Drug delivery carrier modified by dihydroartemisinin and its application in pharmacy

A technology of dihydroartemisinin and drugs, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve the problems of not being able to fully exert the design targeting function

Active Publication Date: 2021-04-23
SHENYANG PHARMA UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, once the targeted delivery form enters the blood, it is adsorbed by substances such as opsonins, complements, macroglobulins, and immunoglobulins in the blood, and a protein hydration crown is formed on the surface of the delivery form, which is then recognized by the reticuloendothelial system, Phagocytosis, clearance from the systemic circulation, cannot fully exert the targeted function conferred by design

Method used

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  • Drug delivery carrier modified by dihydroartemisinin and its application in pharmacy
  • Drug delivery carrier modified by dihydroartemisinin and its application in pharmacy
  • Drug delivery carrier modified by dihydroartemisinin and its application in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of carrier PPD modified by dihydroartemisinin:

[0046] Add polyethylene glycol (HO-PEG2000-COOH) into the three-necked flask, stir for 2 hours under reduced pressure nitrogen in an oil bath at 140°C, then add an equal amount of glycolide, lactide and an appropriate amount of stannous octoate The three-necked flask was refluxed for 10 h under the condition of an oil bath at 140° C., and PLGA-PEG2000-COOH was obtained by precipitation and extraction with ether. The above PLGA-PEG2000-COOH and dihydroartemisinin were reacted for 48 hours under the catalysis of EDCI and HObt to obtain PPD.

[0047]

[0048] The molecular weight of PLGA in the step is 8000, but it is not limited thereto. The PLGA of the present invention can also be PLGA modified with a carboxyl group at one end, but it is not limited to the above substances. The molecular weight of PLGA can be in the range of 8000-38000.

[0049] Determination by NMR 1 H-NMR hydrogen spectrum determines t...

Embodiment 2

[0051] Preparation of Docetaxel-loaded Nanoparticles by Emulsion Solvent Evaporation

[0052] Weigh 1 mg of docetaxel or 0.1 mg of coumarin 6, dissolve it in an appropriate amount of dichloromethane, add 20 mg of the PPD prepared in Example 1, add 5 mL of deionized water containing 0.5% PVA, ultrasonicate the probe at 300 W for 5 min, and use centrifugation Remove unwrapped medication. The preparation method of PP nanoparticles is similar, just replace PPD with PP.

[0053] The nanoparticles prepared in Example 2 were measured by dynamic light scattering and transmission electron microscopy for their particle size and shape. The result is as image 3 , the particle size of the nanoparticles is about 150nm, and the particle size distribution is narrow; the transmission electron microscope shows that the drug-loaded nanoparticles are spherical with uniform particle size.

Embodiment 3

[0055] Preparation of DHA-PEG-Stearate-modified liposomes loaded with docetaxel or coumarin 6 by film dispersion method

[0056] Weigh 1 mg of docetaxel or 0.1 mg of coumarin 6, dissolve in an appropriate amount of dichloromethane, add 2 mg of DHA-PEG-Stearate (dihydroartemisinin-polyethylene glycol-stearate) prepared in Example 2 vehicle), and 30 mg of soybean lecithin and 1 mg of cholesterol. Spin dry to form a film, add 2 mL of deionized water for hydration for 30 min, sonicate the probe at 300 W for 5 min, and remove uncoated drugs by microcolumn centrifugation.

[0057] The liposomes prepared in Example 3 were determined by dynamic light scattering and transmission electron microscopy to determine the particle size and shape of the liposomes. The result is as Figure 4 , 5 , the particle size of the liposome is about 130nm, and the particle size distribution is narrow; the transmission electron microscope shows that the drug-loaded liposome is spherical with uniform pa...

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Abstract

The invention belongs to the field of new excipients and new dosage forms for pharmaceutical preparations, and relates to the design and application of a drug delivery system targeting endogenous apolipoprotein E, including the linking of dihydroartemisinin (DHA) through polyethylene glycol (PEG) Design and synthesis of carrier structures for arm modification of hydrophobic materials. The active customized apolipoprotein E carrier material used uses DHA as the target, polyethylene glycol as the linking arm, and hydrophobic materials (such as PLGA, etc.) as the anchoring site. The nano-delivery preparation prepared by the carrier material can encapsulate a variety of anti-tumor drugs, and can interact with the low-density lipoprotein receptor (LDLr) highly expressed by tumor cells through the surface DHA-bound apolipoprotein E to overcome a variety of anti-tumor drugs. The biological transmission barrier effectively enhances the accumulation of nanoparticles in tumor sites, as well as their uptake in tumor cells and their antitumor activity. The nano-delivery preparation has good stability, high safety and good targeting, can be used for intravenous injection, and has a large market application prospect.

Description

technical field [0001] The invention belongs to the field of new excipients and new dosage forms of pharmaceutical preparations, and relates to the design and application of drug delivery carriers targeting endogenous apolipoprotein E, including dihydroartemisinin (DHA) linked by polyethylene glycol (PEG) The carrier structure design, synthesis and application of the modification of the arm to the hydrophobic material. Background technique [0002] Cancer is also known as malignant tumor. Currently, the most effective treatment is chemotherapy, but while chemotherapy kills tumor cells, it also kills its own healthy cells. Therefore, in order to reduce the toxic and side effects, tumor-targeted nano-drug delivery system came into being. The design principle of targeted nano-drug delivery system is to modify the surface of nano-delivery forms (such as nanoparticles, liposomes, micelles, nanoemulsions, nano-gels, and nanovesicles) with small molecules, ligands, or antibodies. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/22A61K47/34A61K31/337A61P35/00
CPCA61K9/5123A61K9/5146A61K31/337A61P35/00
Inventor 孙进李真宝何仲贵李丹孙英华
Owner SHENYANG PHARMA UNIVERSITY
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