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Self-assembled polymeric nanoparticles containing physiologically active ingredients and external application containing the nanoparticles

A technology of physiologically active ingredients and nanoparticles, which is applied in the field of self-aggregating polymer nanoparticles, can solve the problem of not containing a large amount of active ingredients, and achieve the effect of improving absorption and improving skin

Inactive Publication Date: 2006-08-02
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, conventional methods also have Ostwald ripening (Ostwald ripening) problems, precipitation problems, or flocculation problems due to colloidal instability. When increasing the amount of solid components, the conventional instability of colloids becomes very serious, so that , granules prepared by conventional methods cannot contain a large amount of active ingredients (21th Proceedings of IFSCC International Congress), 2000(2000), 442-458)

Method used

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  • Self-assembled polymeric nanoparticles containing physiologically active ingredients and external application containing the nanoparticles
  • Self-assembled polymeric nanoparticles containing physiologically active ingredients and external application containing the nanoparticles
  • Self-assembled polymeric nanoparticles containing physiologically active ingredients and external application containing the nanoparticles

Examples

Experimental program
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preparation Embodiment 1-9

[0056] [Preparation Example 1-9] Preparation of PCL-PEG block copolymer

[0057] The preparation method of the PCL-PEG block copolymer described in this example is only for reference, and the copolymer of the present invention is not limited thereto.

[0058] The PCL-PEG block copolymer of the present invention is prepared by ring-opening polymerization of polycaprolactone monomer.

[0059] According to Table 1, a specific amount of methoxy PEG [hereinafter referred to as "mPEG" (Formula 6)] and catalyst Sn(Oct) 2 (Sigma, St.Louis, MO, USA) was added to a glass flask containing hexamethyldisilazane silanized by reaction with hydroxyl groups, and polycaprolactone monomer was added thereto and mixed uniformly . The said mPEG (Fluka Chemie GmbH, Buchs, Switzerland) is PEC, one terminal of PEC is substituted with methoxy group to prevent reaction, and the other terminal hydroxyl group can carry out polymerization reaction.

[0060] [Formula 6]

[0061]

[0062] The flask co...

preparation Embodiment 10-11

[0065] [Preparation Example 10-11] Preparation of polycaprolactone-co-polyethylene glycol block copolymer

[0066] Add 10 grams of monomethoxypolyethylene glycol (molecular weight 5000) and 10 grams of caprolactone monomer with a hydroxyl group at one end to a 50 ml dry flask, add 0.05 grams of Sn(Oct) 2 as a catalyst. A Teflon-coated magnetic rod was added to the flask, the mixture was vacuumed for 30 minutes, and the flask was then tightly sealed. The above sealed flask was placed in an oil bath at 150°C and polymerization was carried out for 6 hours.

[0067] The polymer product was in the form of a hard solid, which was completely dissolved with 20 ml of dichloromethane and precipitated with excess ether. This process was repeated 3 times to remove unreacted monomers and oligomers. The precipitated product was vacuum-dried at room temperature for 12 hours to finally obtain 17.3 g of polycaprolactone-block-polyethylene glycol block copolymer.

[0068] Depend on 1H NMR ...

preparation Embodiment 12-13

[0070] [Preparation Examples 12-13] Preparation of block copolymers of polyethylene glycol and poly D,L-lactic acid-co-glycolic acid

[0071] 5 grams of monomethoxypolyethylene glycol (molecular weight 5000) with a hydroxyl group at one end, 7 grams of D, L-lactic acid and 3 grams of glycolic acid were added to a 20 ml dry flask, and 0.025 grams of Sn(Oct) was added thereto. 2 as a catalyst. A Teflon-coated magnetic rod was added to the flask, the mixture was vacuumed for 30 minutes, and the flask was then tightly sealed. The above sealed flask was placed in an oil bath at 130°C and polymerization was carried out for 6 hours.

[0072] The polymer product was in the form of a hard solid, which was completely dissolved with 20 ml of dichloromethane and precipitated with excess ether. This process was repeated 3 times to remove unreacted monomers and oligomers. The precipitated product was vacuum-dried at room temperature for 12 hours to finally obtain 12.7 g of a block copoly...

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Abstract

The present invention relates to self-assembled polymeric nanoparticles containing physiologically active ingredients and to an external application containing the nanoparticles, in particular, relates to a self-assembled polymeric nanoparticles having amphiphilic polymeri, which comprises polycaprolactone as a hydrophobic block and polyethyleneglycol as a hydrophilic block to solubilize and entrap physiologically active ingredients in an aqueous solution, and to an external application for skin containing the particles.

Description

technical field [0001] The present invention relates to self-aggregating polymer nanoparticles containing physiologically active ingredients and an external liniment containing the nanoparticles. Specifically, the present invention provides a self-aggregating polymer nanoparticle having an amphiphilic polymer containing polycaprolactone as a hydrophobic block and polyethylene glycol as a hydrophilic block to The active ingredient is dissolved and embedded in an aqueous solution, and a topical liniment for the skin containing the particles is provided. Background technique [0002] In recent years, existing document (USP 5,338,761) has reported the method for preparing the emulsion particle of nanometer or micron size, and described particle contains medicine, lipid, glycerin, water and phospholipid or nonionic surfactant, also document (USP 6,120,751 ) reported other methods using charged phospholipids as emulsifiers. For example, nanoemulsions are prepared by treating sem...

Claims

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Application Information

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IPC IPC(8): A61K8/97A61Q5/00A61Q19/00
Inventor 南允盛沈钟沅姜炳永黄在晟金俊吾张利燮朴元锡姜亨锡李炳锡曹瑗熙成大石金大权李昶勋韩相勋沈荣哲廉明勋李成日金亨俊梁惠珍
Owner AMOREPACIFIC CORP
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