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Hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) and preparation method and application thereof

A nano-drug carrier and a stable technology, applied in the field of ultra-stable nano-drug carriers, can solve the problems of micellar stability differences and achieve the effects of improved stability, excellent anti-oxidation and biological activity, and favorable hydrophobicity

Inactive Publication Date: 2018-02-02
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have shown that Lu H, Wang J, Bai Y, et al. Ionicpolypeptides with unusual helical stability [J]. Nature communications, 2011, 2: 206. Ionic polypeptides with chiral structure and can be assembled into secondary structures such as α-helical The stability of micelles is better than that of micelles with random coil structure, and the L-type and D-type chiral characteristics of amino acids make the helical structure of polypeptides have left-handed and right-handed points. Can different helical directions lead to micellar stability? The difference has not been reported so far

Method used

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  • Hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) and preparation method and application thereof
  • Hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) and preparation method and application thereof
  • Hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Ultra-stable nano drug carrier mPEG-PGlu(D)-VE(D), represented by formula I:

[0054]

[0055] where m=227, n=25;

[0056] The mPEG-PGlu(D)-VE(D) is an abbreviation of aminated polyethylene glycol monomethyl ether-D-polyglutamic acid-D-vitamin E.

[0057] m can also be any one of 113-273, n can also be any one of 5-50.

Embodiment 2

[0059] The preparation method of ultra-stable nano drug carrier mPEG-PGlu(D)-VE(D) (m=227, n=25), comprises the steps:

[0060] (1) Dissolve 0.5g of D-glutamic acid-5 benzyl ester (BDG) (II) and 0.31g of triphosgene in anhydrous tetrahydrofuran, react at 55°C for 90min, after the reaction, cool down to room temperature, and concentrate the solution by rotary evaporation to 2 mL, the solution was dropped dropwise into 10 mL of ice n-hexane under a low-temperature stirring reaction bath at -20°C, and a white precipitate was formed. The white precipitate obtained by suction filtration was placed in a 50mL beaker, heated and dissolved with 2mL tetrahydrofuran, and n-hexane was added dropwise until it became cloudy and did not disappear. . Suction filtration obtains and obtains D-benzyl glutamate-N-carboxylic acid anhydride (BDG-NCA) (III); see figure 1 ;

[0061] Experiments have shown that 1,4-dioxane, chloroform or ethyl acetate is used to replace the anhydrous tetrahydrofura...

Embodiment 3

[0076] Ultra-stable nano drug carrier mPEG-PGlu(D)-VE(D) (prepared in Example 2, where m=227, n=25) and its reference substances mPEG-PGlu(D)-VE(DL), mPEG-PGlu Structural verification of (L)-VE(D), mPEG-PGlu(L)-VE(DL), mPEG-PGlu(DL)-VE(D) and mPEG-PGlu(DL)-VE(DL). (the preparation of above-mentioned reference substance is prepared with reference to the method for embodiment 2)

[0077] Prepare the concentration of 12.5μg / mL D-α-tocopherol and DL-α-tocopherol, 0.2mg / mL three kinds of polypeptide main chain mPEG-PGlu(D), mPEG-PGlu(L) and mPEG- Methanol solution of PGlu(DL) and 0.25mg / mLmPEG-PGlu(D)-VE(D) and the above five different chiral structure combinations and polypeptide vitamin E conjugate reference substance without chiral structure. Scan the UV wavelength of each sample solution;

[0078] See Figure 5 ;

[0079] In the figure, the maximum ultraviolet absorption peaks of the two vitamin Es are at 292nm, and the maximum ultraviolet absorption peaks of the three vita...

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Abstract

The invention discloses a hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) and a preparation method and application thereof. The hyperstable nano-drug carrier mPEG-PGlu(D)-VE(D) is expressed in the formula I in the specification. Micelle stability is improved through a chiral structure / secondary structure. Hyperstable polymeric nano-micelle prepared from the hyperstable nano-drug carrier can stably encapsulate and deliver various drug molecules. Systematic circulation stability of micelle is raised, and drug bioavailability and efficacy are improved. The product has excellent biocompatibility,and collaborative treatment is realized.

Description

technical field [0001] The invention relates to an ultra-stable nano drug carrier mPEG-PGlu(D)-VE(D), its preparation method and application. Background technique [0002] The rapid development in the field of nanoscience has brought new opportunities for the advancement of biomedicine. Polymer conjugated micelles are a new class of nanocarriers with excellent drug delivery properties. The unique amphiphilic core-shell structure of micelles can wrap insoluble drugs in its hydrophobic core to avoid drug aggregation during blood circulation. In the process of micellar design, increasing the drug loading capacity of micelles and prolonging the systemic circulation time of micelles are essential considerations for improving drug efficacy and drug bioavailability. [0003] After the micelles enter the blood, if the concentration is diluted by the blood to below the critical micelle concentration (CMC), the micellar structure will be cracked, and the drug will be released in adva...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/22A61K47/18A61K47/10
CPCA61K9/1075A61K47/10A61K47/183A61K47/22
Inventor 赵燕军王征高敏
Owner TIANJIN UNIV
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