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Drug Delivery Composition Comprising a Self-Assembled Gelator

Inactive Publication Date: 2011-09-22
RES FOUND THE CITY UNIV OF NEW YORK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0013]One embodiment of this invention relates to drug-delivery compositions. The drug may be delivered in various different ways. The drug-delivery composition may be a drug-derived gelator capable of self assembly, where the drug to be delivered is in the backbone of the gelator and released upon degradation of the gelator. One or more agents can be encapsulated in the self-assembled gels. Degradation of the gelator can release both t

Problems solved by technology

Literature study reveals that there are only limited reports on easily achievable and efficient low-molecular-weight gelators that are able to gel water or even water mixtures with other solvents.
Synthesizing hydrogelators in high quantities is often limited with multiple-step synthesis and poor yields, which make industrial scale production difficult.
Many reported hydrogelators require multiple steps and an elaborated purification process, and many others require costly starting materials and expensive reagents.
An additional problem in drug delivery is striking a balance between toxicity and therapeutic effect.
This could be due to the relatively complex synthesis of LMWGs and concerns about possible toxicity of in situ generated fragments from the degradation of LMWGs.
Additionally, self-assembled hydrogel-based drug delivery has been hindered by the unknown fate of the host gelator after the gel degradation.
Potential problems can arise relating to the quantity of drug that can be encapsulated within hydrogels, and respective encapsulation efficiency may limit the potential dose or release kinetics that can be achieved.
Additionally, polymer-based drug delivery devices that utilize entrapped drug have been known to exhibit an undesired burst release.
However, polymer degradation can lead to polymer fragments with heterogeneous chain lengths that may generate potential toxicity, unwanted side effects, or uncontrollable drug bioavailability.

Method used

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  • Drug Delivery Composition Comprising a Self-Assembled Gelator
  • Drug Delivery Composition Comprising a Self-Assembled Gelator
  • Drug Delivery Composition Comprising a Self-Assembled Gelator

Examples

Experimental program
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Effect test

example 1

Self-Assembled Acetaminophen Prodrugs

[0113]Utilization of enzyme catalysis as a tool to disassemble self-assembled hydrogels to control the release encapsulated drug provides an opportunity to employ a wide range of enzyme-specific low-molecular-weight hydrogelators.

[0114]In this example, low-molecular-weight amphiphilic prodrugs are synthesized as hydrogelators from biocompatible fatty acids and a well-known drug, acetaminophen (Apn), (which belongs to a class of drugs called analgesics (pain relievers) and antipyretics (fever reducers)). This reaction was performed in a single-step esterification. The example shows the prodrug's ability to self-assemble into nanoscale structures in aqueous solutions to form hydrogels that may subsequently encapsulate a second drug such as curcumin, which is a known chemopreventive and anti-inflammatory hydrophobic drug. Upon enzyme triggered degradation, the hydrogel can release single or multiple drugs at physiologically simulated conditions in v...

example 2

Self-Assembling Amphiphiles

[0208]A series of amphiphiles were designed for efficient gelation. The amphiphile was synthesized in a single step that avoids the harsh conditions and is beneficial when synthesizing on an industrial scale. The use of expensive reagents was also eliminated. Compound purification was relatively easy. After the reaction, a simple filtration yielded a pure compound. Collectively these features make the amphiphile attractive for use in various biomedical applications.

[0209]This example focuses on a novel class of gelling agents or thickeners that are based on readily available and economically attractive starting materials. Gelling agents or thickeners capable of gelling or thickening a wide variety of solvents were used, making the gelling agents or thickeners suitable for employment in various applications.

[0210]Exemplary compounds include those having the general formula, RCONHC(CH2OH)3, in which R is a saturated alkyl chain having 9-15 C atoms or an unsa...

example 3

Dye Encapsulated Self-Assembled Nanofibers: In Vitro and In Vivo Analysis

[0230]In vitro: A model dye DiD was encapsulated within the self-assembled nanofibers prepared from salicin prodrug of formula (III). Salicin-deconate (4 wt / v %) was taken in glass vial and to that dye and PBS were added. Homogenous mixture was formed upon heating, subsequent cooling generated the gel. Fibers were isolated by repetitive centrifugation and washing steps. Fibers were incubated with synovial fluid at 37° C. that was extracted from human arthritic joints (inflamed). In the absence of synovial fluid, fibers were stable and preserved the dye within assembled fibers (FIG. 13a). The enzymes that were present in inflamed joints degraded the fibers to release the encapsulated dye. Slow degradation of fibers by enzymes over a period of 15 days was observed (FIG. 13b). The data demonstrates that in the absence of synovial fluid the fibers were intact and dye was confined to the fibers, whereas in the prese...

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Abstract

This invention discloses drug-delivery compositions, methods of making prodrugs, and methods of drug delivery using a self-assembled gelator. The backbone of the gelator can contain a drug or prodrug, such as acetaminophen or salicin. Additional drugs or agents can be encapsulated in the gelator. Enzymatic or hydrolytic cleavage can be used to release the drugs.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of priority to U.S. Provisional Patent Application Ser. No. 61 / 097,565, filed Sep. 17, 2008, the contents of which are incorporated by reference herein in their entirety.FIELD OF THE INVENTION[0002]This application claims the benefit This invention relates to low-molecular-weight amphiphilic gelators which self-assemble into various nano- and micro-structures in a wide range of organic and aqueous solvents. The gelators have the capability to delivery drugs.BACKGROUND[0003]A hydro- or organo gel consists of self-assembled macromolecular networks with a liquid filling the interstitial space of the network. The network holds the liquid in place through its interaction forces and so gives the gel solidity and coherence, but the gel is also wet and soft and capable of undergoing some extent of deformation. The gel state is neither solid nor liquid but has some features of both. Self-assembly has been used to develop molecular...

Claims

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Application Information

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IPC IPC(8): A61K38/43A61K31/167A61K31/7034A61K31/405A61K9/48A61K47/16C07C233/01C07C215/18C07D209/26A61K31/225A61K38/16A61K38/10A61K38/08A61K38/06A61K38/05A61K38/07C07C69/34C07H15/26C07K14/00C07K7/00C07K7/06C07K5/00A61K31/133A61P25/04A61P29/00A61P11/00A61P31/06C12P7/62C12P19/00
CPCA61K9/06A61K31/12A61K47/4813A61K47/481A61K45/06A61K31/7034A61K31/555A61K31/43A61K31/405A61K31/22A61K31/167A61K2300/00A61K47/54A61K47/542A61K47/55A61K47/555A61P11/00A61P23/02A61P25/04A61P29/00A61P31/06
Inventor KARP, JEFFREY M.VEMULA, PRAVEEN KUMARJOHN, GEORGECRUIKSHANK, GREG
Owner RES FOUND THE CITY UNIV OF NEW YORK
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