Oral nanoparticles of artemisinin-loaded citrus pectin

A technology of nanoparticles and artemisinin, which is applied in the field of oral nanoparticles of citrus pectin, can solve the problems of good biocompatibility, strong antigenicity, and not found, and achieve obvious sensitivity, enhanced stability, and high loading The effect of drug efficiency

Active Publication Date: 2022-07-12
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, concanavalin and glucose oxidase are proteins, which have the disadvantages of high cost, instability, and strong antigenicity.
[0007] Therefore, although the way of oral medicine is the best choice for diabetic patients, it has not yet found a drug that has a stable point, low toxicity, good biocompatibility, high drug loading rate and release rate, and has a certain effect on diabetic complications. Oral drugs

Method used

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  • Oral nanoparticles of artemisinin-loaded citrus pectin
  • Oral nanoparticles of artemisinin-loaded citrus pectin
  • Oral nanoparticles of artemisinin-loaded citrus pectin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Example 1 Preparation of Oral Nanosystem Loaded with Artemisinin & Citrus Pectin

[0106] The preparation process of the oral nano-examples loaded with artemisinin / citrus pectin is as follows: figure 1 shown:

[0107] Step 1: Preparation of MCP(ART) Nanoparticles

[0108] First, denature the citrus pectin, put the citrus pectin in distilled water at a concentration of 1.5 mol / L, and increase its pH to 10.0 with sodium hydroxide (3 mol / L) at 55 °C, and continue stirring for 1 hour , then the solution was cooled to room temperature, the pH was adjusted to 10.0 with sodium hydroxide (3 mol / L), and the denatured citrus pectin was dissolved.

[0109] Then add the artemisinin dissolved in the organic solvent under the condition of 55 ℃, make the final concentration of artemisinin be 1.5mol / L 600rmp stir 2 hours, add calcium hydroxide to its final concentration is 0.01mol / L, Stir at 600 rmp at 55°C for 1 hour, finally add sodium bicarbonate to a final concentration of 0.01 ...

Embodiment 2

[0115] Example 2 Characterization of Oral Nanoparticles Loaded with Artemisinin & Citrus Pectin

[0116] 1. Infrared spectroscopy detection

[0117] The raw materials MCP, AAPBA, TMC synthesized by the system and the synthetic materials MCP(ART), MCP(ART)-AAPBA and MCP(ART)-AAPBA-TMC prepared in Example 1 were used for infrared spectrum detection.

[0118] 1. Experimental method

[0119] Freeze-dry the sample to be tested, then put it in a mortar, add a certain amount of KBr, grind the mixture evenly, and grind the mixture to a particle size of less than 2 μm to avoid the influence of scattered light, and then put it in a dryer for drying. The mixture was pressed into a transparent sheet on a hydraulic press with a pressure of about 10 MPa, and was measured using a German Bruker VERTEX 33 Fourier transform infrared spectrometer.

[0120] 2. Experimental results

[0121] In order to understand the changes in the formation stage of artemisinin-loaded / citrus pectin particles, ...

Embodiment 3

[0165] Example 3 Cell experiment of oral nanoparticles loaded with artemisinin & citrus pectin

[0166] 1. Experimental method

[0167] The biotoxicity of MCP(ART)-AAPBA-TMC oral nanotransporters at the cellular level will be evaluated by MTT assay.

[0168] 1. Cell culture

[0169] HepG-2 cell line was provided by Guangdong University of Pharmacy. After the cells were proliferated and cultured to 80% in the culture flask, they were seeded on a 96-well plate at a density of 5000 / well and cultured for 1 or 2 days for subsequent experiments. The cell culture conditions are: high glucose DMEM medium containing 20% ​​newborn bovine serum and non-essential amino acids, 37°C, 5.0% CO 2 .

[0170] 2. MTT transport system toxicity

[0171]Different doses of the transport system were added to the cultured cells, and after 24 hours, the cell viability was measured by MTT method. That is, inoculate HepG-2 cells on a 96-well culture plate, 5000 cells / well, after culturing for 24 hou...

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Abstract

The invention discloses an oral nanoparticle of citrus pectin loaded with artemisinin, and a preparation method thereof comprises the following steps: performing multi-molecular self-polymerization of the citrus pectin; making the citrus pectin form nanoparticles and wrapping and adsorbing the artemisinin carried out; aminophenylboronic acid was linked to citrus pectin nanoparticles; denatured chitosan was encapsulated in the outer layer. The invention combines citrus pectin and artemisinin for the first time, so that the insulin resistance of type II diabetes and the damage of pancreatic islet beta cells are simultaneously improved; the method of transforming islet alpha cells into pancreatic islet beta cells is applied to the nano-treatment of type II diabetes, This method can inhibit the secretion of glucagon, and can also increase the secretion of insulin; both the drug and the delivery material are natural products derived from plants to ensure non-toxicity and easy metabolism in the treatment of type II diabetes.

Description

technical field [0001] The invention relates to the technical field of medical nanomaterials, and more particularly, to an oral nanoparticle of citrus pectin loaded with artemisinin. Background technique [0002] Diabetes mellitus is a metabolic disease with multiple etiologies. It is manifested by insufficient insulin secretion of the pancreas or decreased sensitivity of surrounding tissues to insulin. Therefore, the liver, muscles and other tissues cannot convert glucose in the blood, resulting in metabolic disorder of the body, which can lead to death in severe cases. The number of people with diabetes in the world is about 280 million, of which 5% to 10% are type I diabetes, and type II diabetes accounts for 90% to 95% of new cases of diabetes. The pancreatic islet beta cells have lost 70% to 90% at the first onset of type I diabetes, and all the islet beta cells die 1 to 2 years after the onset of the disease, and the insulin secretion is about zero. Type 2 diabetes us...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/69A61K31/366A61K9/52A61K47/36A61P3/10A61P5/50
CPCA61K31/69A61K31/366A61K9/5161A61P3/10A61P5/50A61K2300/00Y02A50/30
Inventor 关燕清李健黄景敏
Owner SOUTH CHINA NORMAL UNIVERSITY
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