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A kind of acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle 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: 2018-04-24
黑龙江省工研院资产经营管理有限公司
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  • Abstract
  • Description
  • 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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  • A kind of acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle and preparation method thereof
  • A kind of acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle and preparation method thereof
  • A kind of acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle 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 active aldehydes on the surface of the dextran structure through an oxidation reaction base to obtain polyaldehyde dextran, and then react polyaldehyde dextran with hexamethylenediamine to generate hexamethylenediamine-polyaldehyde dextran, and the hexamethylenediamine-polyaldehyde dextran has a stable carbon-nitrogen unit bond structure, and carry 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 Self-assembled into nano-micelles in water, that is, acid-sensitive amphiphilic stearic acid amidated dextran polymer nano-micelles.

specific Embodiment approach 2

[0037] Specific embodiment two: This embodiment is a preparation method of acid-sensitive amphiphilic stearic acid amidated dextran polymer nanomicelle, which is specifically completed according to the following steps:

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

specific Embodiment approach 3

[0046] Embodiment 3: The difference between this embodiment and Embodiment 2 is that the average molecular weight of the dextran in Step ① is 10,000. Others are the same as in 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 cancer deaths in China alone reached more than 2.8 million (about 7,500 people per day on average). However, the current clinical anticancer drugs still have strong toxicity, water-soluble There are a series of restrictive factors such as poor drug resistance, short half-life, easy degradation in vivo, and no specific targeting. Therefore, the research and development of new drug carriers is urgently needed. In recent years, research on micellar drug carriers has risen rapidly. Its structure is controllable, and its drug loading capacity and loading rate are high. , Protecting drugs from phagocytosis by the immune system, inducing the targeting of drugs to tumor cells and the response characteristics of pathogenic stimuli. In particular, the self-assembled...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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