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Polysaccharide core Nanocells as well as preparation method and application thereof

A polysaccharide and core technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve drug leakage and instability, restriction, biocompatibility and affinity Weak and other issues

Active Publication Date: 2021-09-14
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Liposomes are spherical vesicles with a phospholipid bilayer membrane covering a water-based core. They can encapsulate both water-soluble drugs and fat-soluble drugs. Their characteristics similar to cell membranes make them easy to cross biological barriers and have good biocompatibility. and affinity, but the drug leakage and instability during liposome storage limit its application
The drug loading stability of nanoparticles is better than that of liposomes, but the biocompatibility and affinity are relatively weak

Method used

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  • Polysaccharide core Nanocells as well as preparation method and application thereof
  • Polysaccharide core Nanocells as well as preparation method and application thereof
  • Polysaccharide core Nanocells as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] Example 1 Preparation of doxorubicin-loaded polysaccharide nanoparticles

[0141] Take pectin (relative molecular weights are 39, 50, 73kDa), sodium alginate (relative molecular weights are 80, 100, 120kDa) or chitosan (deacetylation degree ≥95%, 85%, respectively, relative molecular weights are 130, 220, 300k Da) were dissolved in water or sodium acetate buffer (pH=4.5~5.5) to obtain concentrations of 0.1, 0.2, 0.5, 1, 5, 10, 20, 25, 30, 35, 40, 45, 50mg / mL pectin, sodium alginate or chitosan solution as water phase, respectively take appropriate amount of emulsifier Span 20, Span80, Span 85 or bis(2-ethylhexyl) sodium sulfosuccinate (AOT) Soluble in oily solvent oleic acid, soybean oil, linoleic acid, linolenic acid or olive oil as different oil phases (the mass percentage concentration of emulsifier in oil phase is 0.1%, 0.2%, 0.5%, 1% respectively , 2%, 2.5%, 5%, 7.5%, 10%, 15%, 20%), respectively 35:1, 30:1, 25:1, 20:1, 15:1, 10:1, 5 : 1, 2: 1 different oil: wate...

Embodiment 2

[0154] Example 2 Preparation of Cytarabine-loaded Pectin Nanoparticles

[0155] According to the mass ratio of drug (cytarabine hydrochloride) to carrier material of 1:1, 1:2.5, 1:5, 1:7.5, and 1:10, pectin (relative molecular weight: 39, 50, 73k Da) Dissolved in water with the drug, the mass percentage concentrations of pectin were 5, 10, 20, 30, 40 mg / mL, respectively, to obtain drug-containing pectin solutions of different concentrations as the water phase, and respectively take the emulsifiers Span 20, Span80, Span 85 or bis(2-ethylhexyl) sodium sulfosuccinate (AOT) in appropriate amount dissolved in oily solvent oleic acid, soybean oil, linoleic acid, linolenic acid or olive oil as different oil phases (emulsifier in oil phase The mass percentage concentrations in the , 15:1, 10:1 different oil:water volume ratios to disperse different water phases in different oil phases (ultrasonic dispersion conditions: power are 100, 200, 300, 400, 500W, respectively, time is 10 seco...

Embodiment 3

[0157] Example 3 Preparation of doxorubicin-loaded polysaccharide core Nanocells

[0158] In this example, any one of the following methods is used to prepare doxorubicin-loaded polysaccharide core Nanocells.

[0159] (1) Method (A): Doxorubicin-loaded polysaccharide nanoparticles, namely, doxorubicin-loaded pectin nanoparticles, doxorubicin-loaded sodium alginate nanoparticles, and doxorubicin-loaded polysaccharide nanoparticles were prepared according to the method in Example 1. Chitosan nanoparticles (obtained by the preferred conditions in Example 1: that is, the mass ratio of doxorubicin and blank pectin nanoparticles is 1:4, and the doxorubicin-loaded pectin nanoparticles are prepared by adsorption and drug loading at room temperature; The mass ratio of blank sodium alginate nanoparticles was 1:4, and the doxorubicin-loaded sodium alginate nanoparticles were prepared by adsorption and drug loading at room temperature; the mass ratio of doxorubicin and blank chitosan nano...

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Abstract

The invention discloses polysaccharide core Nanocells as well as a preparation method and application thereof. Each polysaccharide core Nanocell is of a core-shell structure, a nanoparticle made of a polysaccharide material serve as a core, the outer layer of the nanoparticle is wrapped with a lipid membrane which is formed by a lipid material and similar to a lipidosome capsule membrane, and a medicine is entrapped in the nanoparticle, and / or between the lipid membrane and the nanoparticle core, and / or entrapped on the lipid membrane. According to the polysaccharide core Nanocells, different lipid materials can be adopted, or lipid is modified with different targeting guide molecules, and magnetic particles are wrapped or materials or medicines sensitive to the microenvironment of a corresponding disease site are added, so that the polysaccharide core Nanocell with different targeting functions is obtained; medicines of various mechanisms can be simultaneously entrapped, so that multifunctional treatment on diseases is realized; and the sustained-release long-acting effect is achieved while targeted therapy is achieved, the effect of reversing medicine resistance can be achieved, and the medicine curative effect and the medication compliance are improved.

Description

technical field [0001] The invention belongs to the field of biomedicine, and particularly relates to polysaccharide core Nanocells and a preparation method and application thereof. Background technique [0002] Targeted therapy has always been an ideal way to treat diseases, which can improve the efficacy of drugs and overcome toxic and side effects, which has attracted more attention in the treatment of cancer. Cancer is a serious threat to human health, bringing great physical and mental pain and heavy economic burden to patients and their families. Cancer treatment methods and drugs are constantly being introduced, among which chemotherapy drugs are still the main means of clinical cancer treatment. Common chemotherapeutic drugs are a double-edged sword. They are commonly used and effective in the first-line clinical treatment of cancer. However, due to poor selectivity, they can also cause toxic and side effects such as damage to important organs such as the heart, liv...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/51A61K45/00A61K31/704A61K47/36A61K47/54A61K47/69A61K47/24A61P35/00
CPCA61K9/5161A61K9/5123A61K9/1271A61K9/1277A61K9/5192A61K47/545A61K47/6911A61K47/6939A61K47/36A61K45/00A61K31/704A61P35/00Y02A50/30
Inventor 李沙蒋杰欧阳嘉碧杨莫辉欧金来洪宝贤叶秋绵龚甜
Owner JINAN UNIVERSITY
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