Thermosensitive liposome preparation of vinblastine drugs and preparation method thereof

The technology of liposome preparation and vinblastine, which is applied in the directions of liposome delivery, pharmaceutical formulation, and drug combination, can solve the problems of not significantly improving the curative effect, and achieves good targeting, high encapsulation rate, and not easy to leak. Effect

Inactive Publication Date: 2016-05-11
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

However, compared with the previous formulations, the liposomes prepared by it did not significantly improve the curative effect.

Method used

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  • Thermosensitive liposome preparation of vinblastine drugs and preparation method thereof
  • Thermosensitive liposome preparation of vinblastine drugs and preparation method thereof
  • Thermosensitive liposome preparation of vinblastine drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of vinorelbine long-circulation thermosensitive liposome formulation

[0043] (1) Preparation of blank liposomes

[0044] Medicines and reagents needed: dipalmitoylphosphatidylcholine (DPPC), DSPE-mPEG2000, monostearylphosphorylcholine (MSPC), citric acid, trisodium citrate, sodium carbonate, double distilled water.

[0045] Table 1

[0046] Phosphate ester

DPPC

DSPE-mPEG2000

MSPC

Mass (g)

8.9

0.8

0.3

[0047] Weigh various phospholipids (the amount used to prepare 100ml of blank liposomes) according to Table 1, dissolve them in 80ml of chloroform, and remove organic solvents by rotary evaporation at 50-60°C to obtain a dry and uniform film attached to the bottom of the glass bottle. It was hydrated with 100ml, 0.2M, pH4 citrate buffer to obtain a multilamellar liposome solution. The polycarbonate membrane was extruded, first through the polycarbonate membrane with a pore size of 200 nm, and then through the polycarbonate membrane with a pore si...

Embodiment 2

[0049] Example 2 Preparation of Vinorelbine Long-Circulation Thermosensitive Liposome

[0050] (1) Preparation of blank liposomes

[0051] Same as Example 1.

[0052] (2) Preparation of drug-loaded liposomes by pH gradient method: Weigh 0.3g of vinorelbine and dissolve it in 100ml, 0.2M, pH4 citrate buffer solution to prepare a 3mg / ml drug solution. Take 20ml of the drug solution and add it to 20ml of blank liposome solution (it can be considered that the dosage of the drug is about 0.06g), add sodium carbonate solution at 25°C to adjust the pH of the external phase to 7.45, and load the drug for 60 minutes. Add sucrose (10%), a cryoprotectant, and place in a refrigerator at -20°C for cryopreservation.

Embodiment 3

[0053] Example 3 Preparation of Vinorelbine Long-Circulation Thermosensitive Liposome

[0054] (1) Preparation of blank liposomes

[0055] Medicines and reagents needed: dipalmitoylphosphatidylcholine (DPPC), DSPE-mPEG2000, distearoylphosphatidylglycerol (DSPG), tartaric acid, sodium tartrate, sodium carbonate, double distilled water, the specific dosage is shown in Table 2.

[0056] Table 2

[0057] Phosphate ester

DPPC

DSPE-mPEG2000

DSPG

Mass (g)

7.7

2

0.3

[0058] Weigh various phospholipids (the amount used to prepare 100ml blank liposomes) according to Table 2, and dissolve them in 80ml chloroform and methanol solution (1∶1) to form a clear and transparent solution. Rotary evaporation at 60°C to remove organic solvents to obtain a dry, uniform Film attached to the bottom of the glass bottle. Hydrate with (100ml, 0.2M, pH4) tartrate buffer to obtain a multilamellar liposome solution. Extrusion through a polycarbonate membrane, first through a polycarbonate membrane wit...

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Abstract

The invention relates to a temperature-sensitive liposome preparation of vinblastine medicaments and a preparation method thereof. The temperature-sensitive liposome preparation includes vinblastine medicament, temperature-sensitive phosphatide and optional long circulating material. A molar ratio of temperature-sensitive phosphatide to optional long circulating material is 70:30-92:8; and a weight ratio of vinblastine medicament to blank liposome is 1:10-1:50. The invention employs a pH gradient active drug loading method to reach an entrapment rate of 90.0-99%. The liposome preparation with heat sensitivity of the present invention can make the liposome to passively target a tumour position and release a lot of medicament simultaneously, so as to improve curative effect and reduce toxic and side effects on the whole body.

Description

Technical field [0001] The invention relates to a liposome preparation, in particular to a heat-sensitive liposome preparation containing vinblastine drugs, and a preparation method thereof. Background technique [0002] Vinblastine anti-tumor drugs are a class of alkaloids with anti-cancer activity isolated from the Apocynaceae plant Catharanthus roseus. It is a cell cycle-specific anti-tumor drug. Its mechanism of action is to block the formation of microtubules in the process of mitosis and stop cell division in the middle of mitosis. It is mainly used for the treatment of malignant lymphoma, choriocarcinoma, and advanced esophagus. Cancer, advanced non-small cell lung cancer and breast cancer. At present, my country's marketed dosage forms include intravenous injection and freeze-dried powder injection, but after intravenous injection of the drug, the toxic and side effects are relatively large, and symptoms such as neurotoxicity and blood toxicity, phlebitis, and local skin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/475A61P35/00
Inventor 梅兴国张慧
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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