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Nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and preparation method and application thereof

A technology with attenuating effect and nanoparticles, which can be used in medical preparations with non-active ingredients, medical preparations containing active ingredients, and drug combinations, etc. Reducing the dose of medication, the effect of a clear dose-response relationship

Active Publication Date: 2019-01-18
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are also the problems of high toxicity and side effects of ACGs and a narrow therapeutic window.

Method used

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  • Nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and preparation method and application thereof
  • Nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and preparation method and application thereof
  • Nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0043] The present invention also provides a preparation method of nanoparticles having a synergistic and attenuating effect on the total lactones of anemone apple described in the above technical scheme, comprising the following steps:

[0044] Mix active ingredients, excipients and organic solvents to obtain a mixed solution;

[0045] The mixed solution is added into water under the condition of ultrasonic or stirring, and the organic solvent is removed to obtain the nanoparticles with synergistic and attenuating effects on total annona lactones.

[0046] The invention mixes active components, auxiliary materials and organic solvents to obtain a mixed solution. In the present invention, the organic solvent preferably includes one or more of DMSO, DMF, methanol, ethanol, propanol, acetonitrile, isopropanol, PEG400 and PEG600.

[0047] In the present invention, the mass volume concentration of the active ingredient in the mixed solution is preferably 0.001%-20% w / v, and the m...

Embodiment 1

[0060] Example 1 Preparation of drug-loaded nanoparticles of total lactones of anemone apple with poloxamer as an auxiliary material

preparation example 1

[0062] Weigh 5 mg of total lactones of annuus apple and 25 mg of poloxamer P188 and dissolve them in 0.2 mL of ethanol. Slowly instill the above ethanol solution into 5 mL of deionized water at room temperature under ultrasonic conditions of 250 Hz. After continuing to sonicate for 15 min, the ethanol was removed by rotary evaporation to obtain ACGs nanoparticles (P188-ACGs-NPs). The average particle diameter is 179.9 nm, the polydispersity index (PDI) is 0.130, and the potential value is -19.4 mV.

[0063] Take the P188-ACGs-NPs (1 mg / mL) in Preparation Example 1, dilute to 100 μg / mL, absorb 5 μL and drop it on a 300-mesh copper grid, let it dry naturally in the air, and then stain it with 0.1% uranyl acetate for 10 min, transmission electron microscope image Such as figure 1 As shown, it can be seen that the prepared ACGs-NPs are spherical or spherical.

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Abstract

The invention provides a nanoparticle with effect-enhancing and toxicity-reducing effect on synergistic and attenuating effects on annonaceous acetogenins drugs, and belongs to the field of pharmaceutical preparations. The present invention uses poloxamer P188, Poloxamer P407, Poloxamer P124, one or more of poloxamer P237 and poloxamer P338 are adjuvants, By limiting the kinds and dosage of excipients, the problems of insoluble and difficult administration of annonolactone are solved, and more importantly, the anti-tumor effect in vivo is improved, at the same time, it has better safety, breaks through the bottleneck problem of narrow window of treatment of annonolactone, and provides a feasible solution for clinical application.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a nanoparticle having a synergistic and attenuating effect on anemone lactones, a preparation method and application thereof. Background technique [0002] Annonaceous acetogenins (AAGs), also known as annonaceous acetogenins, are a large class of long-chain fatty acid lactone compounds from Annonaceae. The basic chemical structure is a chemical skeleton composed of 35-37 carbon atoms. Contains 0 to 3 tetrahydrofuran rings (THF), with a methyl-substituted or rearranged γ-lactone ring at the end and 2 long straight alkyl chains connecting these parts, usually containing some in the long aliphatic chain Stereochemically variable oxygen-containing functional groups (such as hydroxyl, acetoxy, ketooxy) or double bonds, etc., usually have multiple chiral carbon atoms, and the three-dimensional structure is relatively complicated. The structural formula is as follow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K9/51A61K47/10A61P35/00
CPCA61K9/5146A61K31/365A61P35/00
Inventor 王向涛高艺璇周欣欣李好文敖惠郭一飞韩美华
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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