Preparation method and application of oral microsphere carrying small molecular nucleic acid drug

A molecular nucleic acid and nucleic acid drug technology, which can be applied to medical preparations with non-active ingredients, non-active ingredients of polymer compounds, and medical preparations containing active ingredients, etc. It can solve the problems of complex preparation, low drug loading rate and treatment efficiency To solve the problem, to achieve the effect of simple method, optimization of size and structure characteristics, and alleviation of inflammatory diseases

Pending Publication Date: 2021-01-22
NANJING DRUM TOWER HOSPITAL
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The present invention provides a preparation method and application of oral small molecule nucleic acid drug microspheres to overc

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  • Preparation method and application of oral microsphere carrying small molecular nucleic acid drug
  • Preparation method and application of oral microsphere carrying small molecular nucleic acid drug
  • Preparation method and application of oral microsphere carrying small molecular nucleic acid drug

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Example Embodiment

[0031]Example 1

[0032]This embodiment provides an oral preparation method of small molecule nucleic acid drug microspheres, specifically the preparation method of GelMA microspheres orally loaded cKGM&TNF-αASO nano nucleic acid, the preparation process is as followsfigure 1 As shown, including the following steps:

[0033]Step 1. Preparation of cKGM&TNF-αASO composite nano medicine:

[0034]Weigh KGM in DMSO, heat and dissolve at 60°C, cool to room temperature, add excess CDI, react at room temperature for 3 hours to fully activate, then add excess ethylenediamine, continue to stir to fully react, dialyze, freeze-dry and vacuum Get cKGM. Prepare a 10% w / v cKGM solution, add a small molecule nucleic acid drug solution, and stand for 0.5h to react to obtain a stable nano nucleic acid drug. The molar ratio of KGM to DMSO is 1:106, The mass ratio of KGM to CDI is 1:2, and the molar ratio of KGM to ethylenediamine is 1:105, The mass ratio of cKGM to TNF-αASO is 1:5.

[0035]Step 2: Preparation of ...

Example Embodiment

[0042]Example 2

[0043]This embodiment provides a preparation method of oral small molecule nucleic acid drug microspheres, specifically the preparation of GelMA microspheres loaded cKGM&TNF-αsiRNA nano nucleic acid, including the following steps:

[0044]Step 1. Preparation of cKGM&TNF-αsiRNA composite nanomedicine:

[0045]Weigh KGM in DMSO, heat and dissolve at 60°C, cool to room temperature, add excess CDI, react at room temperature for 3 hours to fully activate, then add excess ethylenediamine, continue to stir to fully react, dialyze, freeze-dry and vacuum Get cKGM. Prepare a 10% w / v cKGM solution, add a small molecule nucleic acid drug solution, and stand for 0.5h to react to obtain a stable nano nucleic acid drug. The molar ratio of KGM to DMSO is 1:106, The mass ratio of KGM to CDI is 1:2, and the molar ratio of KGM to ethylenediamine is 1:105, The mass ratio of cKGM to TNF-αsiRNA is 1:5.

[0046]Step 2. Preparation of GelMA microspheres carrying cKGM&TNF-αsiRNA:

[0047]Prepare 15% w / v ...

Example Embodiment

[0051]Example 3

[0052]This embodiment provides a method for preparing oral small molecule nucleic acid drug microspheres, specifically the preparation of methacrylate hyaluronic acid (HAMA) microspheres loaded cKGM&TNF-αASO nano nucleic acid, including the following steps:

[0053]Step 1. Preparation of cKGM&TNF-αASO composite nano medicine:

[0054]Weigh KGM in DMSO, heat and dissolve at 60°C, cool to room temperature, add excess CDI, react at room temperature for 3 hours to fully activate, then add excess ethylenediamine, continue to stir to fully react, dialyze, freeze-dry and vacuum Get cKGM. Prepare a 10% w / v cKGM solution, add a small molecule nucleic acid drug solution, and stand for 0.5h to react to obtain a stable nano nucleic acid drug. The molar ratio of KGM to DMSO is 1:106, The mass ratio of KGM to CDI is 1:2, and the molar ratio of KGM to ethylenediamine is 1:105, The mass ratio of cKGM to TNF-αASO is 1:5.

[0055]Step 2: Preparation of GelMA microspheres carrying cKGM&TNF-αASO:...

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Abstract

The invention discloses a preparation method and application of an oral microsphere carrying a small molecular nucleic acid drug. The preparation method comprises the following steps of: step 1, preparing a cationized konjac polysaccharide solution, and adding a small molecular nucleic acid drug solution to obtain a stable nano nucleic acid drug; step 2, preparing a biodegradable carrier solution,mixing the nano nucleic acid drug in the biodegradable carrier solution as an internal phase, generating liquid drops under the shearing action of an immiscible external phase fluid by adopting a microfluidic device, and polymerizing or curing to obtain the microsphere carrying the nano nucleic acid drug; and step 3, loading a preset amount of Eudragit colon-soluble aqueous dispersion coating liquid into coating equipment, and coating the microsphere carrying the nano nucleic acid drug by using the coating equipment to obtain the oral microsphere carrying the small molecular nucleic acid drug. The preparation method disclosed by the invention has the advantages of being flexible, low in cost, simple and easy to operate, safe and reliable, capable of effectively improving the bioavailability and targeting property of the small molecular nucleic acid drug, and the like.

Description

Technical field[0001]The invention belongs to the field of biological materials, and particularly relates to a preparation method and application of oral small molecule nucleic acid drug microspheres.Background technique[0002]Inflammatory bowel disease (IBD) is a chronic inflammatory disease of the gastrointestinal tract. Its recurrence rate is extremely high, which increases the risk of colon cancer and seriously affects the quality of life of patients after recovery. In the current clinical treatment, the oral method is one of the most acceptable treatment methods for most patients because of its unique advantages such as painlessness, simple operation, safety and autonomy. However, the efficacy of most oral drugs is often limited by the complicated digestive tract environment, leading to poor drug absorption and metabolism, which greatly affects the bioavailability of drugs. Monodisperse microcapsules are microcapsules formed by encapsulating pharmaceutical active molecules and b...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/10A61K47/36A61K47/42A61K47/14A61K47/38A61K47/34A61K47/26A61K47/32A61K47/44A61K31/713A61K31/7088A61K31/7084A61P1/00
CPCA61K9/5031A61K9/5026A61K47/36A61K47/42A61K47/14A61K47/38A61K47/34A61K47/26A61K47/32A61K47/44A61K31/713A61K31/7088A61K31/7084A61P1/00
Inventor 孙凌云甘璟璟赵远锦王月桐
Owner NANJING DRUM TOWER HOSPITAL
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