Preparation and application of sodium alginate-based grain size variable door controlled antitumor drug delivery system

An anti-tumor drug and delivery system technology is applied in the field of preparation and application of a variable particle size gated anti-tumor drug delivery system, which can solve problems such as increasing drug penetration, improve drug loading, achieve fixed-point drug release, Effects of high drug loading capacity

Active Publication Date: 2018-12-28
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 ar

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 preparation and application of a sodium alginate-based grain size variable door controlled antitumor drug delivery system and can solve the preparation problem of antitumor drugs effectively. According to the technical scheme, the preparation comprises the following steps: grafting a peptide ligand to a sodium alginate framework by means of a carbodiimide chemical method;uniformly mixing the framework with adriamycin amycin; dropwise adding a FeCl3 crosslinking agent which is covalently crosslinked with -COOH to form a hydrogel; entrapping adriamycin amycin in a spatial lattice structure of the nano gel to obtain the system. The preparation method is simple and energy-saving and environmentally friendly, and the prepared antitumor drug delivery system has a tumortrigger type phase conversion ability, so that responsive drug release of a tumor microenvironment can be achieved. Particle size conversion is achieved by tumor microenvironment stimulation, so thattumor deep penetration is achieved; endogenous H2O2--OH conversion is activated to achieve tumor chemical kinetics-chemotherapy combined treatment without O2, thereby providing a novel concept to improve the tumor treatment efficiency of a chemotherapeutic.

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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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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