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A kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine

A technology of multi-arm polyethylene glycol and nano-drugs, which is applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of water-soluble phase difference, low bioavailability, toxic and side effects, etc., and achieve simple operation and biocompatibility Good sex, low toxicity and side effects

Inactive Publication Date: 2019-02-15
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to aim at the deficiencies in the prior art, provide a kind of pectin-multi-armed polyethylene glycol self-assembly method for preparing nano-medicine, pectin and drug-loaded multi-armed polyethylene glycol can self-assemble in aqueous medium Assemble and form nanoparticles to solve the problems of UA's water-soluble phase difference and low bioavailability. Using pectin and eight-armed polyethylene glycol as drug carriers has good targeting and high drug loading, and avoids incomplete release and sudden release of drugs. Toxic and side effects on patients

Method used

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  • A kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine
  • A kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine
  • A kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine

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Effect test

Embodiment 1

[0026] Embodiment 1, a kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine:

[0027] (1) Acetylation of PET

[0028] Take a certain amount of PET (the degree of esterification is 50% to 75%), slowly add glacial acetic acid, acetic anhydride and sulfuric acid, react for a period of time under ice bath, then raise the temperature to 50°C, stir until the solution is clear, spin the mixture, wash with ethanol To neutrality, freeze-dry to obtain acetylated pectin powder A.

[0029] (2) Synthesis of 8ARM-PEG-UA

[0030] Dissolve 0.5 g of eight-armed polyethylene glycol with 10 ml of tetrahydrofuran, add 0.5 g of activator 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), and 0.06 g of catalyst 4 - Dimethylaminopyridine (DMAP), stirred, then added 1mol ursolic acid to react for 36-48 hours, the reactant mixture was rotary evaporated, dialyzed overnight, and the dialysate was freeze-dried to obtain powder B;

[0031] (3) Sy...

Embodiment 2

[0037] Embodiment 2, a kind of pectin-multi-arm polyethylene glycol self-assembly method for preparing nano-medicine:

[0038] In this example, through the same synthetic method and steps as in Example 1, the molar ratio of eight-arm polyethylene glycol to ursolic acid is 1:4, and the eight-arm polyethylene glycol of the described pectin and drug-loaded When the molar ratio is 1:4, the measured particle size is 20-100nm.

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Abstract

The invention discloses a method for preparing a nano-drug through self-assembling of pectin-multi-arm polyethylene glycol. The nano-drug is nano-particles formed by self-assembling of esterification of pectin (PET) hydroxyl and carboxyl of drug-carrying eight-arm polyethylene glycol. Eight-arm polyethylene glycol carries the drug, drug-carrying nano-particles are prepared, and 10-hydroxycamptothecine (HCPT) is wrapped in the self-assembling process. The drug-carrying capacity of the nano-drug prepared through self-assembling of pectin-multi-arm polyethylene glycol is adjustable, eight-arm polyethylene glycol can carry various water-soluble or hydrophobic drugs, and the nano-drug is good in targeting ability, stability and biological degradability and low in toxicity and has a controlled-release function. The method belongs to the field of biological pharmacy and the nanotechnology, and is simple in preparing technological process and short in cycle.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals and nanotechnology, relates to a drug delivery system, in particular to a method for preparing nano-medicine by pectin-multi-arm polyethylene glycol self-assembly. Background technique [0002] Pectin (Pectin) is a polysaccharide macromolecular substance present in the plant cell wall. It is a food-grade macromolecule nutrient substance together with polyethylene glycol. The hydrophobic drug uses macromolecule eight-armed polyethylene glycol and pectin nanocarriers together. Encapsulation and delivery to target cells can achieve the purpose of slow drug release. The self-assembly process encapsulates another drug to achieve mutual promotion, and can realize the synergistic effect of the two drugs, thereby increasing the curative effect. [0003] Ursolic acid (Ursolic acid, referred to as UA), also known as ursolic acid and ursolic acid, is a pentacyclic triterpenoid compound that is widely found ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/61A61K47/60A61K31/56A61K31/4745A61P35/00
CPCA61K31/4745A61K31/56
Inventor 雷建都刘彦雪陈琳琳王璐莹刘静何静
Owner BEIJING FORESTRY UNIVERSITY
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