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Curcumin micelle drug-loaded system and preparation method thereof

A drug-carrying system, curcumin technology, applied in the direction of pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., can solve problems such as poor stability, achieve the effect of increasing the force and good industrial application prospects

Inactive Publication Date: 2016-08-03
SUZHOU LEINA PHARMA RES DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The polymer micelle material used in this patent is MPEG-PLA, but the stability of the micelle in vivo and in vitro is relatively poor, and it cannot really solve the shortcoming of curcumin’s rapid metabolism in the body

Method used

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  • Curcumin micelle drug-loaded system and preparation method thereof
  • Curcumin micelle drug-loaded system and preparation method thereof
  • Curcumin micelle drug-loaded system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The synthesis of embodiment 1 macromolecule auxiliary material

[0040] 1.1 Preparation of MPEG-PCL-Phe(Boc)

[0041] 5g of methoxypolyethylene glycol with a molecular weight of 2000, 6g of ε-caprolactone, 6mg of stannous octoate, and 10ml of toluene were added to the polymerization bottle, and the toluene was removed by vacuum at 50°C to remove the moisture in the system, and the vacuum-sealed polymerization bottle was placed at 100 Polymerize at ℃ for 24 hours, dissolve the product with dichloromethane, and precipitate with ether to obtain methoxypolyethylene glycol-polycaprolactone block copolymer (MPEG-PCL).

[0042] Dissolve 6.65g of Boc phenylalanine in 50ml of anhydrous ethyl acetate, add 3.5ml of triethylamine, add 3.05ml of pivaloyl chloride after the solution is cooled to -10°C, heat up the reactant to 0°C for 2 hours, then continue the reaction at room temperature 2h. The insoluble matter was removed by filtration, and the ethyl acetate was removed by rotar...

Embodiment 2

[0050] The preparation of embodiment 2 curcumin micelles

[0051] 2.1 Preparation of MPEG-PCL-Phe(Boc) / curcumin micelles

[0052] 20mg of curcumin, 380mg of MPEG-PCL-Phe (Boc) were dissolved in 5ml of ethanol, and the solvent was removed by rotary evaporation at 55°C, and then 5ml of ultrapure water was added to dissolve the drug film. Micellar lyophilized powder.

[0053] 2.2 Preparation of MPEG-PCL-Phe(Fmoc) / curcumin micelles

[0054] 50mg of curcumin, 500mg of MPEG-PCL-Phe (Fmoc) were dissolved in 10ml of acetone, added to a dialysis bag with a molecular weight cut-off of 3000 and dialyzed for 24 hours, and the resulting micellar solution was filtered through a 0.22 μm sterilizing membrane and freeze-dried to obtain curcumin micelles. pink.

[0055] 2.3 Preparation of MPEG-PCL-Phe(Bz) / curcumin micelles

[0056] 1g of MPEG-PCL-Phe(Bz) was heated to 70°C, melted and stirred, then added 100mg of curcumin and stirred and dissolved in the polymer excipient, cooled to 50°C, a...

Embodiment 3

[0057] Embodiment 3 stability comparative test

[0058] Using the MPEG-PLA disclosed in Chinese patent CN201110231519.7 and the polymer excipients prepared in Example 1.1 respectively, the curcumin micelles were prepared by the film hydration process, and the micellar solutions prepared by the two methods were placed in a constant temperature environment of 37°C Observe the drug precipitation time, by Figure 5 It can be seen that when MPEG-PLA is used as the polymer excipient, the drug is obviously precipitated in less than 24 hours at 37°C, while the patented excipient is used, even after 72 hours, the micellar solution is still clear, indicating that the drug is stably encapsulated in the nucleus of the micelles , indicating that the stability of the micelles is significantly higher than that of the micelles disclosed in CN201110231519.7.

[0059] The curcumin micelles disclosed in Chinese patent CN201110231519.7 and the curcumin micelles disclosed in this patent were resp...

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Abstract

The invention relates to a novel micelle drug-loaded system formed by an amphiphilic segmented copolymer and curcumin. The amphiphilic segmented copolymer comprises a hydrophilic chain segment and a hydrophobic chain segment; the hydrophilic chain segment is polyethylene glycol monomethyl ether, the hydrophobic chain segment is polycaprolactone, and the hydrophobic chain segment is terminated by a hydrophobic group. The hydrophobic group is the group having a tertbutyloxycarbonyl or phenyl ring structure, compatibility of the medicine molecules and the hydrophobic chain segment in the segmented copolymer is improved, mutual effort is increased, at the same time, the hydrophobic group provides large space for accommodating the medicine molecules, the prepared micelle can effectively inhibit the medicine molecules in a core of the micelle, and the medicine molecules are not easy to dissolve out, so that the drug-loaded micelle having high stability can be obtained.

Description

technical field [0001] The invention relates to a loading system formed by an amphiphilic block copolymer and curcumin and a preparation method thereof, and belongs to the field of nanomedicine preparations. Background technique [0002] Tumor is a kind of disease that seriously threatens the safety of human life. The study of safe and effective anti-tumor drugs is of great significance to improve the quality of human life. [0003] Curcumin (curcumin) is a polyphenolic compound extracted from the rhizomes of turmeric, curcuma, turmeric, etc. [0004] [0005] Pharmacological experiments show that curcumin has a variety of pharmacological effects, including anti-inflammatory, anti-cancer, anti-oxidation, kidney protection, inhibition of pulmonary fibrosis, inhibition of liver fibrosis, helping muscle damage repair, treatment of cataracts, anti-parasitic diseases, etc., especially In terms of tumor prevention and treatment, it may become a very promising anti-tumor drug c...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/12A61K45/06A61K47/34A61P35/00C08G63/91C08G63/664C08G63/85
Inventor 刘珂郎跃武许卉范华英胡代强韩飞其他发明人请求不公开姓名
Owner SUZHOU LEINA PHARMA RES DEV
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