A compound liposome of docetaxel and its preparation method and application

A technology of compound liposome and docetaxel, which is applied in the field of compound liposome of docetaxel and its preparation, achieves the effects of high encapsulation efficiency, reduction of toxic and side effects, and low dispersion coefficient

CN110251464BActive Publication Date: 2021-09-17南京菲力康医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2021-09-17

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Abstract

The invention belongs to the field of pharmaceutical preparations, in particular to a compound liposome of docetaxel and its preparation method and application. The compound liposome of docetaxel contains docetaxel, pentacyclic triterpenoids, phospholipids and cholesterol, wherein the weight ratio of docetaxel and pentacyclic triterpenoids is 1: (1-200), five Cyclic triterpenoids are preferably ursolic acid. The preparation method of the compound liposome of docetaxel is preferably an ethanol injection method. The docetaxel compound liposome of the present invention not only overcomes its hydrophobic defect, but also can enhance the anticancer effect through a synergistic effect, and reduce the toxic and side effects of docetaxel.
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Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a compound liposome of docetaxel and its preparation method and application. Background technique

[0002] Docetaxel (DTX) is a paclitaxel anti-microtubule chemotherapeutic drug widely used in the treatment of non-small cell lung cancer, breast cancer and prostate cancer. However, docetaxel has poor water solubility, which greatly limits its wide application. Commercially available injections use Tween-80 as a solubilizer and dissolve in ethanol, which can cause serious adverse reactions, including allergy, hemolysis, and neurotoxicity. Over the past few years, extensive research has been devoted to the development of novel nanoformulations of docetaxel to overcome its poor solubility, improve its antitumor effect, and reduce toxicity.

[0003] Ursolic acid (UA) is a pentacyclic triterpenoid compound (as shown in formula 1) from various medicinal plants and fruits. I...

Examples

Embodiment 1-4

[0044] Weigh lecithin 150 mg, cholesterol 30 mg, ursolic acid 30 mg, respectively weigh docetaxel 6 mg according to the type of liposomes prepared (Example 1, DTX and UA mass ratio is 1:5 compound lipid Body DTX 1 / UA 5 -LPs), 1.5 mg (Example 2, the compound liposome DTX with a mass ratio of DTX to UA of 1:20 1 / UA 20 -LPs), 0.6 mg (Example 3, the compound liposome DTX with a mass ratio of DTX to UA of 1:50 1 / UA 50 -LPs), 0.3 mg (Example 4, the compound liposome DTX with a mass ratio of DTX and UA of 1:100 1 / UA 100 -LPs). Dissolve lipids (lecithin and cholesterol) and drugs (docetaxel and ursolic acid) in ethanol and vortex to dissolve completely; slowly drop them into rapidly stirring PBS (600 r / min) , when the ethanol is completely volatilized, a uniform light blue liposome suspension will be obtained, which should be placed at 4°C overnight.