Cubic cyclodextrin framework-RGD composition and preparation method thereof

A technology of cyclodextrin and composition, applied in the field of cubic cyclodextrin skeleton-RGD composition and its preparation

Active Publication Date: 2020-07-24
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, most previous studies have focused on spherical carriers, and no one has attempted to use cubic carriers for targeted therapy of hemorrhage.

Method used

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  • Cubic cyclodextrin framework-RGD composition and preparation method thereof
  • Cubic cyclodextrin framework-RGD composition and preparation method thereof
  • Cubic cyclodextrin framework-RGD composition and preparation method thereof

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preparation example Construction

[0244] Preparation method of cubic cyclodextrin skeleton-RGD composition

[0245] The invention provides a preparation method of a cubic cyclodextrin skeleton-RGD composition.

[0246] In a preferred embodiment of the present invention, a pharmaceutically acceptable cyclodextrin is used as an organic linker, K + As an inorganic metal center, prepare CD-MOF with cubic shape and uniform particle size, use a cross-linking agent to cross-link the CD of CD-MOF to prepare a stable COF in the aqueous phase, and pass the carboxyl (-COOH) of the RGD sequence through ester bonded to the surface of COF to form a cubic cyclodextrin skeleton-RGD composition (RGD-COF). The CD-MOF involved in the present invention is based on a method for preparing cyclodextrin-metal organic framework material (201610125456.X), which is fast, simple, adjustable in size and high in yield.

[0247] In yet another preferred embodiment of the present invention, the preparation method of the cubic cyclodextrin ...

Embodiment 1

[0264] Preparation of nano-scale CD-MOF: Use solvothermal method to directly heat the mixed system of γ-CD, KOH aqueous solution and a part of organic solvent. Weigh 163.0mg of γ-CD and 56.0mg of KOH mixture (γ-CD and KOH molar ratio is 1:8) and dissolve it in 5mL of water, pre-add 3mL of methanol to the mixed solution, heat in a water bath at 50°C for 20min, take out the solution, add Add an equal volume of methanol, then add 64mg PEG20000, let it stand for 1h, centrifuge at 4000rpm for 5min, wash with ethanol (10mL×2) and dichloromethane (10mL×2) respectively, and vacuum-dry the obtained crystals at 50°C for 12h to obtain nano Grade CD-MOF crystal (CD-MOF-Nano), the obtained CD-MOF is in the shape of a regular cube with a particle size of 200-500nm ( figure 1 ).

[0265] Preparation of nanoscale COF: Weigh 778.3mg of nanoscale CD-MOF powder into a round bottom flask, fix it on a magnetic stirrer, add 10mL of dimethylformamide, heat at 80°C, and add 771mg of crosslinking age...

Embodiment 2

[0269] Nanoscale CD-MOF was prepared as in Example 1.

[0270] Preparation of nano-scale COF: Weigh 778.3mg of nano-scale CD-MOF powder into a round bottom flask, fix it on a magnetic stirrer, add 10mL of acetonitrile, heat at 40°C, and add 194.6mg of crosslinking agent N,N under the condition of stirring at 200rpm '-Carbonyldiimidazole (the molar ratio of CD-MOF and cross-linking agent is 1:2) and 450 μL catalyst pyridine, reacted for 48 hours, and the rest were the same as in Example 1. The obtained COF was in the shape of a regular cube, with a particle size of 100-300 nm .

[0271] Preparation of nanoscale RGD-COF: Weigh 230mg nanoscale COF and 14mg linear RGD (the molar ratio of COF and RGD is 1:2) into a round bottom flask, add 5mL acetonitrile, stir well and then add 5mg N,N' - Succinimidyl carbonate and 6mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, placed on a magnetic stirrer at 20°C, stirred at 200rpm for 48h, and the rest were implemented in the ...

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Abstract

The invention provides a cubic cyclodextrin framework-RGD composition (RGD-COF) and a preparation method thereof. Specifically, the cyclodextrin framework-RGD composition of the present invention contains a cyclodextrin framework (COF) having a cubic structure and RGD. The cubic cyclodextrin framework-RGD composition disclosed by the invention can avoid phagocytosis and elimination of macrophages,enhance the mobility and the adhesion to damaged blood vessels and efficiently target and gather at activated blood platelets at the damaged blood vessel parts, and has great application prospects ontargeted diagnosis and treatment of vascular related diseases such as out-of-control hemorrhage, atherosclerosis and cerebral apoplexy. The invention provides a nanoscale cubic cyclodextrin framework-RGD composition which can be used for intravenous injection or a micron-scale cubic cyclodextrin framework-RGD composition which can be used for local external application by utilizing the advantagethat the size of a cyclodextrin-metal organic framework (CD-MOF) is controllable.

Description

technical field [0001] The invention relates to the field of biomaterials, and more specifically relates to a cubic cyclodextrin skeleton-RGD composition and a preparation method thereof. Background technique [0002] The morbidity and mortality of vascular-related diseases such as myocardial infarction and stroke are high worldwide. Non-targeting agents such as urokinase and other thrombolytic drugs have problems such as bleeding side effects and excessive systemic exposure. Due to the complex hemodynamics of the blood circulatory system and the rapid clearance of general carriers, targeted delivery of therapeutic drugs or imaging agents to vascular injury sites still faces great challenges. The physicochemical properties of the carrier, such as shape, can affect the in vivo fate and biological function of nanocarriers. Recent studies have shown that non-spherical drug carriers can evade the body's clearance mechanism, prolong the circulation time, and increase the adhesi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/16C08G81/00C08J3/24A61K31/616A61K31/4365A61K31/4709A61K31/5377A61K31/4174A61K31/4465A61K31/195A61K31/122A61K31/635A61K31/546A61K31/5383A61P7/02A61P31/04A61P7/04A61K47/40A61K45/00C08L5/16
CPCC08B37/0012C08G81/00C08J3/24A61K31/616A61K31/4365A61K31/4709A61K31/5377A61K31/4174A61K31/4465A61K31/195A61K31/122A61K31/635A61K31/546A61K31/5383A61P7/02A61P31/04A61P7/04A61K47/40A61K45/00C08J2305/16C08G83/001C08B37/0015A61K9/0019A61K9/5123A61K9/1617A61K33/38A61K31/197A61K31/43C08L5/16A61K47/64A61K31/724A61K45/06C08B30/18
Inventor 张继稳何亚平苏勇徐建伍丽孙娴
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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