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Paclitaxel pH-sensitive long-circulation liposome and preparation method thereof

A paclitaxel and liposome technology, which is applied in the field of medicine, can solve the problems of encapsulated drug leakage, limited targeting function, poor liposome stability, etc., achieve long action time, prolong circulation time, and improve targeting Effect

Inactive Publication Date: 2017-01-11
SHANGHAI NEW ASIA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, it has been found that the poor stability of liposomes has become a major problem in its application. After liposomes enter the human body, due to various factors such as blood proteins, opsonins, and antibodies in the blood, liposomes rupture and contain Sealed drug leaks quickly and is quickly recognized and absorbed by the reticuloendothelial system, limiting its targeting function

Method used

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  • Paclitaxel pH-sensitive long-circulation liposome and preparation method thereof
  • Paclitaxel pH-sensitive long-circulation liposome and preparation method thereof
  • Paclitaxel pH-sensitive long-circulation liposome and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] paclitaxel 0.5g Half Cholesterol Succinate for Injection 2.8g Dioleoylethanolamine 4.2g PEG2000-DSPE 0.2g tartaric acid 12g sodium tartrate 27g

[0039] Dissolve paclitaxel, half-ester cholesterol succinate for injection, dioleoylethanolamine, PEG2000-DSPE in 95% ethanol (also methanol, chloroform, dichloromethane, etc.) , D solution.

[0040] Pour A into a three-necked bottle; under stirring, add B to A at a constant speed through a glass dropping tube (the speed should be the maximum speed at which the mixed solution can quickly become clear when added.) Mix for about 1 min after complete addition. Add C into the three-necked flask, and mix for about 1 min after complete addition. Slowly add solutions C and D in sequence, and after complete addition, adjust the pH to 5.4 with 1.25M HCl solution (finally keep the solution clear). The reaction solution was added to a rotary evaporator in a water bath, and the rotation speed...

Embodiment 2

[0043] paclitaxel 0.5g Cholesterol for Injection 0.8g Dioleoylethanolamine 4.2g PEG2000-DSPE 0.2g tartaric acid 12g sodium tartrate 27g

[0044]Dissolve the prescribed amount of paclitaxel, cholesterol for injection, dioleoylethanolamine, and PEG2000-DSPE in an organic solvent to form A, B, C, and D solutions respectively. Pour A into a three-necked bottle; under stirring, add B to A at a constant speed through a glass dropping tube (the speed should be the maximum speed at which the mixed solution can quickly become clear when added.) Mix for about 1 min after complete addition. Add C into the three-necked flask, and mix for about 1 min after complete addition. A 1.25M HCl solution was added slowly (to keep the solution clear eventually) to a pH of 5.4. Mix until fully incorporated. The reaction solution was added to a rotary evaporator in a water bath, and the rotation speed was controlled to conduct rotary evaporation.

[0045...

Embodiment 3

[0047] paclitaxel 1.4g Cholesterol for Injection 4.8g dipalmitoyl phosphate 2.5g PEG1000-DLPC 0.1g citrate buffer 39.8g

[0048] Dissolve the prescribed amount of paclitaxel, cholesterol for injection, dipalmitoyl phosphate, and PEG1000-DLPC in organic solvents to form A, B, C, and D solutions respectively. Pour A into a three-necked bottle; under stirring, add B to A at a constant speed through a glass dropping tube (the speed should be the maximum speed at which the mixed solution can quickly become clear when added.) Mix for about 1 min after complete addition. Add C into the three-necked flask, and mix for about 1 min after complete addition. A 1.25M HCl solution was added slowly (to keep the solution clear eventually) to pH 6. Mix until fully incorporated. The reaction solution was added to a rotary evaporator in a water bath, and the rotation speed was controlled to conduct rotary evaporation.

[0049] Dissolve the prescribed amo...

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Abstract

The invention provides a paclitaxel pH-sensitive long-circulation liposome. The paclitaxel pH-sensitive long-circulation liposome is characterized by being prepared from the following matters in percentages by mass: 0.5-3% of paclitaxel, 1-10% of hemisuccinate cholesterol, 5-15% of a pH-sensitive film material, 0.1-1% of a hydrophilic material and 75-90% of a hydration medium material. By the liposome provided by the invention, the shortcoming that the paclitaxel is not water-soluble is overcome. Compared with an existing preparation, the paclitaxel pH-sensitive long-circulation liposome has the characteristics that toxic and side effects are reduced, due to long acting time of the liposome, drug administration time is prolonged, compliance of a patient is increased, meanwhile, targeting ability of the paclitaxel as a chemotherapy drug is improved, and the anti-tumor effect is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pH-sensitive long-circulating liposome of the antineoplastic drug paclitaxel and a preparation method thereof. Background technique [0002] Paclitaxel is a complex diterpene compound, which achieves anti-tumor effect by inhibiting microtubules. It is an excellent broad-spectrum anti-tumor drug. Paclitaxel can produce side effects such as myelosuppression, peripheral neurotoxicity, muscle / joint pain, cardiac arrhythmia, and gastrointestinal toxicity, and its dose-limiting toxicity is neutropenia. Due to the poor solubility of paclitaxel in water, the commercially available formulations use Cremophor EL and ethanol as solvents. Cremophor EL can cause severe allergic reactions, and the incidence of such adverse reactions is still about 41% even with pretreatment with corticosteroids and antihistamines. And the use of Cremophor El makes paclitaxel metabolize nonline...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/10A61K47/28A61K47/12A61K47/18A61K31/337A61P35/00
CPCA61K9/127A61K31/337A61K47/10A61K47/12A61K47/18A61K47/24A61K47/28
Inventor 刘传荣
Owner SHANGHAI NEW ASIA PHARMA
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