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Docetaxel-coated polymeric micelle and preparation method thereof

A technology of docetaxel and polymer glue is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., to achieve the effects of improving treatment effect, avoiding phagocytosis and reducing toxicity

Inactive Publication Date: 2013-12-18
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, due to the sensitivity of taxanes to efflux proteins such as P-gp, MDR has gradually become the main reason for limiting the clinical application of docetaxel.

Method used

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  • Docetaxel-coated polymeric micelle and preparation method thereof
  • Docetaxel-coated polymeric micelle and preparation method thereof
  • Docetaxel-coated polymeric micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Weigh 300mgP105, 3mgF127, 8mg docetaxel, add 3ml acetonitrile, and ultrasonically dissolve the carrier material and drug fully. The solution was evaporated in a rotary evaporator at 37°C for 30 min, and dried in vacuum overnight. Swell the film at 40°C for 10 minutes, add 15ml of water at 40°C and stir for 30 minutes, and filter to obtain the docetaxel Pluronic F127 / P105 mixed micelle preparation.

Embodiment 2

[0048] Weigh 270mgP105, 30mgF127, 6mg of docetaxel, add 3ml of dichloromethane, and ultrasonically dissolve the carrier material and the drug. The solution was evaporated in a rotary evaporator at 37°C for 30 min, and dried in vacuum overnight. The film was swelled at 40°C for 30 minutes, added with 10ml of 40°C water and stirred for 30 minutes, and filtered to obtain the docetaxel Pluronic F127 / P105 mixed micelle preparation.

Embodiment 3

[0050] Weigh 225mg of P105, 75mg of F127, 5mg of docetaxel, add 4ml of dichloromethane, and ultrasonically dissolve the carrier material and the drug. The solution was evaporated in a rotary evaporator at 37°C for 30 min, and dried in vacuum overnight. The film was swelled at 50° C. for 5 minutes, added with 5 ml of 50° C. water and stirred for 30 minutes, and filtered to obtain the docetaxel Pluronic F127 / P105 mixed micelle preparation.

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Abstract

The invention belongs to the technical field of biological medicines, and relates to a docetaxel-coated polymeric micelle and a preparation method thereof. The preparation method is characterized in that a thin-film dispersion method is used for preparing a docetaxel Pluronic F127 / P105 mixed micelle, Pluronic is used as a carrier, and docetaxel is coated in a hydrophobic inner core PPO (poly-p-phenylene oxide) of Pluronic. The mixed micelle prepared by the method can be used for effectively improving the solubility of the docetaxel; the PEO (polyoxyethylene) long chain of F127 can play a role in long circulation and is prevented from being phagocytized by a reticulo-endothelial system, thus the half-life period of the mixed micelle in blood is prolonged; the P105 in the mixed micelle can be used for inhibiting the excretion of P-gp to the maximum degree and can efficiently reverse the multidrug resistance of tumors so as to improve the treatment effect on the tumors. The mixed micelle prepared by the method does not contain Tween-80 or alcohol. Compared with commercially available docetaxel injection, the mixed micelle can be used for obviously improving the toxic and side effects of the medicines and the safety of clinical application.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a polymer micelle carrying docetaxel and a preparation method thereof. technical background [0002] Multidrug resistance (MDR) refers to the cross-resistance of tumor cells to various anticancer drugs with different chemical structures, functions and mechanisms of action. The multidrug resistance of tumor cells to anticancer drugs is the main reason for the failure of tumor chemotherapy, and it is also an important issue that has not been resolved since chemotherapy was involved in tumor treatment. Studies have shown that the mechanism of MDR is more complicated, but the efflux pumps such as P-gp produced by the overexpression of MDR1 can "pump" intracellular drugs, resulting in a decrease in intracellular drug concentration, which is the main mechanism of MDR. [0003] Docetaxel (DTX) is a taxane antineoplastic drug obtained by semi-synthesis from the precursor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/337A61K47/34A61P35/00A61P35/04
Inventor 方晓玲陈亮岑沙先谊
Owner FUDAN UNIV
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