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A pulmonary inhaled chitosan-based nano targeting polymer particles and its production method thereof

A technology of chitosan nanoparticles and chitosan, which is applied in the medical basic application field of biological materials, can solve the problems of easy to cause toxic reactions, poor biocompatibility, low cell phagocytosis rate, etc., and achieves increased bioavailability, biological Good compatibility and uniform particle size distribution

Active Publication Date: 2017-01-04
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The specificity of pulmonary inhalation administration, together with the small aerodynamic diameter of chitosan nanoparticles, will lead to less deposition of nanoparticles in the lungs with exhalation, and low bioavailability and non-targeting of other carriers. At the same time, due to the difficulty of powdering nanoparticles, the application in the lung powder aerosol drug delivery system is limited; the biocompatibility is poor, and the rate of phagocytosis by cells is low; it is easy to cause toxic reactions

Method used

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  • A pulmonary inhaled chitosan-based nano targeting polymer particles and its production method thereof
  • A pulmonary inhaled chitosan-based nano targeting polymer particles and its production method thereof
  • A pulmonary inhaled chitosan-based nano targeting polymer particles and its production method thereof

Examples

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Embodiment 1

[0068] Embodiment 1 A kind of chitosan-based targeted nanopolymer particles for lung inhalation

[0069] The nanopolymer particles include chitosan, sodium tripolyphosphate, cetuximab, lecithin, hydroxypropyl β-cyclodextrin and excipients;

[0070] Described chitosan, molecular weight is 1120Kda; Deacetylation degree 96%, powder form;

[0071] The phospholipid is lecithin;

[0072] The excipient is lactose;

[0073] The mass ratio of chitosan, sodium tripolyphosphate, cetuximab, lecithin, hydroxypropyl beta-cyclodextrin and lactose is 5:1:0.01:2:1:5;

[0074] The preparation method of the lung inhalation chitosan-based targeting nano-polymer particles comprises the following steps:

[0075] (1) Preparation of chitosan solution

[0076] Weigh 500 mg of chitosan, dissolve it in 250 mL of 1% acetic acid solution, and prepare a 2 mg / mL chitosan solution.

[0077] (2) Preparation of sodium tripolyphosphate solution

[0078] Weigh 100 mg of sodium tripolyphosphate, dissolve so...

Embodiment 2

[0096] Embodiment 2 A kind of chitosan-based targeting nanopolymer particles for lung inhalation

[0097] The nanopolymer particles include chitosan derivatives, sodium tripolyphosphate, cetuximab, phospholipid derivatives, hydroxypropyl β-cyclodextrin and excipients;

[0098] Described chitosan derivative, molecular weight is 1250Kda, and degree of substitution is carboxymethyl chitosan of 86%, powder form;

[0099] The phospholipid derivative is dipalmitoylphosphatidylcholine DPPC

[0100] The excipient is mannitol;

[0101] The carboxymethyl chitosan, sodium tripolyphosphate, cetuximab, DPPC, hydroxypropyl β-cyclodextrin, and mannitol mass ratio are 4:2:0.02:3:3:1;

[0102] The preparation method of the lung inhalation chitosan-based targeted nanopolymer particle comprises the following steps:

[0103] (1) Preparation of chitosan solution

[0104] Weigh 400 mg of carboxymethyl chitosan, and dissolve carboxymethyl chitosan powder with a deacetylation degree of 96% in 200...

Embodiment 3

[0122] Example 3 A kind of chitosan-based targeted nanopolymer particle for lung inhalation

[0123] The nanopolymer particles include chitosan derivatives, sodium tripolyphosphate, cetuximab, phospholipid derivatives, hydroxypropyl β-cyclodextrin and excipients;

[0124] Described chitosan derivative, molecular weight is that 1000Kda degree of substitution is the chitosan quaternary ammonium salt of 90%, powder form;

[0125] The phospholipid derivative is 1,2-palmitoylphosphatidylglycerol sodium salt DPPG

[0126] The excipient is trehalose;

[0127] The chitosan quaternary ammonium salt, sodium tripolyphosphate, cetuximab, DPPG, hydroxypropyl β-cyclodextrin, and trehalose have a mass ratio of 3:2:0.01:1:3:5;

[0128] The preparation method of the lung inhalation chitosan-based targeted nanopolymer particle comprises the following steps:

[0129] (1) Preparation of chitosan solution

[0130] Weighed 300 mg of chitosan quaternary ammonium salt, and dissolved chitosan powd...

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Abstract

This invention provides a pulmonary inhaled chitosan-based nano targeting polymer particle which consists chitosan or 1-5 parts of its derivatives; 1-5 parts of sodium tripolyphosphate; 0.01-0.03 parts of cetuximab, phospholipid or 1-3 parts of its derivatives, 1-5 parts of hydroxypropyl-Beta-cyclodextrin and 1-6 parts of excipient. This invention also provides the preparation method of the polymer particle. The particle diameter of this pulmonary inhaled chitosan-based nano targeting polymer particle prepared in this invention is 2-10Mum with uniform distribution. The loaded particle diameter of this pulmonary inhaled chitosan-based nano targeting polymer particle is 50-201nm with good biocompatibility. The particle prepared in this invention improves the stability and the ability for cell phagocytosis. The phagocytic rate of A549 cell reaches 50-60% in 2hours which means an increase of bioavailability. This particle is easy to deposit at lung and resolve at a short time which helps particles work in lung with retention rate of 50-70%.

Description

technical field [0001] The invention relates to a carrier, in particular to a chitosan-based nano targeted polymer particle for lung inhalation and a preparation method thereof, which belongs to the medical basic application field of biological materials. Background technique [0002] Nano-preparation is a new type of drug delivery system developed in recent years. It is prepared from natural or synthetic polymer carrier materials and has solid particles with a particle size of 1 to 1000 nm. Due to its small particle size and large surface energy, it is beneficial to attach to the mucous membrane and other parts and is easier to be phagocytized by cells, and it can be targeted and modified so that it can be actively targeted to the target organ, increasing the high accumulation in the cell . It can also improve the solubility and bioavailability of drugs, and change the efficiency of drug delivery. [0003] Cetuximab is a monoclonal antibody to the EGF receptor. Many studi...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K39/395A61K9/16A61K9/51A61K47/36A61K47/24A61K47/40A61P35/00
CPCA61K9/0073A61K9/1617A61K9/1652A61K9/5161A61K39/395
Inventor 张维芬刘康唐金宝郑增娟
Owner WEIFANG MEDICAL UNIV
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