Carriers for the local release of hydrophilic prodrugs

A hydrophilic and hydrophobic drug technology, applied in pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., can solve the problems of weakening the effectiveness of the targeted delivery concept, different release rates, and inability to adjust the composition.

Inactive Publication Date: 2013-10-02
KONINK PHILIPS ELECTRONICS NV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Another problem is that the above-mentioned prior art scheme of maintaining a balance between retention and release by altering the lipid composition weakens the validity of the concept of truly targeted delivery, since even the release rate may vary between individuals and obviously cannot Adjust composition based on individual

Method used

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  • Carriers for the local release of hydrophilic prodrugs
  • Carriers for the local release of hydrophilic prodrugs
  • Carriers for the local release of hydrophilic prodrugs

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Embodiment Construction

[0014] Broadly, the present invention may be described with reference to the sound recognition that thermosensitive liposomes are able to solve several technical problems associated with the topical delivery of hydrophobic drugs. It will be appreciated that this concept is equally applicable to a broader field than just thermosensitive liposomes, that is to say, to virtually any other carrier capable of releasing its contents in response to a local stimulus ( In particular nanocarriers such as polymersomes or liposomes).

[0015] The specific release by local stimulation of hydrophilic prodrugs contained within the lumen of the carrier, such as that of a liposome, offers the possibility of timed release of the prodrugs. This in turn has the potential advantage of activating the prodrug into the active form of the drug when the prodrug is released.

[0016] The present invention is further described by way of specific embodiments and with reference to certain drawings but the ...

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Abstract

Disclosed is a carrier for the local, targeted administration of a hydrophobic drug. The hydrophobic drug is rendered in to a hydrophilic prodrug thereof, and is contained in the lumen of a thermosensitive liposome or polymersome. Upon administration of the carrier, heat can be applied at the locus where the drug is to be released. After release of the prodrug, it will be activated so as to turn into the active drug.

Description

field of invention [0001] The present invention relates to targeted, localized delivery of hydrophobic drugs by releasing hydrophilic prodrugs of said hydrophobic drugs from a carrier. The invention also relates to a new application of the thermosensitive carrier. Background of the invention [0002] Many diseases that are largely localized to specific tissues are treated with systemically administered drugs. A well-known example of standard cancer therapy is systemic chemotherapy, which is associated with significant side effects in patients due to undesired biodistribution and toxicity. The therapeutic window of these drugs is usually defined by the minimum required therapeutic concentration in diseased tissue on the one hand and the toxic effects in non-target organs (eg liver, spleen) on the other. Localized treatment by, for example, local release of cytostatics from nanocarriers promises to be a more effective treatment with a larger therapeutic window relative to st...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127
CPCA61K9/0004A61K9/0019C07D305/14A61K9/127A61P35/00A61P43/00A61K9/0087
Inventor H·格吕尔S·朗戈埃斯C·F·希欧
Owner KONINK PHILIPS ELECTRONICS NV
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