Thermosensitive liposome and its application

A technology of heat-sensitive liposomes and phospholipids, which is applied in the directions of liposome delivery, medical preparations of non-active ingredients, and drug combinations, can solve problems such as drug leakage, influence of drug-carrying capacity, crystallization, etc. Stability, improving drug-carrying capacity, and the effect of stable properties

Inactive Publication Date: 2012-08-01
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Saturated phospholipids are usually used in the prior art, which has a greater impact on the drug-loading capacity of liposomes. When the drug-loading capacity is slightly higher, stability problems such as drug leakage and crystallization are prone to occur, which limits the use of fat-soluble active agents in liposomes. Applications in plastid preparations

Method used

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  • Thermosensitive liposome and its application
  • Thermosensitive liposome and its application
  • Thermosensitive liposome and its application

Examples

Experimental program
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Effect test

Embodiment 1

[0055] The preparation of embodiment 1 paclitaxel long circulation thermosensitive liposome

[0056] (1) Materials and dosage: (the dosage of 100ml liposome)

[0057]

[0058] (2) Preparation method:

[0059] Weigh various phospholipids and drugs according to the above dosage, dissolve them in chloroform, remove the organic solvent by rotary evaporation at 50-60°C, and obtain a film that is dry and uniformly attached to the bottom of the glass bottle. A solution of multilamellar liposomes was obtained after hydration with lactose-containing phosphate buffer. The polycarbonate membrane is extruded, first through a polycarbonate membrane with a pore diameter of 200nm, and then through a polycarbonate membrane with a pore diameter of 100nm. The measured particle size is 110nm, and the liposome solution is transparent blue opalescent, and has good fluidity.

Embodiment 2

[0060] The encapsulation efficiency measurement of embodiment 2 paclitaxel long circulation thermosensitive liposome

[0061] Take 1 ml of paclitaxel long-circulation thermosensitive liposome prepared in Example 1 in a 1.5 ml EP tube, centrifuge at 8000 r / min for 8 min. Take 0.2ml of the supernatant in a 10ml volumetric flask, and after breaking the membrane with methanol solution to make up the volume, analyze by HPLC to obtain the drug content of paclitaxel loaded in the liposome (C1); Put 0.2ml of liposome sample in a 10ml volumetric flask, and after permeating the membrane with methanol solution to make up the volume, HPLC sample injection analysis was carried out to obtain the total drug content (C2) of paclitaxel in the paclitaxel long-circulation thermosensitive liposome suspension. Encapsulation efficiency (E)=C1 / C2*100%. The results showed that the encapsulation efficiency of paclitaxel long-circulation thermosensitive liposome was 99.2%.

Embodiment 3

[0062] The phase transition temperature measurement of embodiment 3 paclitaxel long circulation thermosensitive liposome

[0063] The phase transition temperature of the paclitaxel long-circulation thermosensitive liposome prepared in Example 1 of the present invention was measured by differential scanning calorimetry (DSC). Dilute the long-circulation thermosensitive liposomes to a phospholipid concentration of about 20 mg / ml, pipette 10 μl into an aluminum dish, and scan in the range of 30-50 °C at a scanning speed of 2 °C / min. Record the phase transition temperature of liposome at about 42.24 ℃ (as figure 1 Middle curve A), the phase transition is obvious and the phase transition temperature range is narrow. By adjusting the ratio of phospholipids, the phase transition temperature can vary between 39-45°C, such as figure 1 In curve B (the content of 100ml liposomes is 7.5g of DPPC, 0.6g of DSPE-PEG2000, 0.6g of DOPC, and 0.3g of MSPC), the phase transition temperature is ...

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Abstract

The invention relates to a thermosensitive liposome, which contains at least one phosphatidylcholine, at least one lysophospholipid, and at least one unsaturated phospholipid. The phase temperature of the liposome is 39.0DEG C-45.0DEG C. The liposome further contains a material having a long circulating characteristic and a fat-soluble active agent. Specifically, the phosphatidylcholine, the lysophospholipid, the unsaturated phospholipid, and the material having a long cycle characteristic are in a weight ratio of 69-94:1-6:1-10:4-15. And all the phospholipids and the fat-soluble active agent are in a weight ratio of 30-120:1-10. The invention also relates to a pharmaceutical composition containing the thermosensitive liposome. The invention additionally relates to application of the thermosensitive liposome and the pharmaceutical composition in preparing drugs treating tumors.

Description

technical field [0001] The present invention relates to a thermosensitive liposome, particularly a thermosensitive liposome comprising a fat-soluble active agent, a pharmaceutical composition comprising the thermosensitive liposome, and the thermosensitive liposome and Use of the pharmaceutical composition. Background technique [0002] In 1978, Yatvin and Weinstein first reported thermosensitive liposomes (Thermosensitive liposomes). Thermosensitive liposomes are divided into two types according to the phase transition temperature and drug release speed: traditional thermosensitive liposome (TTSL), the phase transition temperature is between 43°C and 45°C, and the drug release takes more than 30 minutes ; low temperature sensitive liposome (LTSL), the phase transition temperature is between 39°C and 42°C, and a large amount of drugs can be released within a few seconds of heating. Compared with traditional thermosensitive liposomes, low-temperature thermosensitive liposom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/26A61K47/32A61K47/34A61P35/00A61K47/10
Inventor 梅兴国张慧
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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