Application of Sodium Alginate as Targeting Carrier of Antineoplastic Drugs

An anti-tumor drug, sodium alginate technology, applied in anti-tumor drugs, anti-bacterial drugs, drug combinations, etc., can solve problems such as poor biological selectivity and easy aggregation

Active Publication Date: 2021-04-27
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 Targeting Carrier of Antineoplastic Drugs
  • Application of Sodium Alginate as Targeting Carrier of Antineoplastic Drugs
  • Application of Sodium Alginate as Targeting Carrier of Antineoplastic Drugs

Examples

Experimental program
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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)1721 cm -1 ; υ as (COO − ) 1635 cm -1 ; υ s (COO - ) 1394 cm -1 ; υ (C-O-C) 1236cm -1 ; υ (C-OH) 1028cm -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. The invention utilizes the selectivity of the scavenger receptors on the surface of tumor tissue-associated macrophages to sodium alginate, uses sodium alginate as a carrier, and couples the carboxyl group on the sodium alginate with the amino group in the phthalocyanine compound via an amide bond. Jointly generate the phthalocyanine-sodium alginate conjugate, which not only has high photosensitivity and excellent water solubility and biocompatibility, but also can pass through the scavengers on the surface of tumor-associated macrophages due to sodium alginate Receptor A enters the interior of the cell to achieve its enrichment in tumor tissue, so it has good tumor targeting and can be applied to photodynamic anticancer and photodynamic diagnosis.

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 Patents(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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