Docetaxel compound liposome, preparation method thereof and application of liposome

A technology of compound liposome and docetaxel, which is applied in the field of compound liposome of docetaxel and its preparation, to achieve the effect of reducing the clearance rate, enhancing the anti-cancer effect, and improving the tumor inhibition rate

CN110251464AActive Publication Date: 2019-09-20南京菲力康医药科技有限公司
1 Cites 5 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2019-09-20

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention belongs to the field of medicinal preparations, and particularly relates to a docetaxel compound liposome, a preparation method thereof and an application of the liposome. The docetaxel compound liposome comprises docetaxel, pentacyclic triterpene compounds, phospholipid and cholesterol, the weight ratio of the docetaxel to the pentacyclic triterpene compounds is 1:(1-200), and preferably, the pentacyclic triterpene compounds are ursolic acid. Preferably, the preparation method of the docetaxel compound liposome is an ethanol injection method. The docetaxel compound liposome overcomes a lyophobic shortcoming of the liposome, anti-cancer effect can be enhanced through synergistic effect, and toxic and side effects of the docetaxel are relieved.
Need to check novelty before this filing date? Find Prior Art

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.