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Dihydroartemisinin modified drug delivery carrier and application thereof in pharmaceutical science

A technology of dihydroartemisinin and drugs, which can be applied to drug combinations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Biological transfer barrier, easy operation, good stability

Active Publication Date: 2018-09-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • 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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  • Dihydroartemisinin modified drug delivery carrier and application thereof in pharmaceutical science
  • Dihydroartemisinin modified drug delivery carrier and application thereof in pharmaceutical science
  • Dihydroartemisinin modified drug delivery carrier and application thereof in pharmaceutical science

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 auxiliary materials and new dosage forms for pharmaceutical preparations and relates to design and application of a drug delivery system taking endogenous apolipoprotein E as a target spot, comprising design and synthesis of a carrier structure modifying a hydrophobic material by virtue of a polyethylene glycol (PEG) connecting arm by dihydroartemisinin (DHA). The used carrier material actively customizing apolipoprotein E takes DHA as a target head, PEG as a connecting arm and the hydrophobic material (such as PLGA) as an anchoring part. A nano delivery preparation prepared from the carrier material can encapsulate multiple anti-tumor drugs, and by virtue of interaction of the apolipoprotein combined with DHA on the surface of the nano delivery preparation and low density lipoprotein receptors (LDLr) highly expressed by tumor cells, multiple biological transmission barriers are overcome, and accumulation of nano particles at tumor parts as well as intake and anti-tumor activity in the tumor cells are effectively improved. The nano delivery preparation has good stability, high safety and excellent targeting capability, can be applied to intravenous injection and has a relatively great 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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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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