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Paclitaxel nano micelle and application thereof

A nano-micelle and paclitaxel technology, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem that paclitaxel is difficult to cross the gastrointestinal barrier and reduce the drug concentration of tumor cells , There are no problems such as paclitaxel oral dosage form, etc., to achieve the effect of overcoming multidrug resistance, avoiding allergic reactions, and obvious antitumor activity

Inactive Publication Date: 2012-11-14
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the polyoxyethylene castor oil in the preparation can cause serious side effects in patients, such as allergic reactions, neurotoxicity and nephrotoxicity, and it can also dissolve the plasticizer in the polyvinyl chloride infusion set, and can also cause paclitaxel to precipitate when the preparation is diluted
[0003] Indeed, paclitaxel is difficult to cross the GI barrier due to its low solubility, efflux of P-glycoprotein in the GI tract, and metabolism by cytochrome P-450 3A4 enzymes in the intestine or liver
Researchers have adopted many strategies to improve the bioavailability of paclitaxel, but there is still no ideal oral dosage form of paclitaxel
[0004] Paclitaxel shows obvious multidrug resistance in the treatment of various types of tumor patients after relapse, mainly due to the overexpression of the ABC transporter family (especially P-glycoprotein), which makes antitumor drugs resistant to tumor cells After efflux, thereby reducing the drug concentration in tumor cells

Method used

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  • Paclitaxel nano micelle and application thereof
  • Paclitaxel nano micelle and application thereof
  • Paclitaxel nano micelle and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Embodiment 1, the preparation of paclitaxel nanomicelle

[0061] 1. Raw materials used in the preparation

[0062] 1. Polyethylene glycol-distearoylphosphatidylethanolamine (PEG 2000 -DSPE) has the molecular formula C 135 h 268 NO 56 P, molecular weight is 2829, contains the polyethylene glycol (PEG) that polymerization degree is 45, and molecular structural formula is as shown in formula II:

[0063] (Formula II)

[0064] 2. Polyethylene glycol 1000 vitamin E succinate (TPGS 1000 ) has the molecular formula (C 2 h 4 O) 23 C 33 h 54 o 5 , molecular weight is 1513; Containing degree of polymerization is the polyethylene glycol (PEG) of 23, and structural formula is as shown in formula III:

[0065] (Formula III)

[0066] 3. The molecular formula of dequalinium chloride is C 30 h 40 C 12 N 4 , the molecular weight is 527.57. Structural formula is as shown in formula IV:

[0067] (Formula IV)

[0068] 4. The molecular formula of paclitaxel is C 4...

Embodiment 2

[0131] Embodiment 2, the function of paclitaxel nanomicelle

[0132] 1. The culture method of the cells used in this example

[0133] The medium used for human breast cancer MCF-7 cells is cell culture medium I. The culture medium used for drug-resistant human breast cancer MCF-7 / Adr cells was cell culture medium II (1 μM doxorubicin maintains drug resistance), and was replaced with cell culture medium I for culture one week before the experiment.

[0134] The medium used for human colon adenocarcinoma Caco-2 cells is cell culture medium III.

[0135] All cells were cultured in a 37°C, 5% CO2 incubator.

[0136] Cell culture medium I: composed of RPMI-1640 cell culture medium, fetal bovine serum, penicillin and streptomycin, its proportioning ratio is: RPMI-1640 cell culture medium: fetal bovine serum: penicillin: streptomycin=1ml: 0.1ml : 100U: 100 μg.

[0137] Cell culture medium II: composed of RPMI-1640 cell culture medium, fetal bovine serum, penicillin, streptomycin ...

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Abstract

The invention discloses paclitaxel nano micelle and an application thereof. The paclitaxel nano micelle is prepared from the following components shown in the following (1), (2) or (3): (1) a carrier and paclitaxel, wherein the carrier is a mixture of polyethylene glycol-distearoyl phosphatidyl ethanolamine (PEG-DSPE), D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS) and dequalinium chloride; (2) a carrier and the paclitaxel, wherein the carrier is a mixture of the PEG-DSPE and the TPGS; and (3) a carrier and the paclitaxel, wherein the carrier is the PEG-DSPE. After the functionalized paclitaxel nano micelle disclosed by the invention is orally taken, the paclitaxel can penetrate through a barrier of gastrointestinal tract, thus the multi-drug resistance (MDR) of drug-resistant breast cancer is overcome. The oral formulation of the functionalized paclitaxel nano micelle disclosed by the invention can avoid the anaphylactic response, can be applied to numerous cancer patients and is also suitable for MDR tumors at the same time, thereby having great advantage compared with the traditional intravenous injection formulation.

Description

technical field [0001] The invention relates to a paclitaxel nano-micelle and application thereof. Background technique [0002] Paclitaxel (paclitaxel) is a natural substance with high anti-tumor activity extracted and purified from yew plants, and has significant curative effect on many types of cancer, including ovarian cancer, breast cancer and non-small cell lung cancer. Paclitaxel is not orally bioavailable due to its poor solubility (<1 μg / ml) and poor barrier permeability of the gastrointestinal tract. Paclitaxel preparations currently used in clinical practice are intravenous injections. The commercially available formulation of paclitaxel, Taxol, is a colorless viscous solution made from polyoxyethylene castor oil / absolute ethanol (50 / 50). However, the polyoxyethylene castor oil in the preparation can cause serious side effects in patients, such as allergic reactions, neurotoxicity and nephrotoxicity, and it can also dissolve the plasticizer in the polyvinyl c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/34A61P35/00A61K47/22
Inventor 吕万良姚红娟居瑞军王小星张燕李若婧于洋张亮
Owner PEKING UNIV
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