Preparation and application of a sodium alginate-based anti-tumor drug delivery system with variable particle size gating

An anti-tumor drug, sodium alginate technology, applied in the direction of anti-tumor drugs, drug combinations, medical preparations of non-active ingredients, etc., can solve the problems of increasing drug penetration, achieve high drug loading capacity, and achieve fixed-point drug release Effect

Active Publication Date: 2021-04-30
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the dysfunction of tumor vasculature as well as the high interstitial pressure of the tumor itself, most targeted drug delivery systems can only penetrate 3–5 cell diameters and are mainly located around tumor blood vessels.
Overcoming these deficiencies and increasing drug penetration into the tumor parenchyma are major challenges in developing effective cancer chemotherapy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The present invention is a sodium alginate-based variable particle size gating anti-tumor drug delivery system, which specifically includes the following steps:

[0029] (1) Synthesis of CRGDK-Alg conjugates:

[0030] Dissolve 1g of sodium alginate in 2-(N-morpholine)ethanesulfonic acid (MES) buffer containing 0.3M NaCl at a mass concentration of 0.1M pH6.5 to obtain a mass volume ratio (w / v) of 1%. Alg solution; add 21.6mg of N-hydroxysulfosuccinimide (Sulfo-NHS) and 9.58mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide (EDC) to activate, and the reaction solution; 28.88 mg CRGDK was dissolved in 80 μL MES buffer, added to the above reaction solution, stirred at room temperature for 12 h, the product was purified by dialysis against double distilled water for 1 day, MWCO=4000, and lyophilized to obtain CRGDK-Alg Union;

[0031] (2) Preparation of CRGDK-FeAlg / DOX drug delivery system:

[0032] Add DOX to double distilled water to prepare a 10 mg / ml DOX solution; add...

Embodiment 2

[0035] The present invention is a sodium alginate-based variable particle size gating anti-tumor drug delivery system, which specifically includes the following steps:

[0036] (1) Synthesis of CRGDK-Alg conjugates:

[0037] Dissolve 1g of sodium alginate in 2-(N-morpholine)ethanesulfonic acid (MES) buffer containing 0.3M NaCl at a mass concentration of 0.1M pH6.5 to obtain a mass volume ratio (w / v) of 1%. Alg solution; add 108.56mg of N-hydroxysulfosuccinimide (Sulfo-NHS) and 47.93mg of 1-ethyl-(3-dimethylaminopropyl) carbodiimide (EDC) to activate, and the reaction solution; 144.4 mg CRGDK was dissolved in 100 μL MES buffer, added to the above reaction solution, stirred at room temperature for 18 h, the product was purified by dialysis against double distilled water for 2 days, MWCO=3500, and lyophilized to obtain CRGDK-Alg Union;

[0038] (2) Preparation of CRGDK-FeAlg / DOX drug delivery system:

[0039] Add DOX to double distilled water to prepare a 10 mg / ml DOX solution...

Embodiment 3

[0042] The present invention is a sodium alginate-based variable particle size gating anti-tumor drug delivery system, which specifically includes the following steps:

[0043] (1) Synthesis of CRGDK-Alg conjugates:

[0044] Dissolve 1g of sodium alginate in 2-(N-morpholine)ethanesulfonic acid (MES) buffer containing 0.3M NaCl at a mass concentration of 0.1M pH6.5 to obtain a mass volume ratio (w / v) of 1%. Alg solution; add 216mg of N-hydroxysulfosuccinimide (Sulfo-NHS) and 95.8mg of 1-ethyl-(3-dimethylaminopropyl)carbodiimide (EDC) for activation to obtain a reaction solution ; Dissolve 288.8 mg CRGDK in 120 μL MES buffer, add to the above reaction solution, stir at room temperature for 24 hours, dialyze and purify the product against double distilled water for 2 days, MWCO=3000, freeze-dry to obtain CRGDK-Alg coupling thing;

[0045] (2) Preparation of CRGDK-FeAlg / DOX drug delivery system:

[0046] Add DOX to double distilled water to prepare 10 mg / ml DOX solution; add th...

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Abstract

The invention relates to the preparation and application of a sodium alginate-based variable particle size gating antitumor drug delivery system, which can effectively solve the problem of antitumor drug preparation; Peptide ligands were grafted on the sodium acid skeleton, mixed evenly with doxorubicin under ultrasonic conditions, and FeCl was added dropwise 3 A cross-linking agent, which covalently cross-links with -COOH on the molecular skeleton of sodium alginate to form a nano hydrogel, and at the same time packs doxorubicin in the space grid structure of the nano gel, namely; the preparation method of the present invention Simple, energy-saving and environmentally friendly, the prepared anti-tumor drug delivery system has the ability of tumor-triggered phase inversion, which can realize the release of drugs in response to the tumor microenvironment; realize the particle size transformation through the stimulation of the tumor microenvironment, and realize the deep penetration of the tumor; activate endogenous H 2 o 2 →•OH conversion, realize O-free 2 Participating in tumor chemokinetics-chemotherapy combination therapy, providing new ideas for improving the efficiency of chemotherapy drugs for tumor treatment.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to the preparation and application of a sodium alginate-based antitumor drug delivery system with variable particle size gating. Background technique [0002] At present, the safety and clinical application of nano-preparations have received more and more attention. Sodium alginate (Alg) is a natural anionic polyelectrolyte polysaccharide extracted from kelp or seaweed, composed of β-D-mannuronic acid (M) and its C-4 epimer α-L-guluronic Two structural units of acid (G) are connected by (1→4) glycosidic bonds in three ways (MM segment, GG segment, MG segment). Alg belongs to linear anionic polymer, its skeleton is rich in carboxyl groups, and the Na on the G unit + Can be compared with Fe 3+ Most metal cations (except magnesium) undergo ion exchange reactions, and through metal coordination interactions, G units stack to form a characteristic egg-shaped space structure,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/36A61K47/42A61K31/704A61P35/00
CPCA61K9/06A61K31/704A61K47/36A61K47/42A61P35/00
Inventor 张慧娟张振中陈俭娇张红岭侯琳
Owner ZHENGZHOU UNIV
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