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Amaryllidaceous alkaloid targeted sustained-release preparation and preparation method and use thereof

A slow-release preparation and alkaloid technology, applied in the field of medicine, can solve problems such as changing drug properties, and achieve the effects of low toxicity and improved bioavailability

Inactive Publication Date: 2016-08-17
SHENZHEN ELDERLY MEDICAL RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Prodrugs have the risk of changing drug properties and introducing toxicity, and opening the tight structure of the blood-brain barrier may introduce other harmful substances

Method used

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  • Amaryllidaceous alkaloid targeted sustained-release preparation and preparation method and use thereof
  • Amaryllidaceous alkaloid targeted sustained-release preparation and preparation method and use thereof
  • Amaryllidaceous alkaloid targeted sustained-release preparation and preparation method and use thereof

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Effect test

Embodiment 1

[0073] The Lycoris alkaloids targeted sustained-release preparation of the present invention is composed of Lycoris alkaloids, propylylated chitosan and low-density lipoprotein with azide probe, and the molar ratio of the three is 1:0.5:1.5 .

[0074] The preparation method of the Lycoris alkaloid targeted slow-release preparation of the present invention is:

[0075] Proyne acylation of the alkyne group on chitosan and the azide on the low-density lipoprotein with an azide probe at room temperature by click chemistry for 24 hours to synthesize the LDL targeting end as the amphiphile of the hydrophobic end The molecule self-assembles with the Lycoris alkaloid to form the Lycoris alkaloid nano-brain targeting agent with the LDL targeting end exposed.

[0076] As a natural polysaccharide, chitosan has the characteristics of good biocompatibility and biodegradability, and is especially suitable for drug carriers. However, the main problem limiting its application is poor water ...

Embodiment 2

[0102] Lycoris alkaloids targeted slow-release preparation of the present invention is composed of lycoris alkaloids, propynoylated chitosan and low-density lipoprotein with azide probe, the weight ratio or molar ratio of the three is 1: 1:1.5.

[0103] Others are the same as embodiment 1.

Embodiment 3

[0105] Lycoris alkaloids targeted slow-release preparation of the present invention is composed of lycoris alkaloids, propynoylated chitosan and low-density lipoprotein with azide probe, the weight ratio or molar ratio of the three is 1: 1:2.

[0106] Others are the same as embodiment 1.

[0107] (1) Research on drug release rules and system degradation mechanism of nanobrain targeted preparations

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Abstract

The invention discloses an amaryllidaceous alkaloid targeted sustained-release preparation and a preparation method and a use thereof. The amaryllidaceous alkaloid targeted sustained-release preparation is composed of amaryllidaceae alkaloid, propargyl acylated chitosan and low density lipoprotein having an azide probe, wherein the molar ratio of the three components is 1 to (0.1-1) to (0.1-2). An LDL receptor of blood-brain barrier endothelial cells is selected as a target for transmission of amaryllidaceae alkaloid to treat AD, chitosan having excellent biological compatibility is used as a drug carrier material, the low-toxicity and high-efficiency amaryllidaceous alkaloid nano brain-targeted preparation is developed, and some blanks in researches before clinical application of amaryllidaceae alkaloid as an AD treatment drug at present are filled.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a targeted slow-release preparation of lycoris alkaloids and its preparation method and application. Background technique [0002] Alzheimer's disease (AD) is an senile neurodegenerative disease with memory impairment and cognitive impairment as the main clinical manifestations, and its pathological feature is a large amount of extracellular amyloid peptide (β-Amyloid peptide, Aβ) deposition Senile plaques (Senileplaques, SP), intracellular phosphorylated tau protein-based neurofibrillary tangles (Neurofibrillary tangles, NFT) and a large number of degeneration and loss of central nervous cells dominated by cholinergic neurons. Although the pathogenesis of AD has not been fully elucidated, the cholinergic hypothesis and the Aβ hypothesis have received the most attention. [0003] At present, anti-acetylcholinesterase preparations are still the mainstay of AD drug treatment, esp...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/42A61K47/36A61K36/88A61P25/28
Inventor 吴正治段丽红
Owner SHENZHEN ELDERLY MEDICAL RES INST
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