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Preposed cavitation type marihuana fat-soluble active matter soluble microneedle as well as preparation method and application thereof

A technology of cannabis resin and active substances, which is applied in the field of drug deep penetration, can solve the problem of limited drug dosage, achieve the effects of reducing the dosage, improving the microenvironment, and increasing the transdermal permeability coefficient

Pending Publication Date: 2022-03-25
中纳科(南京)生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But even so, many drugs avoid the blockage of the stratum corneum by physical means, and due to their lack of ability to diffuse and penetrate inward, they will still be trapped in a large amount in the epidermis, and the amount of drug that actually enters the target site is very limited

Method used

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  • Preposed cavitation type marihuana fat-soluble active matter soluble microneedle as well as preparation method and application thereof
  • Preposed cavitation type marihuana fat-soluble active matter soluble microneedle as well as preparation method and application thereof
  • Preposed cavitation type marihuana fat-soluble active matter soluble microneedle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] h 2 - Preparation and characterization of Bub / CBD@PD1 / SD-MNs

[0050] Accurately weigh cannabidiol (CBD) and polyvinylpyrrolidone-K30 (PVP-K30) according to a mass ratio of 1:1, place them in a round bottom flask, add absolute ethanol, stir until the system becomes a clear liquid, and spin evaporate under reduced pressure In addition to the organic solvent, quickly put it in a refrigerator at -20°C for 24 hours to freeze and solidify, then take out the dried product, grind it, and pass it through a 120-mesh sieve to obtain a cannabidiol solid dispersion (CBD-SD).

[0051] Weigh the magnesium particles and disperse them in the isopropanol solution. The mass concentration of the magnesium particles in the mixed solution is 1wt%. Add the mixed solution dropwise on the surface of the conical PDMS mold, centrifuge at 4500rpm for 30min in an ultra-high speed centrifuge, and place in a vacuum Dry in a drying oven at 50°C for 1 h.

[0052] According to the mass ratio of 5:1, ...

Embodiment 2

[0057] h 2 - Preparation and characterization of Bub / CBDA@PD-L1 / SD-MNs

[0058] Accurately weigh cannabidiolic acid (CBDA) and PVP-K30 according to a mass ratio of 1:5, place them in a round bottom flask, add absolute ethanol, stir until the system becomes a clear liquid, remove the organic solvent by rotary evaporation under reduced pressure, and place quickly After freezing and solidifying in a refrigerator at -20°C for 24 hours, take out the dried product, grind it, and pass it through a 120-mesh sieve to obtain CBDA-SD.

[0059] Weigh the calcium particles and disperse them in chloroform. The concentration of calcium particles in the mixed solution is 5wt%. Add the mixed solution dropwise on the surface of the conical PDMS mold, centrifuge at 3000rpm for 20min in an ultra-high speed centrifuge, and place in a vacuum oven for 40 ℃ dry 2h.

[0060] Accurately weigh hyaluronic acid + PVP-K30 mixed matrix (3 / 1, w / w) and dissolve it with the above CBDA-SD in an aqueous soluti...

Embodiment 3

[0065] o 2 - Preparation and characterization of Bub / CBDA@ICG / SD-MNs

[0066] Accurately weigh cannabidiolic acid (CBDA) and PVP-K30 according to a mass ratio of 1:10, place them in a round bottom flask, add absolute ethanol, stir until the system becomes a clear liquid, remove the organic solvent by rotary evaporation under reduced pressure, and place quickly After freezing and solidifying in a refrigerator at -20°C for 24 hours, take out the dried product, grind it, and pass it through a 120-mesh sieve to obtain CBDA-SD.

[0067] Weigh cerium dioxide particles and disperse them in an aqueous solution containing 0.5wt% Tween 80. The concentration of ceria particles in the mixed solution is 1wt%. Add the mixed solution dropwise on the surface of a conical PDMS mold, and place in an ultrahigh-speed centrifuge at 3000rpm Centrifuge at a high speed for 20 minutes, and dry in a vacuum oven at 40°C for 2 hours.

[0068] Accurately weigh hyaluronic acid + PVP mixed matrix (3 / 1, w / ...

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Abstract

The invention relates to a preposed cavitation type hemp fat-soluble active matter soluble microneedle, which comprises a backing layer and a microneedle array fixed on the backing layer, and one of active metal particles, bicarbonate, bicarbonate, cerium dioxide particles or cerium-zirconium composite oxide particles is embedded in the tip part of the microneedle; and the needle body is filled with a soluble microneedle matrix material containing a cannabis fat-soluble active matter solid dispersion. According to the preposed cavitation type cannabis sativa active ingredient microneedle disclosed by the invention, by utilizing preposed bubbles, the delivery resistance of an embedded medicine to a tumor deep layer is greatly reduced, and the transdermal permeability coefficient is greatly improved; generated hydrogen / oxygen / carbon dioxide and the like can remarkably improve the tumor immunosuppression microenvironment and cooperate with other embedded anti-tumor drugs to improve the treatment efficiency; and the required administration dosage is greatly reduced, so that the potential toxicity is reduced, and the comprehensive treatment efficiency on various superficial skin tumors is obviously improved.

Description

technical field [0001] The invention relates to a preparation method of a pre-bubble-type marijuana fat-soluble active substance soluble microneedle drug delivery system and its application in the deep penetration of drugs in the treatment of superficial tumors. Background technique [0002] Cannabinoids are the main constituents of the Moraceae plant cannabis to exert pharmacological activity. The cannabinoid compound CBD (cannabidiol) that is currently isolated and identified. Among them, CBD is the second largest active ingredient of marijuana, which belongs to the category of fat-soluble non-psychoactive cannabinoids, and its oral bioavailability is about 6%. Widely distributed in tissues and body fluids, it can bind to cannabinoid receptor 1 (CB1R), cannabinoid receptor 2 (CB2R), transient receptor potential vanilloid 1 (TRPV1), G protein-coupled receptor-55 (GPR-55 ), and peroxisome proliferator-activated receptor-γ (PPAR-γ) and other multi-target interactions, can be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K31/05A61K33/24A61K36/60A61K9/00A61K47/02A61K47/32A61K47/36A61K47/42A61M37/00A61P35/00
CPCA61K41/0057A61K9/0021A61K36/60A61K31/05A61K33/24A61K47/36A61K47/42A61K47/32A61K47/02A61M37/0015A61P35/00A61M2037/0053A61M2037/0046A61K2300/00
Inventor 瞿鼎陆缘施嘉晨
Owner 中纳科(南京)生物科技有限公司
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