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Macromolecular drug delivery mechanism and delivery method thereof

A technology of macromolecules and biomacromolecules, which is applied to the brain delivery mechanism and field of biomacromolecular drugs, and can solve the problems of ineffective promotion of biomacromolecular drugs, limited popularization and application, and low concentration of drugs entering the brain.

Pending Publication Date: 2021-09-21
温州医科大学慈溪生物医药研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the olfactory pathway provides a feasible pathway for biomacromolecular drugs to enter the brain non-invasively, it is found in clinical practice that the application of this route of administration is limited by many factors, such as the skill of administration, drug molecular weight and concentration, etc., especially body position Therefore, the actual concentration of drugs entering the brain is very low, and long-term effects cannot be formed, thus limiting the popularization and application of biomacromolecular drugs entering the brain through the nasal olfactory pathway
In addition, the drug delivery device using the nasal olfactory pathway is likely to cause discomfort to the patient, especially sneezing, which leads to the inability to guarantee the dosage
[0006] At present, a delivery system for efficiently delivering drugs into the brain has not been seen, which overcomes the problem that the drug delivery system in the prior art cannot effectively promote the entry of biomacromolecular drugs into the brain to take effect, and realizes the efficient delivery of biomacromolecular drugs into the brain to play a role Purpose

Method used

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  • Macromolecular drug delivery mechanism and delivery method thereof
  • Macromolecular drug delivery mechanism and delivery method thereof
  • Macromolecular drug delivery mechanism and delivery method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation method of a macromolecular drug delivery mechanism

[0049] According to the settings of the experimental group in Table 1, using green fluorescent protein as a representative of biomacromolecular drugs, a 0.01% green fluorescent protein aqueous solution was prepared.

[0050] The preparation of the control group is carried out with reference to the experimental group, and the final concentration of the green fluorescent protein in the preparation of the control group is the same as that of the experimental group. In the control group, each experimental group of the nanoparticle preparation of green fluorescent protein, W / O emulsion and water macromolecular drug delivery mechanism is configured according to the components and ratios within the protection scope of the claims of the application, and each control group is a certain A technical feature is missing or the technical feature is beyond the protection scope of the claims of this application....

Embodiment 2

[0054] Example 2 Application effect of a macromolecular drug delivery mechanism

[0055] The second embodiment of the present invention uses the scheme of Example 1 to carry out animal experiments. Several guinea pigs are taken. After anesthesia, each group of ion-assisted microneedle patch systems is fixed on the upper lip or both sides of the nose of the animal face, and the settings are set according to Table 1. The experimental group and the control group were treated, and the same method was operated every other day, and the same method was administered for a total of 3 times (i.e., 1, 3, 5 days of administration). On the first day of execution, the skull was opened, the brain tissue was separated, and fluorescence imaging was performed to observe the green fluorescence intensity of the brain tissue. The fluorescence intensity was divided into 5 levels, and the delivery efficiency of green fluorescent protein into the brain was compared and analyzed between the experimenta...

Embodiment 3

[0062] Example 3 A delivery method of a macromolecular drug of the present invention

[0063] The present invention also relates to a macromolecular drug delivery method, characterized in that the method comprises:

[0064] (A) controlling a low frequency pulsed alternating current device;

[0065] (B) controlling an ultrasound device; and

[0066] (C) A delivery device, under the action of the low-frequency pulsed alternating current device and the ultrasonic device, promotes tissue penetration and nerve transmission of biomacromolecular drugs.

[0067] In a preferred embodiment, in the step (A), the low-frequency pulse alternating current device emits a pulse current of 50-600 Hz.

[0068] In a preferred embodiment, in the step (B), the ultrasonic frequency of the ultrasonic device is 50-400KHz, and the ultrasonic intensity is 0.5-1.0W / m 2 .

[0069] In a preferred embodiment, in the step (A) and the step (B), the low-frequency pulsed alternating current device and the u...

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Abstract

The invention relates to a macromolecular drug delivery mechanism and a delivery method thereof. The delivery mechanism comprises a stimulation device, an ultrasonic device, a delivery device and a microneedle device, the stimulation device is electrically connected with the microneedle device, the delivery device is connected to the microneedle device, under the action of the ultrasonic device and the stimulation device, the macromolecular drug in the conveying device enters cranial nerves through the skin around the upper lip of the face and the wing of the nose so that the brain-entering delivery efficiency is improved. In the delivery mechanism, the alternating current is beneficial to promoting the transdermal permeation and nerve transmission effect of the biological macromolecular drug; ultrasonic waves generated by the ultrasonic device have a cavitation effect and a sound hole effect, and reversible open pore channels can be generated on the surface layer of skin and the surface of subcutaneous tissue cells, so that the permeability of drugs is improved, macromolecular drugs are promoted to enter subcutaneous nervous tissues as soon as possible, and brain-entering delivery of the drugs is achieved through the nerve brain-entering channel.

Description

technical field [0001] The present invention relates to a brain drug delivery device, in particular to a biomacromolecule drug brain delivery mechanism and a delivery method thereof. Background technique [0002] The blood-brain barrier is the most important bottleneck for the treatment of central diseases through peripheral administration of drugs into the brain, especially for hormones, peptides, proteins, genes or vaccines for the treatment of brain diseases. At present, drugs break through the blood-brain barrier mainly through structural or dosage form modification. [0003] The permeability of the blood-brain barrier (BBB) ​​is poor, and peripheral administration such as intravenous, intramuscular, subcutaneous and other routes cannot effectively deliver biomacromolecular drugs to the central nervous system (CNS). In addition, with the increase of the peripheral dose of biomacromolecular drugs, the systemic side effects also increase. [0004] The central administrat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M37/00A61N1/36A61N7/00
CPCA61M37/00A61M37/0015A61N1/36014A61N7/00A61M2037/0007A61M2037/0023A61M2037/003A61M2037/0046A61M2037/0061A61N2007/0039A61M37/0092
Inventor 赵应征鲁崔涛阮战伟张宏宇肖健聂辰瑶
Owner 温州医科大学慈溪生物医药研究院
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