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Mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles and preparation method

A nanoparticle and adhesion-type technology, applied in the field of pharmaceutical preparations, can solve problems such as weak adhesion and difficulty in improving drug transport efficiency, achieve high encapsulation efficiency, improve drug release and transport efficiency, and reduce the frequency of administration.

Active Publication Date: 2018-08-17
NANJING GENERAL HOSPITAL NANJING MILLITARY COMMAND P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there has always been a problem of how to release nanomedicine from the chyme during oral administration (2,4,5). Due to its small particle size and relatively weak adhesion, nanomedicine is difficult to effectively adhere to the intestinal mucosa Surface, so it is difficult for nanoparticle drug delivery system to improve drug delivery efficiency(6)

Method used

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  • Mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles and preparation method
  • Mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles and preparation method
  • Mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Weigh 12.5 mg of 5-aminosalicylic acid and dissolve it in 0.2 mL of 50 mg / ml PEG2000 aqueous solution as the inner water phase; weigh 40 mg of PEG-PLGA and dissolve it ultrasonically in 2 mL of dichloromethane / acetone mixed solvent with a volume ratio of 1:1 as Oil phase: under stirring at 10000r / min, the inner water phase is added dropwise to the oil phase to form colostrum, and then the colostrum is added dropwise to 20mL of 0.5% PVA aqueous solution (outer water phase) to form double emulsion. Then add 60 mL of 0.1% PVA aqueous solution (dispersed phase), put it into a dialysis bag (molecular weight cut off: 14000) and dialyze for 8 hours, then take out and freeze-dry to obtain PEG-PLGA nanoparticles. Put the nanoparticles into 2% sodium alginate aqueous solution, the volume ratio of the two is 1-5, use a 30G needle, and at a voltage of 15KV, slowly electrospray at a speed of 50ul / min, and the collection solution is 0.5uM calcium chloride and 0.5% (w / v) polylysine mi...

Embodiment 2

[0029] The present invention carries out experimental verification in the enteritis model induced by DSS, sets up normal control group, DSS (3,3'-dimethoxybenzidine hydrochloride) control group, 5-aminosalicylic acid traditional medicine treatment group, 5 -Aminosalicylic acid microsphere nanoparticle (prepared in Example 1) administration group was administered according to an effective drug dose of 50 mg / Kg, and a comparative drug effect experiment was carried out.

[0030] DSS modeling method: 6 C57 mice, all male. About 8-10 weeks, body weight is about 25-30g. Experimental reagent: dextran sodium sulfate (DSS) (MW=40000), prepared as a 2.5% concentration solution. The mice were randomly divided into 4 groups, 6 in each group, and the mice were fed normally for 5 days. After 5 days, the normal control group continued to be fed normally, but the DSS control group, the traditional drug treatment group and the microsphere nanoparticle group were respectively fed with 10ml of ...

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Abstract

The invention discloses mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles and a preparation method. The preparation method includes: adopting an emulsifying method to prepare a medicine-containing nanoparticle emulsion as a core; adopting an electrostatic spraying method to prepare the nanoparticle emulsion into microspheres to obtain the mucous membrane adhering microsphere carrying mucous membrane penetrating nanoparticles. Mucous membrane adhering medicine and mucous membrane penetrating medicine are combined to prepare microspheres effectively adheredon the surface of a mucous membrane, and the mucous membrane penetrating nanoparticles are slowly released in the process of degrading the microspheres, so that the problem that the mucous membrane adhering medicine is low in administration efficiency and the problem that the mucous membrane penetrating medicine is difficult to break away from chime are solved, and administration efficiency is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a mucosa-penetrating nanoparticle carried by a mucoadhesive microsphere and a preparation method thereof. Background technique [0002] Enteral drug delivery has always been a hot topic of concern. In the classification of intestinal drugs, intestinal drugs can be divided into mucosa-adhesive drugs and mucosa-penetrating drugs. Both types of drugs have their own advantages and disadvantages. Mucoadhesive drugs, such as sodium alginate, carboxymethylcellulose, etc., can be released from the chyme, effectively bind to the intestinal mucosa, and release the drug locally (1). After the drug is released, it is absorbed by the intestinal epithelial cells through the diffusion effect, but the mucus on the surface of the intestinal mucosa is always in a state of self-renewal, making the method of mucosal drug delivery less efficient (2). With the gradual maturity of nanotechnol...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/36A61K47/34A61K31/606A61K9/51A61P1/00A61P29/00
CPCA61K9/5031A61K9/5036A61K9/5073A61K9/5146A61K31/606A61P1/00A61P29/00
Inventor 任建安赵成吴秀文陈国璞黄金健王革非
Owner NANJING GENERAL HOSPITAL NANJING MILLITARY COMMAND P L A
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