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Lubricating drug-carrying nanospheres, drug and preparation method thereof

A drug-loaded nano-drug technology, applied in the field of lubrication, can solve the problems of loss of lubrication function, thinning, etc.

Active Publication Date: 2021-10-22
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at shear rates typical of sliding articular cartilage surfaces, HA has approximately the same viscosity as water and exhibits shear thinning, thereby losing its lubricating function

Method used

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  • Lubricating drug-carrying nanospheres, drug and preparation method thereof
  • Lubricating drug-carrying nanospheres, drug and preparation method thereof
  • Lubricating drug-carrying nanospheres, drug and preparation method thereof

Examples

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preparation example Construction

[0054] The present application also provides a method for preparing lubricated drug-loaded nanospheres, comprising the following steps:

[0055] a, reacting hyaluronic acid, initiator, catalyst, cystamine dihydrochloride, and aminated β-cyclodextrin in water to obtain thiolated and grafted hyaluronic acid with β-cyclodextrin;

[0056] b, reducing the product of step a and precipitating under acidic conditions to obtain a solid component;

[0057] c. Mix the solid component obtained in step b with tetrabutylammonium hydroxide in water, and dialyze to obtain the solid component;

[0058] d. Dissolving the solid component obtained in step c with 2-methacryloyloxyethyl phosphorylcholine in an organic solvent for reaction, and dialyzing to obtain the solid component.

[0059] The preparation method of this embodiment has simple steps and mild conditions. Compared with other methods, the obtained material has good biocompatibility and lubricity. The preparation is realized by amid...

Embodiment

[0079] (1) Add hyaluronic acid, initiator EDC, catalyst HOBT, cystamine dihydrochloride, and aminated β-cyclodextrin into deionized water, stir at room temperature for 16 hours, and add dithiothreitol to the obtained solution after dialysis , after stirring overnight, adjust the pH to 3.5 by ethanol precipitation and freeze-drying.

[0080] (2) The product of step (1) was dissolved in deionized water, added dropwise into tetrabutylammonium hydroxide solution, stirred at room temperature, dialyzed and freeze-dried.

[0081](3) The product of step (2) was dissolved in dimethyl sulfoxide, added MPC, and reacted for 6 hours under nitrogen protection. The solution was precipitated in acetone, dissolved in deionized water, dialyzed, and then lyophilized and stored.

[0082] (4) The product of step (3) and the drug honokiol were dissolved in dimethyl sulfoxide, added dropwise to deionized water to promote thiol cross-linking, stirred for 24 hours, lyophilized and stored after dialysi...

experiment example 2

[0089] Experimental example 2 drug release

[0090] Carry out drug release test according to conventional method to the lubricated drug particle prepared by embodiment, the result is as follows: figure 2 shown. The results show that the lubricated drug-loaded nanospheres of the present application have the drug-loading ability to honokiol.

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Abstract

The application discloses a lubricating drug-loaded nanosphere, which comprises repeating units formed by copolymerization of hyaluronic acid, β-cyclodextrin and 2-methacryloyloxyethyl phosphorylcholine. The present application also discloses a lubricating drug, which comprises lubricating drug-loaded nanospheres and hydrophobic drugs, and the hydrophobic drug is loaded in the hydrophobic cavity of β-cyclodextrin in the lubricating drug-loaded nanospheres. The present application also discloses a preparation method of lubricating drug-loaded nanospheres, comprising the following steps: a, reacting hyaluronic acid, initiator, catalyst, cystamine dihydrochloride, and aminated β-cyclodextrin in water; b , the product of a is reduced and precipitated under acidic conditions; c, the solid component of b is mixed with tetrabutylammonium hydroxide in water, and dialyzed; d, the solid component of c is mixed with 2-methacryloyloxyethyl phosphoric acid Choline is dissolved in an organic solvent and dialyzed to obtain a solid component. The application also discloses a preparation method of lubricating medicine.

Description

technical field [0001] The invention relates to the technical field of lubrication, in particular to a lubricating drug-loaded nanosphere, a drug and a preparation method thereof. Background technique [0002] The chemical essence of hyaluronic acid (HA) is glycosaminoglycan, which is N-acetylglucosamine and D-glucuronide connected alternately by (1->3) and (1->4) glycosidic bonds A linear natural polysaccharide composed of acid. Hyaluronic acid widely exists in various tissues of animals and humans, and is the main component of synovial fluid and articular cartilage. Clinically, HA is commonly used as a mucus supplement for intra-articular injection to relieve osteoarthritis by increasing the viscosity of joint synovial fluid. However, at the typical shear rates of sliding articular cartilage surfaces, HA has a viscosity approximately the same as that of water, exhibiting shear thinning, thereby losing its lubricating function. Therefore, we tried to find a way to ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K45/00A61K31/05A61P19/02B82Y5/00B82Y40/00C08F287/00C08F230/02
CPCA61K31/05A61K45/00A61K47/6951A61P19/02B82Y5/00B82Y40/00C08F287/00C08F230/02
Inventor 张洪玉郑意为
Owner TSINGHUA UNIV
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