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Polymer-flavonoid conjugates and hydrogels for biomedical applications

A technology for polymers and flavonoids, which can be used in pharmaceutical combinations, pharmaceutical formulations, inactive components of polymer compounds, etc., can solve the problems of poor stability of flavonoids, and no way of preparing stable polymer-flavonoid conjugates. , to achieve the effect of improving bioavailability, improving biological activity, and avoiding the separation process

Inactive Publication Date: 2016-06-08
AGENCY FOR SCI TECH & RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Furthermore, there is currently no way to prepare stable polymer-flavonoid conjugates
However, there is a need to create such conjugates to improve the poor stability of flavonoids and to make them useful in biomedical applications such as gels

Method used

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  • Polymer-flavonoid conjugates and hydrogels for biomedical applications
  • Polymer-flavonoid conjugates and hydrogels for biomedical applications
  • Polymer-flavonoid conjugates and hydrogels for biomedical applications

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Embodiment approach

[0057] According to the present invention, the polymer is modified with thiol groups for attachment to flavonoids. According to a preferred embodiment of the present invention, described method further comprises the following steps:

[0058] (a) linking a thiol- or disulfide-containing compound to the polymer in the presence of a reducing agent; and

[0059] (b) cleaving any disulfide formed at the disulfide bond to form said polymer with terminal thiol groups.

[0060] This method is suitable, for example, for the preparation of flavonoid-terminated polymer conjugates. The conjugate was obtained in high purity and high yield (over 90%). The method is easy to perform and scale up. It is a non-enzymatic method that does not require complex purifications.

[0061] The thiol- or disulfide-containing compound may be, for example, aminoalkylthiol derivatives such as cysteamine hydrochloride and cystamine dihydrochloride.

[0062] According to a preferred embodiment, said linki...

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Abstract

There is provided polymer-flavonoid conjugates. Flavonoid-grafted and flavonoid-terminated polymer conjugates are disclosed according to the invention. The linkage of flavonoids to the polymers has been achieved via thiol linkages. The inventive processes allow for making of the conjugates in high yield avoiding complex purification steps. The conjugates can be easily autoxidized to hydrogels with uses in many biomedical applications where a higher stability of the flavonoid is necessary. The hydrogels can be potentially used as viscosupplement, anti-adhesion film or dermal filler.

Description

technical field [0001] The present invention generally relates to a polymer-flavonoid conjugate, wherein the polymer is conjugated to the flavonoid via a thiol linker. The invention also relates to methods of making the conjugates as well as hydrogels comprising the conjugates and methods of making the hydrogels and using the hydrogels in biomedical applications. Background technique [0002] Flavonoids have been shown to have a wide range of biological and pharmacological activities in vitro. Examples include antiallergic activity, antiinflammatory activity, antioxidant activity, antimicrobial activity, antibacterial activity, antifungal activity, antiviral activity, anticancer activity, and antidiarrheal activity. Over the past few decades, for example, green tea catechins have received significant attention as protective agents against coronary heart disease and cancer (Bushman, J.L. -9; 1998; and Zaveri, N.T. Greentea and its polyphenolic catechins: medicinal uses in c...

Claims

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Application Information

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IPC IPC(8): C07D311/32A61K38/00A61K39/00A61K47/36A61K47/42A61K31/353
CPCA61K47/36C07D311/32A61K9/0019A61K9/06A61K47/32A61K8/498A61K8/735A61K8/8147A61K8/042A61K2800/57A61K2800/91A61K47/61A61K31/353A61Q19/00A61P17/00A61P19/02A61P41/00
Inventor 栗泽元一裵基见
Owner AGENCY FOR SCI TECH & RES
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