Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of PDGF monoclonal antibody pirfenidone nanostructure lipid carrier and preparation method thereof

A nanostructured lipid and pirfenidone technology is applied in the research field of new drug delivery systems, which can solve problems such as short half-life, and achieve the effects of reducing distribution, efficient targeted therapy, and improving drug treatment efficiency.

Active Publication Date: 2021-06-04
NINGBO UNIV
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug is accompanied by more side effects during use, such as gastrointestinal reactions (nausea, vomiting, indigestion, diarrhea), fatigue and photosensitivity rash, etc., and because the half-life is very short, in order to maintain the effective concentration in the body, high doses And high-frequency medication has become a mandatory dosing regimen, and its side effects can only be alleviated by reducing the dose or stopping treatment

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of PDGF monoclonal antibody pirfenidone nanostructure lipid carrier and preparation method thereof
  • A kind of PDGF monoclonal antibody pirfenidone nanostructure lipid carrier and preparation method thereof
  • A kind of PDGF monoclonal antibody pirfenidone nanostructure lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] On the other hand, the invention provides a method for preparing PDGF monoclonal antibody pirfenidone nanostructured lipid carrier, the steps are as follows:

[0030] 1) Accurately weigh 5%-15% pirfenidone, 84%-94% lipid material, 0%-10% polyethylene glycol monostearate (molecular weight: 2000) and 1% monoamino-terminated polyethylene glycol stearate, a total of 100 mg of the above materials, mixed to obtain material A;

[0031] 2) Add 1mL of ethanol to material A in step 1), and heat it in a water bath at 60°C to completely dissolve to obtain material B; absorb 0.45mL of material B with a syringe, dilute it to 0.5mL with ethanol, and obtain material C;

[0032]3) Using deionized water as the dispersion medium, inject 0.5mL of material C into 9.5mL of deionized water heated in a 60°C water bath at a stirring speed of 400rpm, take it out after the injection is completed and stir for 30s, and naturally cool to room temperature to obtain a lipid concentration of 9mg / mL pi...

Embodiment 1

[0042] 1. Synthesis of monoamino-terminated polyethylene glycol stearate

[0043] Weigh 119.8mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 24.0mg N-hydroxysuccinimide, 35.5mg stearic acid dissolved in 3mL anhydrous dimethyl base sulfoxide, 400rpm at 60°C for 30min, the reaction solution was slowly added dropwise to 250mg of diamino-terminated polyethylene glycol solution dissolved in 2mL of anhydrous DMSO, and stirred at room temperature for 24h at 400rpm. After the reaction, the reaction solution was transferred to a dialysis bag (molecular weight cut-off: 7kDa), dialyzed with pure water for 48 hours to remove water-soluble by-products, and freeze-dried to obtain monoamino-terminated polyethylene glycol stearate.

[0044] 2. Preparation of pirfenidone nanostructured lipid carrier modified by PDGF monoclonal antibody

[0045] Solvent diffusion method is used to prepare pirfenidone nanostructured lipid carrier. The specific method is: accurately weigh 5 mg pi...

Embodiment 2

[0052] 1. Synthesis of monoamino-terminated polyethylene glycol stearate

[0053] Weigh 119.8mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride, 24.0mg N-hydroxysuccinimide, 35.5mg stearic acid dissolved in 3mL anhydrous dimethyl base sulfoxide, 400rpm at 60°C for 30min, the reaction solution was slowly added dropwise to 250mg of diamino-terminated polyethylene glycol solution dissolved in 2mL of anhydrous DMSO, and stirred at room temperature for 24h at 400rpm. After the reaction, the reaction solution was transferred to a dialysis bag (molecular weight cut-off: 7kDa), dialyzed with pure water for 48 hours to remove water-soluble by-products, and freeze-dried to obtain monoamino-terminated polyethylene glycol stearate.

[0054] 2. Preparation of pirfenidone nanostructured lipid carrier modified by PDGF monoclonal antibody

[0055] Solvent diffusion method to prepare pirfenidone nanostructured lipid carrier, specific method: accurately weigh 10mg pirfenidone, 89mg...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a PDGF monoclonal antibody pirfenidone nanostructure lipid carrier and a preparation method thereof. The PDGF monoclonal antibody pirfenidone nanostructured lipid carrier includes pirfenidone nanostructured lipid carrier, N,N'-disuccinimidyl carbonate and PDGF monoclonal antibody; the pirfenidone nanostructured Structural lipid carrier consists of 5-15 parts by mass of pirfenidone, 84-94 parts by mass of lipid material, 0-10 parts by mass of polyethylene glycol monostearate, 1 part by mass of monoamino-terminated Made of polyethylene glycol stearate; the N,N'-disuccinimidyl carbonate is monoclonal by combining the amino group of the monoamino-terminated polyethylene glycol stearate on the carrier with the PDGF monoclonal The amino groups on the antibody are linked to allow the antibody to be grafted onto the carrier. The PDGF monoclonal antibody pirfenidone nanostructured lipid carrier provided by the present invention can target activated hepatic stellate cells, improve the distribution of drugs in the lesion, and start from the targeted intervention of activated hepatic stellate cells to explore a A new approach for safe and efficient targeted therapy of liver fibrosis.

Description

technical field [0001] The invention belongs to the research field of new drug delivery systems, and in particular relates to a PDGF monoclonal antibody pirfenidone nanostructured lipid carrier and a preparation method thereof. Background technique [0002] Hepatic fibrosis is a compensatory response in the tissue repair process secondary to various forms of chronic liver injury, and is also a common pathological process of all chronic liver diseases. Its terminal stage will develop into cirrhosis, portal hypertension, liver failure and liver failure. cell carcinoma. The essence of liver fibrosis is the excessive deposition of extracellular matrix (ECM) mainly composed of collagen types I and IV, which damages the normal structure and function of the liver. In recent years, the morbidity and mortality of hepatic fibrosis have been increasing, seriously endangering human health. Therefore, effective prevention and treatment of liver fibrosis is a major medical problem to be...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/68A61K31/4418A61P1/16
CPCA61K9/1271A61K9/1277A61K31/4418A61K47/68A61P1/16
Inventor 胡静波王金辉谭学莹赵玉芬
Owner NINGBO UNIV