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A kind of chitosan lipoprotein nasal administration nanocomposite and its preparation method and application

A nano-composite and nasal drug delivery technology, which is applied in nano-drugs, drug combinations, drug delivery, etc., can solve problems such as burden, and achieve the effects of good absorption, high-efficiency brain targeting, and smooth and round appearance

Active Publication Date: 2022-07-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of nanocomposite involves the catabolism of chitosan after entering the brain, which brings unnecessary burden to the body

Method used

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  • A kind of chitosan lipoprotein nasal administration nanocomposite and its preparation method and application
  • A kind of chitosan lipoprotein nasal administration nanocomposite and its preparation method and application
  • A kind of chitosan lipoprotein nasal administration nanocomposite and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Weigh 0.5 g of chitosan (molecular weight is 150KDa, deacetylation degree is 98%) and dissolve it in 60 mL of 0.5% acetic acid solution. Another 4-carboxyphenylboronic acid (PBA) and 206.6 mg of N-hydroxysuccinimide (NHS) with 0.45 times the molar amount of chitosan units were weighed and dissolved in 30 mL of methanol, and stirred at room temperature for 30 min. 342.57 mg of 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC·HCl) was weighed and added to the PBA / NHS mixed solution, and the mixture was stirred to dissolve uniformly. Then the PBA / NHS / EDC·HCl mixed solution was added to the acetic acid solution of chitosan (the volume ratio of methanol and water in the reaction system was 1:2), stirred at room temperature for 24 hours, and the reaction solution was transferred to a molecular weight cut-off of 14 ×10 3 Dialyzed in deionized water for 72h, changing the water every 4h. The dialyzed samples were freeze-dried to obtain a light yellow powdery chitosan-phenyl...

Embodiment 2

[0046] With reference to the process conditions of Example 1, chitosan (molecular weight is 150KDa, deacetylation degree is 98%) is adjusted to chitosan (molecular weight is 150KDa, deacetylation degree is 60%) to obtain chitosan-phenylboronic acid For the grafted polymer, the graft ratio of 9% was obtained by calculating the peak area of ​​NMR.

Embodiment 3

[0048] With reference to the process conditions of Example 1, chitosan (molecular weight is 150KDa, deacetylation degree is 98%) is adjusted to chitosan (molecular weight is 150KDa, deacetylation degree is 80%) to prepare chitosan-phenylboronic acid For the grafted polymer, the NMR peak area calculation method was used to obtain a graft ratio of 12%.

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Abstract

The invention belongs to the field of pharmaceutical preparations, and discloses a chitosan lipoprotein intranasal administration nanocomposite, comprising lipoprotein nanoparticles, chitosan or / and chitosan derivatives having the effect of promoting absorption of nasal mucosa. The invention also discloses a preparation method of chitosan lipoprotein intranasal administration nanocomposite, comprising: self-assembling chitosan or / and chitosan derivatives and lipoprotein nanoparticles through dynamic force to form a good membrane permeability nasal preparations. The preparation condition of the chitosan lipoprotein intranasal administration nanocomposite is mild, the process is simple, and the industrialized production is easy. The system is safe, non-toxic, and has good biodegradability, which can improve the absorption of lipoprotein drugs in the nasal mucosa and ensure high-efficiency brain targeting. The dosage form is administered by nasal drops, sprays, etc., and is easy to operate, convenient for patients who take the medicine for a long time, and has a good clinical application prospect in the treatment of central nervous system diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a chitosan lipoprotein nasal administration nanocomposite and a preparation method and application thereof. Background technique [0002] In recent years, the research and development of central nervous system (CNS) diseases such as Alzheimer's disease, Parkinson's disease, stroke, and glioma are very fast. However, due to the existence of the blood-brain barrier (BBB), the natural physiological barrier of brain tissue, more than 98% of the drugs with central therapeutic activity lose their efficacy because they cannot cross the BBB. Although peptides and small protein molecules can cross the BBB to the brain by systemic administration, high therapeutic doses result in a series of adverse effects. Although the drug can be delivered directly into the brain by direct injection into the ventricle or parenchyma, this invasive mode of administration is significa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K9/19A61K47/61A61K45/00A61P25/16A61P25/28A61P35/00B82Y5/00B82Y30/00B82Y40/00
CPCA61K9/0043A61K9/5169A61K9/19A61K45/00A61K47/61B82Y5/00B82Y30/00B82Y40/00A61P25/28A61P25/16A61P35/00
Inventor 周建平丁杨张华清于淼金熠
Owner CHINA PHARM UNIV
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