Preparation method and application for cRGD-modified pH-sensitive polylactic acid nanoparticles

A technology of nanoparticles and polylactic acid, which can be applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the problems of limited application of polymer nanoparticles and so on.

Inactive Publication Date: 2020-02-18
温宁
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Biocompatible and biodegradable polymer nanoparticles, such as polyemulsion, ε-caprolactone, and polylactide, have high drug loading capacity and encapsulation efficiency, but the high hydrophobicity of the polymer host properties, making the application of these polymeric nanoparticles limited

Method used

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  • Preparation method and application for cRGD-modified pH-sensitive polylactic acid nanoparticles
  • Preparation method and application for cRGD-modified pH-sensitive polylactic acid nanoparticles
  • Preparation method and application for cRGD-modified pH-sensitive polylactic acid nanoparticles

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Embodiment 1

[0032] (1) Synthesis of 2-benzylamine-1,3-propanediol carbonate (CAB) monomer: 5g 2-amino-1,3-propanediol was dissolved in 150mL of NaHCO 3 Solution (10%), first mixed with 75mL of 1,4-dioxane, then added 7.5mL of benzyl chloroformate, stirred at room temperature for 10h; ethyl acetate extracted 2-benzylamide-1,3-propanediol, Evaporate to dryness under reduced pressure. Then take 5g of dry matter and mix with 4.2mL ethyl chloroformate, dissolve in the mixed solution of 150mL tetrahydrofuran and 6.2mL triethylamine, further react, remove triethylamine hydrochloride by filtration, purify with tetrahydrofuran / diethyl ether, and obtain CAB single body;

[0033](2) Preparation of polylactic acid-based polymer: Diethyl zinc is used as an initiator, CAB monomer and lactide monomer are polymerized at a molar ratio of 2:1, and then benzyl groups are removed to obtain P(LA-co- CA) monomer; 100 mg of P(LA-co-CA) monomer and 600 mg of polyethylene glycol aldehyde were dissolved in 5 mL ...

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Abstract

The invention discloses a preparation method for cRGD-modified pH-sensitive polylactic acid nanoparticles and an antitumor application of the nanoparticles. The method includes the following steps: step 1, synthesis of a 2-benzylamino-1,3-propylene glycol carbonate monomer; step 2, preparation of a polylactic acid-based polymer; step 3, preparation of polylactic acid nanoparticles; and step 4, preparation of the doxorubicin-supported polylactic acid nanoparticles. The injectable nanoparticles with pH-sensitive properties prepared by the method can be used as carriers of anti-tumor drugs, realizes the active targeted modification of cRGD polypeptides, and realizes pH-controlled drug release; the performance of the product obtained by the method meets the basic requirements of the nano-drugcarriers, physical encapsulation of doxorubicin is realized, and after intravenous injection, the nanoparticles can be enriched in tumor sites and realize pH-sensitive release, thereby realizing anti-tumor drug targeting and slow drug release; and the nanoparticles improve the tumor suppression rate, reduce toxic and side effects of the antitumor drugs, and have the potential to become the drug carriers.

Description

technical field [0001] The invention belongs to the field of material preparation and application, and in particular relates to a preparation method of pH-sensitive polylactic acid nanoparticles and an antitumor application. Background technique [0002] At present, the research on polymer nano drug delivery system mainly focuses on three categories: polymer nanoparticles, polymer micelles and dendrimers. Due to the relatively large molecular weight of the polymer, this type of drug delivery system can prolong the residence time of the drug at the tumor site; the use of degradable materials to construct the polymer can effectively avoid the residue of the carrier material in the body after the drug is released; by adjusting the polymer material The solubility, surface charge or the introduction of specific chemical bonds can control the release of drugs in vivo; many modification sites of polymer materials can be connected with different markers to prepare different targeted...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K9/52A61K47/34A61K47/42A61K31/704A61P35/00
CPCA61K9/5146A61K9/5169A61K31/704A61P35/00
Inventor 李云霞张建军温宁王宇付之光王欢欢
Owner 温宁
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