Cristal Delivery B.v.

Universiteit Utrecht

Cornelis Franciscus Van Nostrum

Wilhelmus Everhardus Hennink

Cristianne Johanna Ferdinand Rijcken

Osamu Soga

Marinus Jacob Van Steenbergen

Isil Altintas

Robertus Matthias Joseph Liskamp

Steffen Van Der Wal

Silvia Johanna De Jong

Johannes Anna Wilhelmus Kruijtzer

Cristianne Johanna Rijcken

The present invention relates to a particular class of biodegradable linkers, ensuring transiently stable conjugation of building blocks and/or bioactive compounds into drug delivery systems (DDS), such as DDS based on polymeric micelles or hydrogels. In addition, the present invention relates to compounds, comprising said linkers, such compounds preferably being prodrugs. Further, the invention is directed to the use of said linkers, and especially said biodegradable linkers, in a drug delivery system. Moreover, the invention relates to controlled release system comprising a polymer matrix, capable of releasing an active ingredient, wherein the active ingredient is covalently linked to the polymer molecules of the polymer matrix through said linkers, as well as to a method of synthesizing these linkers and preparing such controlled release systems.

Tunable, biodegradable linker molecules for transient conjugation of components in drug delivery systems, and drug delivery systems prepared therewith

The present invention relates to a method for the preparation of a controlled release system and especially to a method for entrapment of compounds in polymer carriers for controlled release of active ingredients, preferably bioactive ingredients, such as drugs. This method results in a system for controlled release of active ingredients and especially for controlled drug delivery. In accordance with the present invention, the term 'controlled release' encompasses all kinds of controlled release, including slow release, sustained and delayed release. Particularly, the present invention results in active ingredients, entrapped in or otherwise incorporated in or coupled to polymer carriers or polymeric devices, such as micelles, nanoparticles, microspheres and other types of polymer devices for controlled release; the active ingredients are covalently bonded to the polymer carriers or polymeric devices.

Method for preparation of a controlled release system

The present invention relates to a method for the preparation of a controlled release system and especially to a method for entrapment of compounds in polymer carriers for controlled release of active ingredients, preferably bioactive ingredients, such as drugs. This method results in a system for controlled release of active ingredients and especially for controlled drug delivery. In accordance with the present invention, the tem controlled release' encompasses all kinds of controlled release, including slow release, sustained and delayed release. Particularly, the present invention results in active ingredients, entrapped in or otherwise incorporated in or coupled to polymer carriers or polymeric devices, such as micelles, nanoparticles, microspheres and other types of polymer devices for controlled release; the active ingredients are covalently bonded to the polymer carriers or polymeric devices.

The present invention relates to compositions comprising polymers whose solubility characteristics can be changed by incubation and particularly poly (hydroxyalkyl(meth) acrylamide mono/di-lactate_interpolymers. Another aspect of this invention is the application of such temperature sensitive polymers as release systems of biologically active compounds. The polymers of the present invention comprise monomers, which have modifiable functionality. The functionality of the monomers can for example be modified by the presence of hydrolysable groups. The modification is effected by the incubation, leading to a change of the water solubility characteristics of the polymer. The polymers used in the present invention contain hydrolysable chemical groups. As a result the polymer's solution characteristics, specifically its lower critical solution temperature (LCST), change upon incubation.

Temperature sensitive polymers

The present invention relates to compositions comprising polymers whose solubility characteristics can be changed by incubation and particularly ploy (hydroxyalkyl (meth) acrylamide mono/di-lactate) interpolymers. Another aspect of this invention is the application of such temperature sensitive polymers as release systems of biologically active compounds. The polymers of the present invention comprise monomers, which have modifiable functionality. The functionality of the monomers can for example be modified by the presence of hydrolysable groups. The modification is effected by the incubation, leading to a change of the water solubility characteristics of the polymer. The polymers used in the present invention contain hydrolysable chemical groups. As a result the polymer's solution characteristics, specifically its lower critical solution temperature (LCST), change upon incubation.

The invention relates to hydrogel compositions, which can be applied as biodegradable materials and to the processes to prepare such hydrogels. The hydrogel of the present invention comprises a stereocomplex gel structure which is the result of the interaction of oligomerized monomers of one chirality with that of oligomerized monomers of the opposite chirality, both grafted to hydrophilic polymers. The grafts form an interaction which is different from a covalent chemical interaction and thus provide the gel with the required coherence.

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Utrecht, Netherlands

Cornelis Franciscus Van Nostrum