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A nanoemulsion drug carrier and its preparation method and application

A nanoemulsion, nanoemulsion technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of short residence time and reduce the bioavailability of tacrolimus, and achieve good biocompatibility and increase solubility. Effect

Active Publication Date: 2021-02-19
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, nasolacrimal drainage, lacrimal irrigation, and short residence time of topical solutions reduce the bioavailability of tacrolimus

Method used

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  • A nanoemulsion drug carrier and its preparation method and application
  • A nanoemulsion drug carrier and its preparation method and application
  • A nanoemulsion drug carrier and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] (1) Preparation of β-cyclodextrin maleic acid monoester: Dissolve 11.34g β-cyclodextrin and 9.8g maleic anhydride in 50ml N,N-dimethylformamide at room temperature , heated to 60°C to react for 8 hours, precipitated with dichloromethane and washed with acetone, collected the product by suction filtration, and dried to obtain β-cyclodextrin maleic acid monoester.

[0071] (2) Preparation of β-cyclodextrin maleic acid monoester connected with chitosan quaternary ammonium salt: β-cyclodextrin maleic acid monoester obtained by dissolving 4g of step (1) in 50ml water, adding The cross-linking agent 1g NHS and 1g EDC were activated for 2h; 3g of chitosan quaternary ammonium salt was dissolved in 50ml of water, added to the above solution under magnetic stirring, reacted at room temperature for 12h, dialyzed 3 times, each time for 12h, freeze-dried, The product is collected to obtain the quaternary ammonium salt of β-cyclodextrin maleic acid monoester connected with chitosan. ...

Embodiment 2

[0075] (1) Preparation of β-cyclodextrin maleic acid monoester: Dissolve 11.34g β-cyclodextrin and 19.6g maleic anhydride in 100ml N,N-dimethylformamide at room temperature , heated to 90°C to react for 12 hours, precipitated with dichloromethane and washed with acetone, collected the product by suction filtration, and dried to obtain β-cyclodextrin maleic acid monoester.

[0076] (2) Preparation of β-cyclodextrin maleic acid monoester connected chitosan quaternary ammonium salt: dissolve 2g of β-cyclodextrin maleic acid monoester obtained in 50ml of water in step (1), add Cross-linking agent 0.5g NHS and 1.5g EDC activation 3h; Dissolve 1.5g chitosan quaternary ammonium salt in 25ml water, add to the above solution under magnetic stirring, react at room temperature for 36h, dialyze 3 times, each 24h, Freeze-dry and collect the product to obtain the quaternary ammonium salt of β-cyclodextrin maleic butene monoester and chitosan.

[0077] (3) Preparation of tacrolimus inclusio...

Embodiment 3

[0080] (1) Preparation of β-cyclodextrin maleic acid monoester: at room temperature, 11.34g β-cyclodextrin and 14.4g maleic anhydride were stirred in 75ml pyridine and heated to 75°C for reaction After 10 hours, precipitate with dichloromethane and wash with acetone, collect the product by suction filtration, and dry to obtain β-cyclodextrin maleic acid monoester.

[0081] (2) Preparation of β-cyclodextrin maleic acid monoester connected chitosan quaternary ammonium salt: dissolve 4g of β-cyclodextrin maleic acid monoester obtained in 50ml of water in step (1), add cross-linking 1g NHS and 1.5g EDC were activated for 2.5h; 3g chitosan quaternary ammonium salt was dissolved in 100ml water, added to the above solution under magnetic stirring, reacted at room temperature for 24h, dialyzed 3 times, each time for 18h, freeze-dried, The product is collected to obtain the quaternary ammonium salt of β-cyclodextrin maleic butene monoester and chitosan.

[0082] (3) Preparation of tac...

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Abstract

The invention discloses a nanoemulsion drug carrier, a preparation method and application thereof. In the present invention, β-cyclodextrin has the ability to increase the water solubility of hydrophobic drugs, and grafts it onto the bioadhesive chitosan quaternary ammonium salt to load tacrolimus or other hydrophobic drugs. Using the principle of polycation and polyanion to form a polyelectrolyte complex through electrostatic interaction, the drug-loaded β-cyclodextrin-chitosan quaternary ammonium salt is combined with carboxymethylcellulose sodium solution to obtain the target pharmaceutical preparation; If loading of tacrolimus or other hydrophobic drug is omitted, the result is a nanoemulsion drug carrier. The nanoemulsion drug carrier of the present invention has good biocompatibility after being loaded with drugs, realizes double sustained release, and can achieve long-acting treatment effects. The obtained emulsion preparation has good stability, uniform particle size, safety and non-toxicity, and has a wide range of applications. Applications.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymers, and in particular relates to a nanoemulsion drug carrier and its preparation method and application. Background technique [0002] Dry eye syndrome is a multifactorial disorder of the tear fluid and ocular surface, manifested by ocular discomfort, visual disturbance, and tear film instability, with potential damage to the ocular surface, often associated with ocular surface inflammation. Seemingly a minor problem, dry eye affects people's quality of life and is already a growing public health problem, driving millions to seek eye care. Its pathogenesis is very complicated, and various inducements can affect the normal function of the lacrimal gland in different ways. The reduction of tears makes the ocular surface in a relatively dry environment, resulting in excessive stimulation of the ocular surface nerves, and at the same time activates the autoimmune mechanism, causing eye diseas...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/69A61K47/36A61K47/38A61K31/436A61P27/02
CPCA61K9/0048A61K9/1075A61K31/436A61K47/36A61K47/38A61K47/6951A61P27/02
Inventor 蒋刚彪胡汉剑袁进胡甜李伟雄钟菁
Owner SOUTH CHINA AGRI UNIV
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