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A preparation method of carrier-free macrolide immunosuppressive drug nanoparticles

A macrolide, immunosuppressive technology, applied in pharmaceutical formulations, pharmaceutical combinations, medical preparations containing active ingredients, etc. Low problems, to solve potential toxicity, high drug loading efficiency, and improve water solubility

Inactive Publication Date: 2021-06-22
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to provide a method for preparing self-assembled nanoparticles of macrolide immunosuppressive drugs without a carrier, so as to solve the problems of low drug loading and encapsulation efficiency and uncertain carrier biotoxicity existing in existing nanometer drug delivery systems. The preparation process of the carrier is cumbersome and other problems

Method used

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  • A preparation method of carrier-free macrolide immunosuppressive drug nanoparticles
  • A preparation method of carrier-free macrolide immunosuppressive drug nanoparticles
  • A preparation method of carrier-free macrolide immunosuppressive drug nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of carrier-free rapamycin self-assembled nanoparticles

[0032] Accurately weigh 0.004 g of rapamycin powder, 6 parts in total, dissolve in 50 μL, 100 μL, 125 μL, 200 μL, 250 μL and 500 μL of methanol respectively, sonicate for 10 min to dissolve, add dropwise to the vortex Shake in 1000 μL of water, and keep shaking for 0.5 h~1 h. Dry the organic solvent with pure nitrogen, sonicate for 30-60 min, centrifuge at 3000 rpm, and remove free drug for 10 min to obtain organic solvent-water ratios of 1:20, 1:10, 1:8, 1:5, and 1, respectively. :4 and 1:2 carrier-free rapamycin self-assembled nanoparticle solutions. The molecular structure of rapamycin is figure 1 As shown, the obtained particle size diagrams of different ratios of carrier-free rapamycin self-assembled nanoparticle solutions are shown in Figure 2.

[0033] When the ratio of organic solvent to water ranges from 1:2 to 1:20, the particle size gradually decreases to stabilize at around 130 nm, becau...

Embodiment 2

[0035] Determination of Drug Loading Capacity and Encapsulation Efficiency of Carrier-free Rapamycin Self-Assembled Nanoparticles

[0036] The carrier-free rapamycin self-assembled nanoparticle solutions of different proportions prepared in Example 1 were measured with a UV photometer, according to drug loading = (drug content in nanoparticles / total weight of nanoparticles) × 100 %, Encapsulation Efficiency = (Total Drug Amount - Free Drug Amount) / Total Drug Amount × 100 % Calculate the drug loading and encapsulation efficiency of each ratio. The result is as image 3 , each ratio has a higher drug loading and encapsulation efficiency, which is superior to the traditional organic or inorganic nano drug loading system, and when the organic solvent-water ratio is 1:10, the particle size is moderate, the drug loading is 87.45% and The encapsulation rate is 95.53%, which is the best ratio.

Embodiment 3

[0038] Determination of the Morphology of Self-Assembled Nanoparticles of Carrier-Free Rapamycin

[0039] Carrier-free rapamycin self-assembled nanoparticles with an organic solvent-water ratio of 1:10 prepared according to the method of Example 1 were diluted 5 times with water, dropped on a flat and clean mica sheet surface for natural adsorption for 20 min, The surface of the mica flakes was then carefully cleaned with ultrapure water and immediately dried with nitrogen gas. The obtained samples were placed under the AFM instrument of the model Multimode 8 (Bruker, Germany) to observe the morphology through intelligent mode scanning imaging in air. The result is as Figure 4 As shown, the obtained carrier-free rapamycin self-assembled nanoparticles are round-shaped particles with relatively uniform size.

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Abstract

The invention provides a preparation method of a carrier-free macrolide immunosuppressive drug nanoparticle. The carrier-free macrolide immunosuppressive drug nanoparticles are self-assembled to form small-molecule carrier-free nanoparticles through a solvent exchange method, which effectively improves the water solubility of the macrolide immunosuppressive drug and inhibits concentration-dependently. growth of tumor cells. The method is convenient to operate, simple and easy to operate, the prepared nanoparticles have small particle size, high drug loading efficiency and good stability, thereby improving the availability of macrolide immunosuppressive drugs.

Description

technical field [0001] The invention relates to the field of biomaterials and nanotechnology, in particular to a preparation method for self-assembling hydrophobic drugs into carrier-free nanometer drugs. Background technique [0002] According to the latest global cancer statistics in 2018, there are an estimated 18.19 million new cancer cases and 9.6 million cancer deaths worldwide. In China, about 10,000 people are diagnosed with cancer every day, and 7 people are diagnosed with cancer every minute. Therefore, effectively treating cancer has become an urgent problem in the medical field. [0003] Immunosuppressants refer to drugs that can suppress the immune response of the body, and can inhibit the proliferation and function of macrophages related to the immune response, such as T cells and B cells, thereby reducing the antibody immune response. Immunosuppressants are currently mainly used for anti-rejection after organ transplantation and autoimmune diseases such as l...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/436A61P37/06
CPCA61K9/14A61K31/436A61P37/06
Inventor 邵敬伟乐景青郭燕李超
Owner FUZHOU UNIV
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