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Preparation of a poly(l-glutamic acid)-b-polyethylene glycol drug-loaded nanomicelle

A drug-loaded nano-polyethylene glycol technology, which is applied to non-active ingredient medical preparations, active ingredient-containing medical preparations, anti-tumor drugs, etc., to enhance drug efficacy, strong salt resistance and dilution resistance , the effect of reducing the probability of drug leakage

Active Publication Date: 2017-08-04
南京邦鼎生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the research on the encapsulation and triggered release of anti-tumor drugs by this kind of stimuli-responsive polymer micelles with cross-linked structure is still in the early stage, but it will surely bring new breakthroughs in the diagnosis and treatment of tumors and other diseases

Method used

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  • Preparation of a poly(l-glutamic acid)-b-polyethylene glycol drug-loaded nanomicelle
  • Preparation of a poly(l-glutamic acid)-b-polyethylene glycol drug-loaded nanomicelle
  • Preparation of a poly(l-glutamic acid)-b-polyethylene glycol drug-loaded nanomicelle

Examples

Experimental program
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Effect test

Embodiment 1

[0018] Embodiment 1: Preparation of thiol-terminated poly(L-glutamic acid-γ-benzyl ester)

[0019] Adding mercaptoethylamine (AET) and BLG-NCA with a molar feed ratio of 1:40 in the three-necked flask replaced with nitrogen in advance, the two are dissolved in methylene chloride solvent, so that the total concentration of reactants is 10w%, Stir magnetically at room temperature in a nitrogen atmosphere for 72 hours, concentrate the reaction solution, and drop it into excess butyl acetate, ice-bath for half an hour to obtain a flocculent precipitate, centrifuge to obtain a light yellow precipitate, and vacuum-dry at 35°C to obtain a terminal mercapto group Poly(L-glutamic acid-γ-benzyl ester), referred to as PLT.

Embodiment 2

[0020] Example 2: Preparation of poly(L-glutamic acid-γ-benzyl ester)-b-polyethylene glycol

[0021] PLT and polyethylene glycol methacrylate (MAPEG) are co-dissolved in the DMF solution, and the molecular weight of the polyethylene glycol methacrylate used is M n =475g / mol, the molar ratio of PLT to polyethylene glycol methacrylate is 1:1~1:1.5, the two are dissolved in DMF solvent, the total concentration of the reactants is 15w%, and the total weight of the reactants is 1 % of AIBN as the initiator, free radical polymerization was carried out at 60°C, and after 24 hours, the reaction solution was added dropwise into ultrapure water to obtain a milky white turbid liquid, which was transferred to a dialysis bag with a molecular weight cut-off of 3500 for dialysis for 72 hours. Change the water every 12 hours, and finally freeze-dry the product to obtain light yellow solid poly(L-glutamic acid-γ-benzyl ester)-b-polyethylene glycol, referred to as PLE;

Embodiment 3

[0022] Example 3: Cross-linking of micelles

[0023] Mix PLE obtained in Example 2 and cystamine into the DMF solvent, cystamine and PLE are fed in molar ratios of 1:1, 2:1, and 4:1 respectively, and the total concentration of the two dissolved in the DMF solvent is 12w %, stirred magnetically at 30°C for 5 hours, cooled to room temperature, took the reaction solution, added dropwise into ultrapure water and stirred until Tyndall effect was evident, dialyzed with a dialysis bag with a molecular weight cut-off of 3500 for 72 hours, and then freeze-dried , and then prepared a micellar solution with a concentration of 0.8w% for later use; a series of cross-linked micelles with different cross-linking degrees were prepared according to the above ratio. Synthetic route see figure 1 .

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Abstract

The invention firstly adopts mercaptoethylamine to trigger ring opening polymerization of L-glutamic acid-gamma-benzyl ester-N-carboxylic acid anhydride (BLG-NCA) to prepare mercaptyl-terminated (L-glutamic acid-gamma-benzyl ester) polymer, the mercaptyl-terminated (L-glutamic acid-gamma-benzyl ester) polymer is used as a macromolecular chain transfer agent to perform free radical polymerization with activated monomer polyethylene glycol metacrylic acid ester (MAPEG, Mn is equal to 475g / mol), and thereby amphiphilic poly(L-glutamic acid)-b-polyethylene glycol is obtained; cystamine is used for crosslinking L-glutamic acid-gamma-benzyl ester therein, meanwhile the residual gamma-benzyl ester groups are converted into carboxylic acid groups and adriamycin amycin is statically loaded, and thereby the nano micelle is formed by self-assembling in aqueous solution.

Description

technical field [0001] The invention relates to the preparation of poly(L-glutamic acid)-b-polyethylene glycol drug-loaded nano micelles, belonging to the technical field of biomaterials and sustained release. Background technique [0002] The special core-shell structure of polymer micelles can be used as a micro-storage of anti-tumor drugs, and it is an ideal drug release system. However, due to the lack of recognition and response functions to tumor cells, traditional polymer micelles cannot release drugs quickly and timely at the tumor site, and the therapeutic effect is not good. There are very few examples of clinical application. It also has problems such as being unable to maintain its own stability in response to changes in the temperature and pH factors of the surrounding environment; at the same time, after the micelles are taken orally or injected into the body and are highly diluted by body fluids, the disintegration of micellar nanoparticles occurs, resulting i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/704A61K47/60A61P35/00C08G69/08C08G81/00C08F293/00
Inventor 倪才华杨期颐张丽萍石刚
Owner 南京邦鼎生物科技有限公司
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