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Nanoparticles

A nanoparticle, free radical technology, applied in the field of nanoparticles, can solve problems such as being unsuitable for clinical environments

Pending Publication Date: 2021-03-30
新泰福托特股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, known inhibitors do have various disadvantages
For example, MSA is a strong acid that breaks down acid-labile compounds (such as active pharmaceutical ingredients, or APIs), and neither MSA nor BHT are suitable for use in a clinical setting due to their toxicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0186] Example 1 (comparative): Synthesis of particles with 0.18% DiR dye and free radical inhibitor (BHT).

[0187] Solution 1 (aqueous phase): 120 mg of Kolliphor HS 15 (Sigma Aldrich), 0.120 g of Brij L23 (Sigma Aldrich) and 12.0 g of 0.1 M hydrochloric acid solution (Merck) in water were mixed in a glass bottle until the solids were completely dissolved.

[0188] Solution 2 (monomer phase): 0.80 g of n-butyl cyanoacrylate (monomer, Henkel Loctite, Ireland), 0.010 g of butylated hydroxytoluene (BHT, Fluka) and 0.060 g of the dye DiR (Marker Gene Technology) (dissolved in Miglyol 812 (Caeser and Loretz GmBH, so that 1.6 mg of DiR was added to the mixture)) was mixed well in a glass vial.

[0189] Solution 1 and Solution 2 were mixed for 30 seconds in a 20 ml glass bottle placed on ice using a magnetic stirrer. The oil-in-water emulsion was immediately sonicated on ice for 3 minutes (6 x 30 sec intervals) (Branson digital sonifier 450 CE, 25% amplitude). After sonication,...

Embodiment 5

[0192] Example 5: Synthesis of particles with 0.10% DiR dye and dual inhibitor (vanillin).

[0193] Solution 1 (aqueous phase): 125 mg of Kolliphor HS 15 (Sigma Aldrich), 0.125 g of Brij L23 (Sigma Aldrich) and 11.5 g of 0.1 M hydrochloric acid solution (Merck) in water were mixed in a glass bottle until the solids were completely dissolved.

[0194] Solution 2 (monomer phase): a solution of 2.25 g of n-butyl cyanoacrylate (monomer, Henkel Loctite, Ireland), 0.240 g of vanillin (Sigma Aldrich) and 0.100 g of the dye DiR (Marker Gene Technology) (dissolved in Miglyol 812 (Caeser and Loretz GmBH, so that 2.6 mg of DiR was added to the mixture)) was mixed well in a glass vial.

[0195] Solution 1 and Solution 2 were mixed for 30 seconds in a 20 ml glass bottle placed on ice using a magnetic stirrer. The oil-in-water emulsion was immediately sonicated on ice for 3 minutes (6 x 30 second intervals) (Branson digital sonifier 450 CE, 25% amplitude). After sonication, the formed m...

Embodiment 7

[0198] Example 7 (comparative): Synthesis of particles with 0.6% Nr668 dye without any inhibitor (negative control).

[0199] Solution 1 (aqueous phase): 120 mg of Kolliphor HS 15 (Sigma Aldrich), 0.120 g of Brij L23 (Sigma Aldrich) and 12.0 g of 0.1 M hydrochloric acid solution (Merck) in water were mixed in a glass bottle until the solids were completely dissolved.

[0200] Solution 2 (monomer phase): a solution of 0.80 g of n-butyl cyanoacrylate (monomer, Henkel Loctite, Ireland) and 0.048 g of dye NR668 (modified Nile Red, SINTEF) (dissolved in Miglyol 812 ( Caeser and Loretz GmBH, so that 5.1 mg of NR668 was added to the mixture)) Mix well in a glass vial.

[0201] Solution 1 and Solution 2 were mixed for 30 seconds in a 20 ml glass vial placed on ice using a magnetic stirrer. The oil-in-water emulsion was immediately sonicated on ice for 3 minutes (6 x 30 sec intervals) (Branson digital sonifier 450 CE, 25% amplitude). After sonication, the formed miniemulsion was po...

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Abstract

The present invention provides a nanoparticle comprising a poly(alkyl cyanoacrylate) homopolymer, or copolymer, at least one active agent and an anionic and radical inhibitor, wherein the anionic andradical inhibitor is a compound having the following formula: wherein R1 is H; and R3, R4, R5, R6 and R7 are independently selected from the group consisting of -H, -OH, C1-C6 alkoxide, C1-C6 alkyl, halides, carboxylic acid, ketone or aldehyde; wherein the anionic and radical inhibitor is present in an amount of 0.001 to 15 wt%, as well as a process suitable for manufacture of the nanoparticle.

Description

technical field [0001] The present invention relates to poly(alkylcyanoacrylate) nanoparticles and methods of making said nanoparticles. Background technique [0002] The use of nanoencapsulation offers exciting possibilities in many markets where volatile, sensitive or hazardous materials / compounds need to be protected / concealed / masked / isolated and delivered / co-delivered to desired The goal. This is especially important in the rapidly developing field of nanomedicine. [0003] Two areas where the use of nanoparticles has begun to show particular value are drug delivery and molecular imaging. However, apart from medical applications, nanoparticles are also very beneficial in the nanoencapsulation of various materials / compounds, such as aromatic compounds, fragrances, flavors, dyes, nutrients, herbicides and insecticides agent. [0004] Nanoparticles for the delivery of therapeutic agents have the potential to circumvent many of the challenges associated with conventional...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/08
CPCA61K9/5138A61K9/5192A61K45/06B82Y5/00
Inventor R·施密德P·莫尔斯沃思Y·马尔奇E·苏尔海姆H·约翰森
Owner 新泰福托特股份有限公司
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