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Preparation of norcantharidin targeted liposome and application of freeze-drying preparation of norcantharidin targeted liposome

A technology of methylcantharidin lipid and norcantharidin, which is applied in the preparation of norcantharidin liver-targeted liposomes and its application in freeze-dried preparations, and can solve the problems of large tablet dosage, adverse reactions, and clinical application limitations and other problems, to achieve the effect of simple operation and uniform particle size

Inactive Publication Date: 2018-03-06
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, norcantharidin preparations mainly include tablets and injections. The dosage of tablets is large, and the bioavailability of injections is poor, and it has strong irritation to the urinary system and adverse reactions to the gastrointestinal tract.
Therefore, the clinical application is limited, which affects the anticancer effect

Method used

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  • Preparation of norcantharidin targeted liposome and application of freeze-drying preparation of norcantharidin targeted liposome
  • Preparation of norcantharidin targeted liposome and application of freeze-drying preparation of norcantharidin targeted liposome
  • Preparation of norcantharidin targeted liposome and application of freeze-drying preparation of norcantharidin targeted liposome

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Effect test

Embodiment 1

[0026] The phospholipid material lecithin 60mg, cholesterol 8mg, and stearyl glycyrrhetinate 6mg were dissolved in chloroform, dissolved by ultrasound, and then placed in an eggplant-shaped bottle and rotary steamed at 37°C to form a film. Dissolve 6mg of norcantharidin in 50ml phosphate buffer (pH 7.4), then add it to a thin eggplant-shaped bottle and hydrate for 1 hour. After hydration, the suspension probe will be sonicated (150W, 3min) to obtain fat. The plastid solution has a measured particle size of about 200nm.

Embodiment 2

[0028] The phospholipid material lecithin 60mg, cholesterol 8mg, and stearyl glycyrrhetinate 6mg were dissolved in 150ml ether, and then placed in an eggplant-shaped bottle, and rotary steamed at room temperature to form a film. Add ether to dissolve the membrane, dissolve 6mg of norcantharidin in 50ml phosphate buffer (pH 7.4), add lipid-containing ether, phacoemulsify the probe in an ice water bath, and then rotate the emulsion on a rotary evaporator After 20 minutes, the liposome suspension was obtained, and the probe was sonicated (150W, 3 minutes) to size the liposome solution, and the measured particle size was about 150 nm.

Embodiment 3

[0030] Ethanol injection method (such as figure 1 Shown): Dissolve 6 mg of norcantharidin in phosphate buffer (pH 7.4), place it on a magnetic stirrer and stir at a water bath temperature of 50°C; phospholipid material lecithin 60 mg, cholesterol 8 mg, and stearyl glycyrrhetinate 6mg is dissolved in 5ml ethanol, the lipid-containing ethanol solution is slowly injected into the medicated PBS solution with a syringe, incubated for 0.5h, and then rotary steamed to remove residual ethanol to obtain liposome suspension, and the probe is ultrasonically adjusted The liposome solution is obtained from the granule, and the measured particle size is about 90nm.

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Abstract

The invention belongs to the technical field of medicine. The invention discloses a norcantharidin liver-targeting liposome, a preparation method thereof and the application of a freeze-dried preparation. The norcantharidin liver-targeting liposome of the present invention is connected with a glycyrrhetic acid derivative on the surface of the liposome, which can be combined with the glycyrrhetic acid receptor on the surface of liver tumor cells and undergo endocytosis, thereby producing a tumor-suppressing effect. ; Norcantharidin is encapsulated in liposomes, which has better drug bioavailability and enhanced curative effect. The norcantharidin liposome freeze-dried preparation prepared by the invention has good stability, safety and reliability, is easy to store, and is beneficial to industrialized production.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation of norcantharidin liver-targeted liposomes and the application of freeze-dried preparations. Background technique [0002] Liver cancer is the second highest mortality rate in the world and one of the malignant tumors most threatening to human life. Among them, hepatocellular carcinoma (HCC) is a primary liver cancer with high mortality. Although the treatment of HCC has improved, the overall morbidity and mortality have not improved significantly. Chemotherapy is the second-line treatment or the next-line treatment for HCC in some cases. However, chemotherapy is limited by many factors, including: non-specific cytotoxicity, drug tolerance, tumor recurrence, limited solubility of chemotherapy reagents, and drug stability in plasma. Therefore, there is an urgent need to develop safer and more effective HCC treatment methods or drugs. [0003] Liposomes are ult...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/28A61K47/24A61K47/26A61K31/34A61P35/00
CPCA61K9/1277A61K31/34A61K47/24A61K47/26A61K47/28
Inventor 吴卫朱静刘庚贵唐欣
Owner GUILIN MEDICAL UNIVERSITY
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