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Lycorine nanoparticle as well as preparation method and application thereof

A nanoparticle and lycorine hydrochloride technology, which is applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of high quality requirements, high production risk, and high price, and achieve high mechanical strength, suitable mechanical properties, and stability good sex effect

Pending Publication Date: 2020-09-18
HUBEI UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] For a long time, lycorine has been used as an anticancer drug and is often made into injections. Although injections have the characteristics of fast onset of action, they have poor compliance, are expensive, have high quality requirements, and have high production risks.

Method used

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  • Lycorine nanoparticle as well as preparation method and application thereof
  • Lycorine nanoparticle as well as preparation method and application thereof
  • Lycorine nanoparticle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Preparation of Lycorine Hydrochloride Nanoparticles:

[0058] (1) Purification of DL lactide

[0059] Take about 4 g of lactide powder, add 30 mL of ethyl acetate solution to the beaker, pour the obtained lactide into the beaker, stir to dissolve in a water bath at a temperature of 95 ° C, and then cool it at room temperature, After the temperature dropped to room temperature, it was stored in a refrigerator at 4°C, filtered after 2 hours, and dried in a vacuum drying box for 36 hours to obtain the crystal powder of lactide. The above experiment was repeated twice.

[0060] (2) Preparation of racemic polylactic acid

[0061] Weigh an appropriate amount of recrystallized lactide as a raw material, stannous octoate as a catalyst, and an appropriate amount of water as an initiator. The oil bath was heated to 120°C, and the reaction was carried out for 3 hours under stirring. Dichloromethane was added to the product obtained by the reaction to speed up the dissolution, an...

Embodiment 2

[0068] The preparation method is the same as in Example 1, and the difference is:

[0069] In (i) of step (3), the consumption of racemic polylactic acid is 15mg, and the consumption of lycorine hydrochloride is 6mg; ultrasonic power is 200w;

[0070] The concentration of SDS in (ii) of step (3) becomes 2%; ultrasonic power is 40W;

Embodiment 3

[0072] The preparation method is the same as in Example 1, and the difference is:

[0073] In (i) of step (3), the consumption of racemic polylactic acid is 30mg, the consumption of lycorine hydrochloride is 12mg, and the ultrasonic power is 220w;

[0074] The concentration of SDS in (ii) of step (3) was changed to 3%; the ultrasonic power was 50W.

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Abstract

The invention provides a lycorine nanoparticle as well as a preparation method and application thereof. The nanoparticle is prepared by dissolving a drug in or packaging the drug with a high polymer carrier material containing an emulsifying agent, wherein the drug is lycorine; and the carrier material is racemic polylactic acid. Proportions are as follows: the volume ratio of an oil phase to an inner water phase is (2 to 1)-(5 to 1); and the mass ratio of the carrier to the drug is (2.5 to 1)-(5 to 1). The prepared nanoparticle has a clear blue appearance, a nanoparticle solution has the specific characteristic that the appearance presents blue opalescence, the prepared nanoparticle is nano-scale, the average particle size is 96.3+ / -5.1nm, a PDI (polydispersion index) is 0.141+ / -0.020 (the particle sizes of the particles are more uniformly and stably dispersed when the PDI value is lower), and a centrifugal accelerated experiment result shows that conditions of precipitation and demulsification do not exist; after the nanoparticles are released for 24h, the accumulated release rate of the nanoparticles reach up to 98.99%, and a fitting Ritger-Pappas model (R=0.9327) is best matched with a releasing mechanism. An optimized prescription and process of the nanoparticle meet the demands, and an in-vitro slow-release effect of the particle is obvious.

Description

technical field [0001] The content of the invention belongs to the technical field of medicine. The invention relates to a lycorine nanoparticle and its preparation method and properties. The nanoparticle is prepared by emulsification solvent evaporation method, which can be used for inducing tumor cell apoptosis, inhibiting tumor angiogenesis, inhibiting and blocking cell cycle and mediating cell autophagy and other aspects, and has targeted, reducing the toxic and side effects of tumor treatment. Background technique [0002] The bulbs of the Amaryllidaceae plant Lycoris are extracted to obtain the traditional Chinese medicine Lycoris. This traditional medicinal plant Lycoris has a long history of clinical application. "Graphic Classics of Materia Medica" was the first to discover its pharmacological effects, mainly used for "applying swollen poison". Lycorine was first extracted and discovered by Japanese Morishima Kutai after separating the bulbs of the Amaryllidaceae...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/4745A61P35/00B82Y5/00B82Y40/00
CPCA61K31/4745A61K47/6937A61P35/00B82Y5/00B82Y40/00Y02A50/30
Inventor 罗斌华何流王慧丽
Owner HUBEI UNIV OF SCI & TECH
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