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Antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer

An antioxidant and nanosphere technology, applied in antitumor drugs, animal repellents, plant growth regulators, etc., can solve the problem that the molecular mechanism of antitumor effect is not clear.

Inactive Publication Date: 2014-06-04
CEDARS SINAI MEDICAL CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The molecular mechanisms underlying the antitumor effects of NSAIDs are still poorly understood and are a matter of further research

Method used

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  • Antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer
  • Antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer
  • Antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0336] In order to prepare cy3 / cy5 / cy5.5-labeled antioxidant-antitumor nanospheres, antioxidant antitumor nanospheres were prepared by the same procedure as described in Example A-Example D below, except that the 0.1-2 mg of 1-octadecanethiol (Aldrich, code O1858) was added to the organic phase ( figure 1 in A).

[0337] Add 500 μL of 10× PBS and 1.5 molar equivalents of Cy3 / Cy5 / Cy5.5 maleimide to 3 mL of the suspension of antioxidant-antitumor nanospheres containing 1-octadecanethiol ( figure 1 in B). Such as figure 1 As shown in C in , this intermediate can be used to modify the carrier drug to have a maleimide group.

[0338] Such as figure 2 As shown, the SH-maleimide pair can be replaced by NH 2 - NHS pair or other substitution.

Embodiment A

[0339] Embodiment A-antioxidant-preparation of anti-tumor nanospheres

[0340] Nanospheres were prepared according to the method using spontaneous emulsification with slight modifications. Briefly, 15 mg of the mixture (camptothecin derivatives and ALA 2(a mixture of 1,12-dodecanediol)) was dissolved in acetone (5 mL, 0.1% polysorbate 80). The organic solution was poured into the aqueous phase prepared by dissolving 25 mg of Pluronic F68 in 10 mL of double distilled water (0.25% w / v) with gentle stirring on a magnetic plate. After magnetic stirring for 15 minutes, the acetone was removed under reduced pressure at room temperature. Nanospheres were filtered through a 0.8 μm hydrophilic syringe filter and stored at 4 °C. Hydrodynamic size measurements and size distributions of nanospheres were performed by dynamic light scattering (DLS) using a Coulter N4-Plus Particle Sizer (Coulter Corporation, Miami, FL).

[0341] Separately, 25 mg of a mixture (an antioxidant camptothe...

Embodiment B

[0345] Example B-Preparation of antioxidant and anti-tumor nanospheres

[0346] According to the method described in Example 5, nanospheres were prepared from 25 mg of the mixture (a mixture of camptothecin derivative and α-tocopherol) using spontaneous emulsification. In the absence of camptothecin derivatives, by α-tocopherol or Ibu 2 TEG to prepare control nanospheres.

[0347] Table 2. Size and Polydispersity Index (P.I.):

[0348] Antioxidant-Anti-tumor Nanosphere II

[0349] α-tocopherol (mg)

Compound C-10(mg)

Size (nm)

P.I.

25

1

128±45

0.25

25

0

121±40

0.20

[0350] Example C- Preparation of anti-inflammatory-anti-tumor nanospheres

[0351] According to the method described in Example 5, nanospheres were prepared from 25 mg of a mixture (a mixture of camptothecin derivatives, non-steroidal anti-inflammatory drug (NSAID) derivatives and alpha-tocopherol) using spontaneous emulsification. Contr...

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Abstract

This invention relates to antioxidant, neuroprotective and antineoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, NSAIDs and statins, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant, neuroprotective and anti-neoplastic nanoparticles comprising a therapeutic agent on an amphiphilic spacer or an amphiphilic polymer and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these neuroprotective and anti-neoplastic nanoparticles for the preparation of delivery devices of other pharmaceuticals and / or drugs.

Description

technical field [0001] The present invention relates to antioxidant and anti-tumor nanoparticles comprising therapeutic agents on amphiphilic spacers or amphiphilic polymers. Background technique [0002] As used herein, publications are incorporated by reference to the same extent as if each individual publication or patent application was specifically and individually indicated to be incorporated by reference. The following description includes information useful for understanding the present invention. It is not an admission that any of the information presented herein is prior art or relevant to the presently claimed invention, nor that any publication specifically or implicitly referenced is prior art. [0003] Antitumor effect of camptothecin [0004] Camptothecin is a plant alkaloid that was first isolated from the wood and bark of Camptotheca acuminate (Asteraceae) and shown to have anti-inflammatory properties through DNA topoisomerase I inhibition of DNA relaxat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14C07D339/02C07D405/00A01N43/26
CPCA61K38/00A61K49/0093A61K49/0052A61K47/481A61K9/5123A61K49/0032A61K47/48869A61K47/55A61P3/06A61P9/10A61P35/00A61P39/06A61K9/16A61K31/355A61K47/02A61K47/10A61K47/50
Inventor 约翰·俞李凤燮
Owner CEDARS SINAI MEDICAL CENT
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