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Preparation method of pH-responsive amphiphilic rod-like adriamycin polymer prodrug

An amphiphilic and doxorubicin technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of strong toxic and side effects, poor blood circulation stability, and low medical efficiency, etc. problems, to achieve effective treatment

Active Publication Date: 2018-01-19
SOUTHWEST UNIVERSITY
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  • Claims
  • Application Information

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Problems solved by technology

[0003] The most common problems of anticancer drug molecules including doxorubicin are poor water solubility, small molecular size and non-selectivity. In the process of drug delivery, there are poor blood circulation stability, low drug bioavailability, strong side effects and Low medical efficiency and other issues

Method used

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  • Preparation method of pH-responsive amphiphilic rod-like adriamycin polymer prodrug
  • Preparation method of pH-responsive amphiphilic rod-like adriamycin polymer prodrug
  • Preparation method of pH-responsive amphiphilic rod-like adriamycin polymer prodrug

Examples

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Embodiment 1

[0040] Example 1 Preparation of pH-responsive Dex-P(MGMA)-b-P(OEGMA) amphiphilic rod-like polymeric prodrugs

[0041] (1) Preparation of Dex-Br: under argon atmosphere, dextran (Dex) dissolved in ionic liquid (1-allyl-3-methylimidazole chloride) was cooled to 0 °C, and N was added. -Mixed solution of methylpyrrolidone (NMP) and N,N-dimethylformamide (DMF), then slowly add 2-bromoisobutyryl bromide (BIBB), ice bath for 0.5-2h, then warm to room temperature (25 ℃) and react in the dark for 12-72h, then precipitate in deionized water, dissolve the obtained precipitate with acetone, and repeat the purification three times to obtain a light yellow intermediate product, which is dried in a vacuum drying oven (25-30 ℃), and then the obtained The pale yellow intermediate product was dissolved in NMP, cooled to 0°C, then slowly added BIBB, ice bathed for 0.5-2h, then warmed to room temperature (25°C) and reacted in the dark for 12-72h, then precipitated in deionized water, washed with ...

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Abstract

The invention relates to the fields of chemical synthesis and biological representation, and more particularly, provides a preparation method and an application of a pH-responsive amphiphilic rod-likepolymer prodrug, which is represented as the drawing in the specification. The preparation method of the amphiphilic rod-like polymer material includes the following steps: 1) synthesizing a rod-likeATRP initiator on the basis of glucan; 2) introducing a pH-responsive hydrophobic block on the basis of ATRP reaction; 3) introducing a hydrophilic block on the basis of ATRP reaction to obtain an amphiphilic polymer material; 4) substituting an ester group on the terminal of MGMA by means of hydrazine hydrate, thus producing a pH-responsive precursor; 5) forming a hydrazone bond by means of a carbonyl group on adriamycin and an amino group on the polymer material, thus producing the pH-responsive polymer prodrug. By means of weak acidity of interior of cancer cells, the amphiphilic rod-likepolymer prodrug can selectively release a drug by means of pH-stimulating response. The polymer prodrug is high in micelle stability, is high in drug carrying capacity and enables drug release to be under stimulating response control.

Description

technical field [0001] The invention relates to the field of chemical medicines and biological applications, in particular to an amphiphilic rod-shaped polymeric prodrug responsive to pH stimulation and its preparation and use. Background technique [0002] Doxorubicin (DOX) is one of the common anticancer drugs, its CAS number: 23214-92-8, chemical structure: C 27 H 29 NO 11 , relative molecular weight: 543.52, it can inhibit the synthesis of RNA and DNA, and has the strongest inhibitory effect on RNA. Doxorubicin is a cycle non-specific drug, which has an effect on a variety of tumors. Therefore, it can inhibit tumor cells of various growth cycles. All have a killing effect. Doxorubicin is mainly used for acute leukemia, and has a certain therapeutic effect on acute lymphoblastic leukemia and myeloid leukemia. It is generally used as a second-line drug, that is, it can be considered when the drug is resistant to the first choice. Its mechanism of action is mainly that ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/56A61K9/107A61K31/704A61P35/00C08B37/02C08F251/00C08F285/00C08F8/30C08F8/32C08F220/28
Inventor 许志刚石潇潇马晓倩白霜薛鹏康跃军
Owner SOUTHWEST UNIVERSITY
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