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Lysine-based polyesteramide nano drug delivery system as well as preparation method and application thereof

A technology of polyester amide and lysine, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of being unable to entrap drugs in nanoparticles and achieve good biosafety Sexuality, efficient and controllable release, enhanced utilization effect

Active Publication Date: 2020-02-18
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, polyesteramide is a kind of hydrophobic polymer, which cannot self-assemble to form nanoparticles with core-shell structure for drug loading.

Method used

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  • Lysine-based polyesteramide nano drug delivery system as well as preparation method and application thereof
  • Lysine-based polyesteramide nano drug delivery system as well as preparation method and application thereof
  • Lysine-based polyesteramide nano drug delivery system as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1 Preparation of a lysine-based polyester amide polymer drug carrier

[0055] 1, the preparation method of the polyester amide polymer based on lysine, comprises the following steps:

[0056] (1) Synthesis of dibasic carboxylic acid di-p-nitrophenyl ester monomer (Nx):

[0057] (a) Weigh a certain amount of p-nitrophenol, measure the same equivalent of triethylamine, add it into a single-necked flask with enough acetone, stir well at room temperature, and then store it at -78°C with dry ice and acetone Down;

[0058] (b) Measure oxalyl chloride (or succinoyl chloride or suberoyl chloride) slightly less than one-half of the p-nitrophenol equivalent and add it to an appropriate amount of acetone, mix well, and then add the triethyl chloride prepared in the previous step dropwise. In the frozen amine solution, stir at -78°C for 2h, then transfer to 25°C and stir overnight (10-16h);

[0059] (c) adding the reacted solution into a large beaker with sufficient d...

Embodiment 2

[0073] Example 2 Preparation of a lysine-based polyester amide-bovine serum albumin (BSA) nanocomposite drug delivery system (Lys-PEA@BSA)

[0074] 1, its preparation process comprises the following steps:

[0075] The polyester amide polymer aqueous solution of different lysine prepared in Example 1 was mixed with the BSA aqueous solution according to the ratio of material to protein mass ratio of 250:1, and vortexed for 5 minutes to prepare spherical nanoparticles based on Polyesteramide-BSA nanocomposite drug delivery system of lysine.

[0076] 2. Results

[0077] (1) The shape of the prepared nanoparticles was characterized by transmission electron microscopy: the nanoparticles Lys-PEA@BSA exhibited a uniform and dispersed spherical structure with a particle size of less than 100 nm.

[0078] (2) Using dynamic light scattering to characterize the stability of nanoparticles, the blank nanoparticles polyester amide polymer Lys-PEA and the drug-loaded nanoparticles Lys-PEA@...

Embodiment 3

[0080] Example 3 Preparation of a lysine-based polyester amide-insulin nanocomposite drug delivery system (Lys-PEA@INS)

[0081] 1, its preparation process comprises the following steps:

[0082] The polyester amide polymer aqueous solution of different lysine prepared in Example 1 and the insulin hydrochloric acid solution are respectively 10:1, 50:1, 100:1, 250:1, 500:1 according to the mass ratio of material to protein , mixed at a ratio of 1000:1, and vortexed for 5 minutes to prepare a lysine-based polyester amide-insulin nanocomposite drug delivery system (Lys-PEA@INS) in the form of spherical nanoparticles.

[0083] 2. Results

[0084] (1) Characterize the morphology of the prepared nanoparticles by transmission electron microscope: as image 3 As shown, the nanoparticles Lys-PEA@INS have a uniform and dispersed spherical structure with a particle size of less than 100nm.

[0085] (2) Using dynamic light scattering to characterize the stability of nanoparticles, the ...

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Abstract

The invention discloses a lysine-based polyesteramide nano drug delivery system as well as a preparation method and application thereof. The preparation method of the polyesteramide polymer includes the following steps: synthesizing a dicarboxylic acid di-p-nitrophenyl ester monomer; synthesizing a di-lysine di-p-toluenesulfonate ester monomer; and adding the dicarboxylic acid di-p-nitrophenyl ester monomer and the di-lysine di-p-toluenesulfonate ester monomer according to a mass ratio of equal to or less than 1:1 into a reaction solvent, adding triethylamine dropwise under stirring at 65-85 DEG C as a reaction catalyst, and performing a heating reaction at 60-80 DEG C for 24-96 h to obtain the polyesteramide polymer with good water solubility. The polyesteramide polymer can efficiently load and deliver and controllably release water-soluble protein drugs, has good biosecurity and drug release, and significantly improves the stability and bioavailability of the protein drugs in a systemic circulation.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials. More specifically, it relates to a lysine-based polyester amide nano drug delivery system suitable for high-efficiency loading delivery and controlled release of water-soluble protein drugs, as well as its preparation method and application. Background technique [0002] Diabetes mellitus is a metabolic disease that causes hyperglycemia due to impaired blood glucose regulation mechanisms in the body. my country is one of the countries with the fastest growing prevalence of diabetes. Long-term high blood sugar levels in diabetic patients will lead to many complications such as chronic damage and dysfunction of the eyes, kidneys, and heart, which greatly increases the risk of blindness, kidney failure, heart disease, and stroke. seriously affect the quality of life. The formation of long-term hyperglycemia is mainly caused by defects in insulin secretion (absolute lack of insulin), ...

Claims

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Application Information

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IPC IPC(8): C08G69/44C08G69/42A61K9/14A61K9/51A61K38/28A61K47/34A61P3/10
CPCA61K9/146A61K9/5146A61K38/28A61K47/34A61P3/10C08G69/42C08G69/44
Inventor 吴钧韩书彦顾志鹏
Owner SUN YAT SEN UNIV
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