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Docetaxel-resveratrol co-loaded nano long-circulating liposome as well as preparation method and application thereof

A long-circulation liposome and docetaxel technology, which is applied in liposome delivery, nanotechnology, nanotechnology, etc., can solve the problem that liposomes cannot reach the target site completely, the treatment effect is not good, easy aggregation and penetration Leakage and other problems, to improve drug penetration and retention effects, more clinical application value, reduce side effects

Pending Publication Date: 2020-08-25
THE SECOND HOSPITAL OF SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inventors have found that liposomes also have some problems and deficiencies, such as poor stability, easy aggregation and leakage, and are easily cleared quickly by the reticuloendothelial system (Reticuloendothelial system, RES) after entering the blood simultaneously, making the lipid The body cannot fully reach the target site, resulting in poor treatment effect

Method used

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  • Docetaxel-resveratrol co-loaded nano long-circulating liposome as well as preparation method and application thereof
  • Docetaxel-resveratrol co-loaded nano long-circulating liposome as well as preparation method and application thereof
  • Docetaxel-resveratrol co-loaded nano long-circulating liposome as well as preparation method and application thereof

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Experimental program
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preparation example Construction

[0034] Specifically, the preparation method includes:

[0035] Co-dissolve the above-mentioned active pharmaceutical ingredients and lipid membrane materials in an organic solvent, evaporate under reduced pressure to form a lipid film, and then dry to completely remove the solvent;

[0036] The dried film is hydrated with PBS and then ultrasonically processed to obtain crude liposomes; the crude liposomes are filtered and granulated.

[0037] In another specific embodiment of the present invention, the organic solvent may be any one or more of methanol, absolute ethanol, acetonitrile and methylene chloride;

[0038] In another specific embodiment of the present invention, the reduced pressure evaporation temperature is controlled to be 30-60°C;

[0039] In another specific embodiment of the present invention, the ultrasonic treatment control time is 10-30 minutes;

[0040] In another specific embodiment of the present invention, the specific method for filtering and granulating is: passi...

Embodiment

[0050] 1. Research process

[0051] 1) Study on the anti-tumor effect of different ratios of docetaxel-resveratrol combined

[0052] Apply different ratios of docetaxel-resveratrol to human prostate cancer cells (PC3, DU145), lung cancer cells (A549, H460) and liver cancer cells (HepG2, HUH7) to study resveratrol by inhibiting proliferation and inducing apoptosis The synergistic anti-tumor activity of attriol and docetaxel was evaluated by the combination index (CI) to evaluate the combined anti-tumor effect on tumor cells based on the combination of different ratios of DTX-Res. Calculated as follows:

[0053]

[0054] Among them, D m1 Refers to the corresponding concentration of Drug-1 when used alone to produce X cell inhibition rate; D 1 Refers to the corresponding concentration of Drug-1 when the drug-1 and Drug-2 are used in combination to produce the same inhibition rate of x; similarly, D m2 Refers to the corresponding concentration when the drug alone produces the X cell inh...

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Abstract

The invention provides a docetaxel-resveratrol co-loaded nano long-circulating liposome as well as a preparation method and application thereof, and belongs to the technical field of medicament preparation. The nano long-circulating liposome comprises a medicinal active component and a lipid membrane material, wherein the medicinal active component comprises docetaxel and resveratrol; and the lipid membrane material comprises soya bean lecithin, cholesterol and DSPE-PEG2000. It verifies for the first time that a combination of the traditional Chinese medicine resveratrol with anti-tumor activity and the docetaxel has a relatively strong synergistic anti-tumor effect when acting on human prostate cancer cells and human lung cancer cells; meanwhile, the docetaxel and the resveratrol are prepared into the nano long-circulating liposome, the solubility of the nano long-circulating liposome is effectively improved, and meanwhile, the drug permeation and retention effects can be improved; the side effects of the docetaxel are reduced on the basis of enhancing the anti-tumor activity of the docetaxel; and a foundation is laid for development and research of a novel docetaxel nano preparation.

Description

Technical field [0001] The invention belongs to the technical field of medicament preparation, and specifically relates to a nano-long circulating liposome co-loaded with docetaxel-resveratrol, and a preparation method and application thereof. Background technique [0002] Disclosure of the background information is only intended to increase the understanding of the overall background of the present invention, and is not necessarily regarded as an acknowledgement or in any form suggesting that the information constitutes the prior art known to those of ordinary skill in the art. [0003] Docetaxel (DTX) is a taxane anticancer drug obtained by semi-synthesis of the precursor 10-DAB extracted from the needles of Taxus baccata (Europeanyew). It belongs to the inhibition of microtubule depolymerization. Agent. Clinically, DTX is widely used in the treatment of various cancers. The FDA has approved its use in the treatment of ovarian cancer, breast cancer, non-small cell lung cancer an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/127A61P35/00B82Y5/00A61K31/05
CPCA61K9/1277A61K31/05A61K31/337A61P35/00B82Y5/00A61K2300/00
Inventor 张璐
Owner THE SECOND HOSPITAL OF SHANDONG UNIV
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