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Nano preparation for pulmonary fibrosis and preparation method thereof

A nano-preparation and pulmonary fibrosis technology, applied in the field of medicine, can solve the problem of weakening the therapeutic effect of drugs on diseases, achieve efficient lung delivery and prolong circulation time

Active Publication Date: 2019-10-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In patients with advanced obstructive pulmonary disease and fibrosis, mucus secreted by airway goblet cells acts as part of a clearance system that traps drugs reaching the airways through steric hindrance or adhesion and subsequently clears them from the mucus , leading to a decrease in the drug reaching the deep lungs, resulting in weakened therapeutic effect of the drug on the disease

Method used

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  • Nano preparation for pulmonary fibrosis and preparation method thereof
  • Nano preparation for pulmonary fibrosis and preparation method thereof
  • Nano preparation for pulmonary fibrosis and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1 Synthesis and preparation of nano-preparation components, such as figure 1 , figure 2 Shown:

[0059] 1. Preparation of double-drug / single-drug PLGA-PEG-MAL nanoparticles

[0060] In the present invention, the film dispersion method is preferably used to prepare the PLGA-PEG-MAL nanoparticles loaded with anti-pulmonary fibrosis drug Z. The specific preparation method is as follows:

[0061] Weigh 100 mg PLGA-PEG-MAL and 10 mg anti-pulmonary fibrosis drug Z, respectively, and dissolve them in 2 mL ethyl acetate solution, and ultrasonically dissolve. Under stirring conditions, the ethyl acetate solution was spin-dried by a rotary evaporator, then 3 mL of distilled water was added for ultrasonic dissolution for 30 min, and the unencapsulated free drug was removed by centrifugation at 2500 rpm / min for 20 min. Nanoparticles were concentrated to a volume of 500 μL using ultrafiltration tubes with a molecular weight of 10,000.

[0062] Antioxidant anti-fibro...

Embodiment 2

[0109] Example 2 Papain can specifically degrade papain

[0110] According to Example 1, papain, an analog of mucin in the mucus layer, was taken as the research object, and different concentrations of protease were added to act for 24 hours, and the morphological changes of papain under the transmission electron microscope were photographed by transmission electron microscopy (TEM). The results of transmission electron microscopy showed that papain could be degraded by mucin after interacting with mucin for 24 h, such as Figure 5 , Figure 6 shown.

Embodiment 3

[0111] Example 3 Determination of Responsive Release of Nano-Preparations under Slightly Acid and Enzyme Sensitive Conditions

[0112] Prepare PP / (pirfenidone), PPZ / (containing protease X and pirfenidone), PPV / (containing protease X and Fe 3+ mediated complex) and PPZV / (contains pirfenidone, protease X and Fe 3+ mediated complexes) nanoformulations. After the nano-preparation was concentrated to 200 μL, 1 mL of PBS with pH 6.8 was added, and then placed at 4 ºC for 24 h, the particle size and potential of the nanoparticles in different environments were characterized by a particle size analyzer.

[0113] (1) After measuring the particle size with the Malvern Panalytical Visible Particle Size Analyzer, the particle size is inspected again after the action of micro-acid and enzyme, and the particle size change is observed;

[0114] The particle size data that the present embodiment measures is as Figure 7 , Figure 8 and Figure 9 As shown, the particle size change of nano...

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Abstract

The invention discloses a nano preparation for pulmonary fibrosis and a preparation method thereof, namely a nano preparation modified with protease with mucin degradation and a carrier of the nano preparation. The preparation method comprises the steps that firstly, the nano preparation is responsively released by virtue of the property of mucin degradation of the protease, and then therapeutic drugs are efficiently delivered to a pulmonary fibrosis injury part, so that efficient targeted delivery of anti-pulmonary fibrosis drugs is realized, and the purpose of efficiently treating the pulmonary fibrosis is achieved. Aiming at the problem that deep delivery difficulty generally exists in currently marketed tracheal and inhaled administration dosage forms, that is, a large number of drugsare difficult to deliver to the deep alveoli to come into play due to excessive secretion of mucus by goblet cells in a trachea, the change of the excessive secretion of the mucus in a pulmonary fibrosis trachea microenvironment is adopted, and the nano preparation which is responsively released and can efficiently pass through a trachea barrier is constructed, so that the therapeutic drugs are efficiently delivered to the pulmonary fibrotic injury part in the deep alveoli, and the efficiency of the nano preparation reaching the deep alveoli is improved.

Description

technical field [0001] The invention discloses a nano-preparation for pulmonary fibrosis and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Idiopathic pulmonary fibrosis (IPF) is one of the severe and common forms of interstitial lung disease (ILD). ILD is a progressive lung disease that can lead to pulmonary fibrosis at an advanced stage. During the development of the disease, the damaged alveolar epithelial cells will secrete a large amount of inflammatory factors, thereby activating the excessive proliferation of fibroblasts and transforming into myofibroblasts at the same time, resulting in excessive deposition of extracellular matrix (ECM), and damage to the lung parenchyma. Destruction, eventually leading to the death of the patient due to respiratory failure. Although the new anti-fibrotic drug pirfenidone (PFD) has been approved for clinical treatment in Europe and other countries, there are still some prob...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/42A61K47/34A61K45/06A61K31/155A61K31/4418A61P11/00A61P29/00
CPCA61K9/5146A61K9/5169A61K31/155A61K31/4418A61K45/06A61P11/00A61P29/00A61K2300/00
Inventor 姜虎林常鑫邢磊林伊君李玲
Owner CHINA PHARM UNIV