Acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle and preparation method thereof

A technology of stearic acid amidated glucan and fatty acid amidated glucan is applied in the field of drug-loaded micelles and their preparation, which can solve the problems of no pH response of stearic acid glucan micelles and the like, and achieve drug-loaded micelles. Release the effect of enhancing and enhancing solubility

Active Publication Date: 2016-08-10
黑龙江省工研院资产经营管理有限公司
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

[0003] The purpose of the present invention will solve the problem that the existing stearic acid dextran micelles have no pH response characteristics, and provide a kind of acid-sensitive type amphiphilic stearic acid amidated dextran polymer nano-micelles and preparation method thereof

Method used

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  • Acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle and preparation method thereof
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  • Acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle and preparation method thereof

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specific Embodiment approach 1

[0036] Specific embodiment 1: This embodiment is an acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle, which uses dextran as a raw material and introduces reactive aldehydes on the surface of the dextran structure through an oxidation reaction Base to obtain polyaldehyde dextran, and then react polyaldehyde dextran with hexamethylene diamine to generate hexamethylene diamine-polyaldehyde dextran. The hexamethylene diamine-polyaldehyde dextran has a stable carbon Bond structure and carrying active amino groups; hexamethylenediamine-polyaldehyde dextran is acylated with stearic acid to obtain stearic acid amidated dextran polymer, and the amphiphile of stearic acid amidated dextran polymer It self-assembles into nanomicelles in water, which is acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelles.

specific Embodiment approach 2

[0037] Specific embodiment 2: This embodiment is a method for preparing acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelles, which is specifically completed as follows:

[0038] 1. Preparation of polyaldehyde dextran: ①. Dissolve dextran in distilled water to obtain an aqueous solution of dextran with a concentration of 5mmol / L~15mmol / L; ②. Dissolve sodium periodate in distilled water to obtain concentration Sodium periodate aqueous solution of 0.11mol / L~0.33mol / L; ③, the concentration of dextran aqueous solution with the concentration of 5mmol / L~15mmol / L and the concentration of 0.11mol / L~0.33mol / under dark conditions L sodium periodate aqueous solution was mixed, and the reaction was stirred for 4h-8h at a temperature of 25°C and a rotation speed of 800r / min~1600r / min in a dark condition to obtain the reaction product. The reaction product was transferred to the dialysis bag. The molecular weight cut-off of the dialysis bag is 3500, the deionized wate...

specific Embodiment approach 3

[0046] Specific embodiment three: The difference between this embodiment and the specific embodiment two is: the average molecular weight of the glucan in step one (1) is 10,000. Others are the same as the second embodiment.

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Abstract

The invention provides an acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle and a preparation method thereof and relates to a drug-loading micelle and a preparation method thereof. According to the acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle and the preparation method, the problem that stearic acid glucan micelles in the prior art have no pH response property. According to the preparation method, a stearic acid amidated glucan polymer is prepared from glucan as a raw material by virtue of oxidization, hexamethylendiamine reduction reaction and stearic acid amidation and is self-assembled in water by virtue of amphipathicity so as to form the nano-micelle. The preparation method comprises the following steps: (1) preparing polyaldehyde glucan; (2) preparing hexamethylendiamine-polyaldehyde glucan; (3) preparing stearic acid amidated glucan; and (4) carrying out self-assembling to form the nano-micelle, so as to obtain the acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle. The acid-sensitive amphipathic stearic acid amidated glucan polymer nano-micelle prepared by virtue of the preparation method is used as a carrier of hydrophobic antitumor drugs.

Description

Technical field [0001] The invention relates to a drug-loaded micelle and a preparation method thereof. Background technique [0002] Cancer is one of the major public health problems in the world. In 2015, the number of deaths due to cancer in China alone reached more than 2.8 million (about 7500 people per day on average), but the current clinical anti-cancer drugs still have strong toxicity and water solubility in practical applications. A series of restrictive factors such as poor performance, short half-life, easy degradation in the body, no specific targeting, etc. Therefore, the development and preparation of new drug carriers are urgently needed. In recent years, the research of micellar drug carriers has risen rapidly, with controllable structure, high drug loading and high loading rate, which can enhance drug efficacy, reduce toxicity, increase blood drug concentration, control drug release, and promote the solubilization and oxygen carrying of hydrophobic drugs. , Pro...

Claims

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Application Information

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IPC IPC(8): C08J3/07C08L5/02C08B37/02A61K9/107A61K47/36A61P35/00
CPCA61K9/1075A61K47/36C08B37/0006C08J3/07C08J2305/02
Inventor 王路李玮李书彬王振宇
Owner 黑龙江省工研院资产经营管理有限公司
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