Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug

A doxorubicin and amphiphilic technology, which is applied in the field of amphiphilic rod-shaped polymeric prodrugs and their preparation, can solve the problems of strong toxic and side effects, non-selectivity, low medical efficiency and the like, and achieve the effect of effective treatment

Active Publication Date: 2019-10-22
SOUTHWEST UNIV
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  • Description
  • 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 a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug
  • Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug
  • Preparation method of a class of pH-responsive amphiphilic rod-shaped doxorubicin polymer prodrug

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Embodiment 1

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

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

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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 fields of chemical medicine and biological application, in particular to a pH-stimulated amphiphilic rod-like polymeric prodrug 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. Adriamycin is a cycle non-specific drug, which has effects on a variety of tumors. Therefore, it is effective on tumor cells of various growth cycles All have a killing effect. Doxorubicin is mainly applicable to 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 first-line drug is resistant. Its mechanism of action is mainly that the drug intercalates i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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 UNIV
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