle forms liposomes that are also useful for intravenous administration.

Description

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention concerns the preparation of liposomal formulations containing Temoporfin or other non-polar photosensitizers and their use in therapy, particularly using intravenous injection. 2. Information Disclosure Statement Liposomes are artificial vesicles composed of concentric lipid bilayers separated by water-compartments and have been extensively investigated as drug delivery vehicles. Due to their structure, chemical composition and colloidal size, all of which can be well controlled by preparation methods, liposomes exhibit several properties which may be useful in various applications. The most important properties are colloidal size, i.e. rather uniform particle size distributions in the range from 20 nm to 10 μm, and special membrane and surface characteristics. Liposomes are used as carriers for drugs and antigens because they can serve several different purposes (Storm & Crommelin, Pharmaceutical Scien...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K41/00
CPCA61K41/0071A61K9/127A61P1/02A61P1/04A61P11/00A61P15/00A61P17/00A61P31/00A61P35/00A61P43/00
Inventor ALBRECHT, VOLKERFAHR, ALFREDSCHEGLMANN, DIETRICHGRAFE, SUSANNANEUBERGER, WOLFGANG
Owner BIOLITEC PHARMA MARKETING
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