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Corosolic acid liposome as well as preparation method and application thereof

A technology of corosolic acid and liposome, which is applied in the field of medical technology and nanomedicine, can solve the problems of poor water solubility of corosolic acid, short circulation half-life, and limited clinical application, and achieve good stability and high drug loading capacity. High, stable and regulating fluidity effect

Active Publication Date: 2019-12-10
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention can solve the problems of limited clinical application of corosolic acid, such as poor water solubility, low bioavailability and short circulation half-life in vivo. In particular, the corosolic acid liposome CALP can be used as a carrier of antitumor drugs, Make targeted anti-tumor CALP, realize the combined targeted delivery and synergistic treatment of corosolic acid CA (corosolic acid, CA,) and anti-tumor drugs, and then expand the application of corosolic acid liposome CALP in tumor-targeted therapy Applications in the field

Method used

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  • Corosolic acid liposome as well as preparation method and application thereof
  • Corosolic acid liposome as well as preparation method and application thereof
  • Corosolic acid liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1 film dispersion method prepares CALP

[0046] Weigh 100mg HSPC, 33.3mg DSPE-MPEG2000, 39mg corosolic acid, dissolve in chloroform / methanol (4 / 1, v / v) to obtain a clear solution; rotary evaporate in a water bath at 40°C, remove the organic solvent, and obtain The membrane was added with physiological saline, hydrated with rotation at 60°C for 2 hours, ultrasonicated at 200W for 20 minutes in an ice-water bath, and eluted through a Sephadex column to obtain a purified CALP liposome suspension. The particle size of the liposome is 90-95nm, and the CA content is 23.2% (w / w).

Embodiment 2

[0047] Embodiment 2 injection method prepares CALP

[0048] Weigh 12mg DSPC, 4mg DSPE-MPEG2000, 4.8mg corosolic acid, dissolve in ethanol, inject the ethanol solution into 60°C physiological saline slowly at a uniform speed, stir continuously at 1000rpm, and ultrasonicate at 200W for 20 minutes in an ice-water bath. Centrifugal purification at 10000rpm to obtain CALP liposome suspension. Its particle diameter and CA content of the CALP prepared by this method are similar to those in Example 1.

Embodiment 3

[0049] Embodiment 3 freeze-thaw method prepares CALP

[0050] Weigh 15mg of DPPC, 4mg of DSPE-MPEG2000, 4.8mg of corosolic acid, dissolve in chloroform / methanol (4 / 1, v / v), rotatively evaporate in a water bath at 40°C, remove the organic solvent to form a film, add physiological saline, Rotating hydration at 40°C for 2 hours to obtain a crude liposome suspension. Place the suspension in a refrigerator at -80°C, take it out after 12 hours and let it melt at room temperature, then place it in a refrigerator at -80°C, and place it at room temperature after 12 hours, repeat this operation 10 times, and then squeeze Press through a 100nm polycarbonate membrane to obtain a CALP liposome suspension. Its particle diameter and CA content of the CALP prepared by this method are similar to those in Example 1.

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Abstract

The invention belongs to the technical field of medical technology and nano-medicine and relates to a corosolic acid liposome as well as a preparation method and application thereof. For the liposome,corosolic acid is used for replacing cholesterol as a liposome membrane component and is combined with phospholipid to prepare the corosolic acid liposome with high drug loading capacity and good stability, and the liposome has dual effects of a liposome membrane material and a therapeutic drug at the same time. The liposome can solve the problems of poor absorption, low bioavailability, difficulty in effective delivery and the like of the corosolic acid and is capable of obviously improving the curative effects of reducing sugar and resisting inflammation and tumors of the corosolic acid. The liposome can load various antitumor drugs for antitumor therapy according to the needs so as to realize multidrug targeting co-delivery, efficacy enhancement and toxicity reduction, avoids multidrugresistance and has the synergistic anti-tumor effect, wherein the anticancer effect and the safety of prepared doxorubicin hydrochloride-corosolic acid liposome are obviously superior to the anticancer effect and the safety of doxorubicin hydrochloride lipidosome injection on the market.

Description

technical field [0001] The invention belongs to the fields of medical technology and nanomedicine technology, and in particular relates to a corosolic acid liposome and its preparation method and application. [0002] technical background [0003] The prior art discloses that corosolic acid (CA), namely 2α-hydroxyursolic acid, is a triterpenoid compound present in plants such as Lagerstroemia indica, loquat, and nasturtium. Studies have found that CA has the functions of lowering blood sugar, losing weight, anti-tumor, anti-inflammation, anti-virus and anti-cardiovascular disease, among which the activities of lowering blood sugar, anti-inflammation and anti-tumor are the most in-depth studies; CA has a physiological effect similar to insulin, and has been Known as "Plant Insulin", as a new drug for the prevention and treatment of obesity and type 2 diabetes, it has entered the Phase III clinical pharmacodynamic evaluation of the US FDA; CA has a significant inhibitory effect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K31/56A61K31/704A61K31/513A61K31/337A61K31/4745A61P35/00A61P3/10A61P3/04A61P9/00A61P29/00
CPCA61K9/1277A61K47/24A61K47/28A61K31/56A61K31/704A61K31/513A61K31/337A61K31/4745A61P35/00A61P3/10A61P3/04A61P9/00A61P29/00A61K2300/00
Inventor 姜嫣嫣李绪乾
Owner FUDAN UNIV
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