Method for preparing targeted curcumin nanoparticles for treating ulcerative colitis

A technology of curcumin and nanoparticles, applied in the field of medicine, to achieve the effects of prolonging half-life, improving burst release, and good freeze-drying and reconstitution performance

Inactive Publication Date: 2010-05-26
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The purpose of the present invention is to propose a curcumin nanomedicine system prepared based on emulsified solvent volatilization method, aiming at the defects that curcumin is insoluble in water and easy to decompose, by wrapping curcumin in degradable polymers to make nanoparticles, thereby Improve the hydrophobic properties of curcumin, prolong the residence and action time of curcumin in the body, improve the bioavailability of curcumin, and enhance the targeting of ulcerative colitis

Method used

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  • Method for preparing targeted curcumin nanoparticles for treating ulcerative colitis
  • Method for preparing targeted curcumin nanoparticles for treating ulcerative colitis
  • Method for preparing targeted curcumin nanoparticles for treating ulcerative colitis

Examples

Experimental program
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preparation Embodiment 1

[0023] Preparation Example 1: Preparation of Curcumin PLGA Nanoparticles

[0024] Table 1 The composition of the prescription of curcumin PLGA nanoparticles

[0025]

[0026] Preparation:

[0027] Co-dissolve the PLGA and curcumin in the above prescription amount in dichloromethane to obtain the organic phase. The prepared PVA solution is the water phase. Pour the organic phase into the water phase, stir at 15000rpm for 2-3min, and place it in a probe-type ultrasonic cell. In the crushing instrument, 400W ultrasonic 60-240 times, then take out and carry out low-temperature high-speed centrifugation 10000rpm-20000rpm, collect curcumin PLGA nanoparticles ( figure 1 ), freeze-dried after redispersing with 2%-10% sucrose solution to obtain curcumin PLGA nanoparticles ( figure 2 ).

preparation Embodiment 2

[0028] Preparation Example 2: Particle Size Measurement of Nanoparticles

[0029] The particle size and distribution of nanoparticles were measured by laser particle size analyzer. The measured particle size is 409±11nm, which is a normal distribution of effective diameter.

preparation Embodiment 3

[0030] Preparation Example 3: Determination of Nanoparticle Drug Loading Rate

[0031] Weigh the freeze-dried powder of nanoparticles, add a certain amount of acetone to dissolve it, measure the content of curcumin at 425nm, and calculate the drug loading rate and encapsulation efficiency of nanoparticles.

[0032] Table 2 Drug loading rate and encapsulation efficiency of curcumin PLGA nanoparticles

[0033]

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Abstract

The invention discloses a prescription of targeted curcumin-polylactic acid-hydroxyacetic acid copolymer (PLGA) nanoparticles for treating ulcerative colitis and a preparation process thereof. The prescription uses the targeting characteristic of the nanoparticles to an inflammatory part to reduce a medicament administration dosage and side effect and improve treatment effect. The preparation process comprises the following steps: taking a biodegradable material PLGA as a carrier material, polyvinyl alcohol as an emulsifier and 2 to 5 percent cane sugar as a freeze-drying protective agent, adding PEG 6000 into a water phase, and preparing the curcumin-PLGA nanoparticles by an emulsion-solvent volatilization method. The prescription process is optimized by taking the grain sizes of the nanoparticles and a medicament-loading rate as indexes. The prepared nanoparticles are round or elliptic and uniform in the size, have a mean grain size of 20 to 800nm and the medicament-loading rate of 10 to 20 percent, reduce dumping effect and have obviously better treatment effect on an animal pattern than a 5-aminosalicylic acid control group.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a method for preparing ulcerative colitis-targeted curcumin nanoparticles. The curcumin-PLGA nanoparticles prepared by the invention have a particle diameter of 200-800nm ​​and a drug loading rate of 10%-20%, the encapsulation rate is 50-80%, good freeze-drying formability, reconstitution meets the requirements of medicine. Background technique [0002] Turmeric is the dry rhizome of Curcuma longa L. Curcumin (curcumin) is one of the main active components of turmeric. It has been widely used as pigment, food additive and condiment. The toxicity is very low, and the LD50 of mice is greater than 2g / kg. [0003] The molecular formula of curcumin is C 21 h 20 o 6 ,. Curcumin is a polyphenolic compound with a B-diketone structure. Due to the structure interchanging into an enol structure, it is acidic. The pKa values ​​​​of the three acidic protons are 8.38, 9.88 an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/12A61P3/06A61P31/04A61P29/00A61P35/00A61P39/06
Inventor 崔京浩钱颖
Owner SUZHOU UNIV
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