A kind of hydration icariin nanoparticle and its preparation method and application

A hydrated icariin and nanoparticle technology, applied in the field of medicine, can solve the problems of difficulty in administration, limitation of clinical application of HICT in vivo research, and low bioavailability

Active Publication Date: 2021-03-19
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

[0005] However, like many flavonoids, HICT is poorly water soluble, making it difficult to administer due to low bioavailability
The administration method in the existing literature is mainly HICT / DMSO solution, but the drug solution using DMSO as solvent can be used in animal experiments, but cannot be used orally or injected in humans and clinically; even in the case of animal experiments, Since the HICT / DMSO solution enters the digestive tract and is diluted by digestive juice, intraperitoneal injection by peritoneal fluid, or intravenous injection by blood, drug crystals may be precipitated, and the experimental results obtained are only of reference value, which greatly limits HICT. In vivo studies and further clinical applications

Method used

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  • A kind of hydration icariin nanoparticle and its preparation method and application
  • A kind of hydration icariin nanoparticle and its preparation method and application
  • A kind of hydration icariin nanoparticle and its preparation method and application

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preparation example Construction

[0043] The present invention provides the preparation method of the hydrated epimeditin nano-particle described in above-mentioned technical scheme, comprises the following steps:

[0044] mixing icariin hydrate, a stabilizer, an organic solvent and water to obtain a precursor solution;

[0045] The organic solvent in the precursor solution is removed to obtain hydrated icariin nanoparticles.

[0046] The invention mixes hydration icariin, stabilizer, organic solvent and water to obtain a precursor solution. In the present invention, the concentration of icariin hydrate in the precursor solution is preferably 0.01-100 mg / mL, more preferably 0.1-50 mg / mL, and most preferably 1-30 mg / mL. In the present invention, the organic solvent is preferably the first organic solvent, or a mixture of the first organic solvent and the second organic solvent; the first organic solvent preferably includes methanol, ethanol, acetone, dimethylsulfoxide and One or more of N,N-dimethylformamide,...

Embodiment 1

[0063] Dissolve 20mg HICT and 20mg vitamin E-mPEG1000 succinate in 1mL DMSO as the organic phase; add the organic phase dropwise to 10mL water under 1000r / min magnetic stirring, centrifuge at 13000r / min for 20min, and use 10mL deionized water for precipitation Ultrasonic dispersion for 20 min, 2000 bar homogenization 10 times, to obtain hydrated icariin nanoparticles (HICT-NPs).

[0064] 1. Characterize the HICT-NPs, as follows:

[0065] (1) Particle size, polydispersity index (PDI), Zeta potential investigation

[0066] A Zetasizernano ZS particle size analyzer was used to measure the particle size distribution and Zeta potential of the HICT-NPs at 25 °C through the principle of dynamic light scattering (DLS), and each sample was measured 3 times in parallel.

[0067] figure 1 It is the particle size distribution diagram of the HICT-NPs (n=3, mean±SD), the results show that the average particle size is (201.7±1.3) nm, and the PDI is 0.17±0.07, indicating that the particle s...

Embodiment 2

[0158] A series of HICT-NPs were prepared under different conditions, and the particle size, PDI and Zeta potential were investigated, as follows:

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Abstract

The invention relates to the technical field of medicine, in particular to hydrated icariin nanoparticles and a preparation method and application thereof. The hydrated icariin nanoparticles comprisehydrated icariin and a stabilizer. According to the hydrated icariin nanoparticles and the preparation method and application thereof, the stabilizer is adopted to enable water-insoluble hydrated icariin drugs to be uniformly dispersed in a water phase in the form of nano-sized particles, so that the problems of insolubility and difficult administration are solved, and the bioavailability of the hydrated icariin is improved; based on the hydrated icariin nanoparticles, the water-insoluble hydrated icariin drugs can be further prepared into various clinically common dosage forms through a modern preparation process so as to meet various clinical medication requirements; and meanwhile, the stabilizer can improve the biological activity of hydrated icariin and further improve the bioavailability of the hydrated icariin.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a hydrated icariin nanoparticle and a preparation method and application thereof. Background technique [0002] Hydrated Icaritin (Hydrous Icaritin, HICT, Formula A), Molecular Formula C 21 h 22 o 7 , with a molecular weight of 386.4, is a flavonoid compound isolated from Epimedium, similar in chemical structure to dehydrated icariin (formula B), and the specific structure is as follows: [0003] [0004] However, unlike a large number of literatures reporting on the activity of dehydroicariin, so far only a few literatures have studied the activity of HICT. It has been reported that injecting 10 mg / kg of HICT in dimethyl sulfoxide (DMSO) solution every other day around the tumor can significantly inhibit the growth of renal carcinoma (Li, S., et al., Icaritin inhibits JAK / STAT3 signaling and growth of renal cell carcinoma.PLoS One,2013,8.); Intraperitoneal injection of 3...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/352A61K47/10A61K47/34A61K47/24A61K47/42A61P9/00A61P25/00A61P29/00A61P35/00A61P39/06
CPCA61K9/146A61K31/352A61P9/00A61P25/00A61P29/00A61P35/00A61P39/06
Inventor 王向涛李怡静王一安敖惠李好文韩美华郭一飞
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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