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Application of sodium alginate as antitumor drug targeting carrier

An anti-tumor drug, sodium alginate technology, used in anti-tumor drugs, anti-bacterial drugs, drug combinations, etc., can solve the problems of poor biological selectivity and easy aggregation, and achieve significant anti-tumor effects, rich sources, and improved Effects of Aggregate Behavior

Active Publication Date: 2020-04-17
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the currently reported biologically active phthalocyanine complexes still have shortcomings, such as easy aggregation in physiological solutions, poor bioselectivity, etc., which limit their clinical application.

Method used

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  • Application of sodium alginate as antitumor drug targeting carrier
  • Application of sodium alginate as antitumor drug targeting carrier
  • Application of sodium alginate as antitumor drug targeting carrier

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] A conjugate prepared using sodium alginate as a targeting carrier, the preparation method comprising the following steps:

[0031] 1) Disperse sodium alginate in 70 vol% formic acid / water solution or 1M hydrochloric acid / ethanol solution, stir in ice water for 1 hour, transfer to 20~35°C and continue stirring for 5 hours, filter, and obtain crude alginic acid Wash with 70vol%~95vol% ethanol aqueous solution and acetone, disperse it in purified water after vacuum drying, slowly add 10~40 wt% tetrabutylammonium hydroxide aqueous solution to adjust pH=8±1, then freeze immediately, and carry out lyophilization, Obtain tetrabutylammonium alginate;

[0032] 2) Dissolve the obtained tetrabutylammonium alginate in DMSO, and stir at 20-35°C under the protection of nitrogen to dissolve completely; then add CMPI dissolved in DMSO and activate for 1 hour; then add phthalocyanine compound and three Ethylamine, continue to react for 20 hours, finally add 2.5M NaCl solution to the re...

Embodiment 1

[0042] (1) Preparation of alginic acid

[0043] Disperse 2 g (9.1 mmol) of low-molecular-weight sodium alginate (MW=40kDa, 9.1 mmol of repeating units) in 100 mL of formic acid / water solution (7:3, v / v) at 4°C, and stir in ice water for 1 h. Transfer to 20~35°C and continue to stir for 5 hours, then filter, the obtained crude alginic acid is washed with 300mL of absolute ethanol, and then washed with 100mL of acetone, and vacuum-dried at 40°C to obtain 1.44g of light yellow powdery solid, which is alginic acid (1).

[0044] Product Characterization Data: FTIR (ATR): υ (OH) 3371 cm -1 ; υ as (CH) 2925cm -1 ; υ (C=O inCOOH) 1723 cm -1 ; υ as (COO − ) 1636 cm -1 ; υ s (COO - ) 1402 cm -1 ; υ (C-O-C) 1232 cm -1 ; υ (C-OH)1029 cm -1 .

[0045] (2) Synthesis of tetrabutylammonium alginate

[0046] Disperse 1g (repeating unit 5mmol) of alginic acid in 200mL of purified water, then slowly adjust the pH=8±1 with 40wt% tetrabutylammonium hydroxide aqueous sol...

Embodiment 2

[0049] Adjust the molecular weight of sodium alginate in step (1) of Example 1 to 1230 kDa, except for washing with 300mL ethanol / water solution (7:3, V:V) and then washing with 100mL acetone, other steps are carried out in the same way In Example 1, 1.51g of alginic acid (2) and 2.03g of tetrabutylammonium alginate (2) were obtained.

[0050] Product characterization data are as follows:

[0051] Alginic acid (2): FTIR (ATR): υ (OH) 3359 cm -1 ; υ as (CH) 2925cm -1 ; υ (C=O in COOH) 1721cm -1 ; υ as (COO − ) 1635 cm -1 ; υ s (COO - ) 1394 cm -1 ; υ (C-O-C) 1236cm -1 ; υ (C-OH) 1028 cm -1 .

[0052] Tetrabutylammonium Alginate (2): FTIR (ATR): υ (OH) 3384 cm -1 ; υ (CH) 2961cm -1 , 2935 cm −1 and 2875cm −1 ; υ as (COO - ) 1603cm -1 ; δ as (CH 2 and CH 3 ) 1487 cm −1 and 1465 cm −1 ; δ s (CH 3 )1385 cm −1 ;(C-O) 1315 cm −1 and 1285cm −1 ;(C-O-C) 1171 cm −1 , 1147 cm −1 and 1099cm −1 , (C-OH) 1031 cm −1 .

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Abstract

The invention discloses an application of sodium alginate as an antitumor drug targeting carrier and a phthalocyanine-sodium alginate conjugate prepared based on the application. According to the invention, the characteristic that a scavenger receptor on the surface of tumor tissue related macrophages has selectivity on sodium alginate is utilized; sodium alginate is used as a carrier; the phthalocyanine-sodium alginate conjugate is generated by coupling a carboxyl group on sodium alginate and amino in a phthalocyanine compound through an amido bond. The conjugate not only has high photosensitive activity and excellent water solubility and biocompatibility, but also has good tumor targeting and can be applied to photodynamic anti-cancer and photodynamic diagnosis due to the fact that sodium alginate can enter cells through scavenger receptors A on the surfaces of tumor-associated macrophages to achieve enrichment of sodium alginate in tumor tissues.

Description

technical field [0001] The invention belongs to the field of medicine preparation, and in particular relates to an application of sodium alginate as an antitumor drug targeting carrier, and a phthalocyanine-sodium alginate conjugate prepared based on the application. Background technique [0002] Tumor-associated macrophages (TAMs) are abundant and widely present in various tumor tissues, so TAMs can be used as effective targets for anti-tumor therapy and diagnosis. The surface of TAM can express a variety of receptors related to its recognition of phagocytosis, including lectin, mannose receptor, scavenger receptor (SR) and so on. [0003] Sodium alginate is a naturally occurring anionic polymer, usually obtained from brown seaweed, which is composed of β-D-mannuronic acid (β-D-mannuronic, M) and α-L-guluronic acid (α-L-guluronic, G) is a linear copolymer linked by (1→4) glycosidic bonds. Sodium alginate is widely used in the field of biomedicine because of its natural ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/61A61P35/00A61P31/04A61P1/02A61P9/10A61P17/02A61P17/00A61P31/12A61K49/00
CPCA61K41/0071A61K49/0036A61K47/61A61P1/02A61P9/10A61P17/00A61P17/02A61P31/04A61P31/12A61P35/00
Inventor 黄剑东唐凤翔谢伟李思聪郑碧远
Owner FUZHOU UNIV
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