Multifunctional nanoparticle conjugates and their use

A technology of nanoparticles and conjugates, applied in the field of multifunctional nanoparticle conjugates and their applications, which can solve the problems that dispersion cannot be completely prevented

Inactive Publication Date: 2009-05-20
EMORY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This dispersion cannot be completely prevented, resulting in the need to administer an overdose of the drug to achieve the desired effect

Method used

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  • Multifunctional nanoparticle conjugates and their use
  • Multifunctional nanoparticle conjugates and their use
  • Multifunctional nanoparticle conjugates and their use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0170] Synthesis of conjugated compounds

[0171] This example describes the paclitaxel-heparin-FA conjugate according to the process figure 1 Synthesis. Heparin (1 mmol) was activated overnight at 4°C with DCC (20 mmol) and NHS (22 mmol) in formamide. Dicyclohexylurea (DCU) was removed by filtration, and then heparin-NHS was obtained by recrystallization. Activated heparin-NHS (1 mmol) and aminated FA (20 mmol) were reacted again at room temperature for 1 day. FA was aminated with a conjugate with ethylenediamine. Dialysis removed unreacted aminated FA (molecular weight cutoff 2000). The yellowish final product was obtained by lyophilization. The yield of the conjugate was 95% (w / w). After the heparin-FA conjugate was dissolved in formamide (1 mmol), paclitaxel (30 mmol) and DCC (30 mmol) in DMSO were added. The mixture was reacted overnight at room temperature. After the reaction, recrystallization and filtration were performed to remove unreacted DCC. For further p...

Embodiment 2

[0176] Identification of conjugated compounds

[0177] This example describes the identification of paclitaxel-heparin-FA produced in Example 1. UV-Vis absorption spectra were recorded on a Shimadzu UV-2401PC scanning spectrophotometer operating with a slit width of 1.0 nm. The content of paclitaxel conjugated to heparin-FA was estimated by UV measurement (λ = 228 nm) based on a standard curve generated with known concentrations of paclitaxel in methanol. IR spectra of paclitaxel-heparin-FA were acquired on a Fourier transform infrared spectrometer (FT-IR) with a Perkin Elmer system 2000 spectrometer and samples were analyzed as KBr pellets.

[0178] The synthesis of heparin-FA is through the 1 A signal was present at δ 6.75-8.77 ppm of the H-NMR spectrum and confirmed by absorption at λ = 280 nm of the UV spectrum of heparin-FA. The linkage between paclitaxel and heparin-FA is achieved through the DCC-mediated reaction between the hydroxyl group of paclitaxel and the carbo...

Embodiment 3

[0183] Identification of microtubule-binding activity

[0184] This example describes the microtubule polymerization assay used to evaluate compounds of the disclosure. Microtubule assembly reactions were performed in G-PEM buffer (1 mM GTP, 80 mM PIPES, 1 mM EGTA, 0.5 mM MgCl; pH 6.8) in the presence of drugs (10 μM) at concentrations of microtubule (Cytoskeleton Inc., Boulder, CO) It is 1mg / ml (10μM). The instrument was zeroed at 4°C with this solution. Paclitaxel or heparin-paclitaxel conjugates were then rapidly mixed into the microtube solution to a final concentration of 10 [mu]M, and absorbance was continuously monitored for a period of 80 minutes. Such samples were placed in quartz cuvettes and incubated at 32°C. Microtubule polymerization was observed by measuring the absorbance (340 nm) of the solution.

[0185] refer to image 3 , the ability of paclitaxel and paclitaxel-heparin-FA conjugates to induce microtubule assembly in vitro was determined at 10 μM pacli...

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Abstract

Disclosed herein are conjugates comprising a nanocarrier, a therapeutic agent or imaging agent and a targeting agent. Also disclosed herein are compositions comprising such conjugates and methods for using the conjugates to deliver therapeutic and / or imaging agents to cells. Also disclosed are methods for using the conjugates to treat particular disorders, such as proliferative disorders.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application 60 / 617,158, filed October 7, 2004, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention discloses drug delivery of therapeutic drugs or imaging agents to target tissues. The compounds disclosed in this application include a targeting component, a therapeutic or imaging component and a nanocarrier component. The present disclosure also relates to compositions containing the compounds and methods of using the compounds and compositions. Background technique [0004] Considerable research has been directed towards the discovery of systems by which agents can be selectively delivered to the desired anatomical site, ie, the site in need of treatment. Despite some progress in this field, many drug treatments for various diseases or health risks pose considerable risks to patients due to lack of selective drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G06F11/34G06F17/30
CPCA61K47/48561A61K47/48315A61K47/48076A61K47/4823B82Y5/00A61K47/48107A61K49/0002A61K47/48923A61K47/547A61K47/551A61K47/61A61K47/645A61K47/6849A61K47/6939A61P35/00A61P35/02
Inventor 聂书明李容圭格洛娅·金
Owner EMORY UNIVERSITY
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