Paclitaxel entrapped polymeric micelle for treating tumors, and preparation method thereof

A technology of polymer glue and paclitaxel, which is applied in the field of polymer micelles loaded with paclitaxel and its preparation, to achieve the effects of improving therapeutic effect, increasing drug loading, and reducing adverse reactions

Inactive Publication Date: 2015-10-28
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Studies have also shown that paclitaxel is a typical P-gp efflux substrate, and there is an obvious phenomenon of tumor multidrug resistance MDR (Multidrug resistance, MDR) after multiple administrations.

Method used

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  • Paclitaxel entrapped polymeric micelle for treating tumors, and preparation method thereof
  • Paclitaxel entrapped polymeric micelle for treating tumors, and preparation method thereof
  • Paclitaxel entrapped polymeric micelle for treating tumors, and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Weigh 217.5mg PEG-PLA, 32.5mg Vitamin E-TPGS, 100mg paclitaxel, add 4ml acetonitrile, and ultrasonically dissolve the carrier material and drug fully. Place the solution in a rotary evaporator at 40°C for 30 minutes to evaporate the organic solvent to dryness, and place it in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 15ml of deionized water and stir at a constant speed of 500rpm for 30min. Pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain paclitaxel PEG-PLA / Vitamin E-TPGS mixed micellar preparation.

Embodiment 2

[0047] Weigh 217.5 mg PEG-PLA, 32.5 mg Vitamin E-TPGS, and 100 mg paclitaxel, add 4 ml of dichloromethane, and ultrasonically dissolve the carrier material and the drug. Place the solution in a rotary evaporator at 30°C for 30 minutes to evaporate the organic solvent to dryness thoroughly, and place it in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 10ml of deionized water and stir at a constant speed of 500rpm for 30min. Pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain paclitaxel PEG-PLA / Vitamin E-TPGS mixed micellar preparation.

Embodiment 3

[0049] Weigh 217.5 mg PEG-PLA, 32.5 mg Vitamin E-TPGS, and 120 mg paclitaxel, add 4 ml of dichloromethane, and ultrasonically dissolve the carrier material and the drug. Place the solution in a rotary evaporator at 30°C for 30 minutes to evaporate the organic solvent to dryness thoroughly, and place it in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 10ml of normal saline and stir at a constant speed of 500rpm for 30min. Pass the hydration solution through a 0.22 μm cellulose acetate filter membrane to obtain paclitaxel PEG-PLA / Vitamin E-TPGS mixed micellar preparation.

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Abstract

The invention belongs to the technical field of biomedicines, and relates to a paclitaxel entrapped polymeric micelle for treating tumors, and a preparation method thereof. The preparation method comprises the following steps: preparing paclitaxel PEG-PLA/Vitamin E-TPGS mixed micelle through adopting a film dispersion technology, and entrapping paclitaxel into the hydrophobic core of the mixed micelle by using the mixed micelle composed of PEG-PLA and Vitamin E-TPGS as a carrier. The prepared paclitaxel paclitaxel PEG-PLA/Vitamin E-TPGS mixed micelle can effectively increase the solubility of paclitaxel and substantially improves the paclitaxel load of a micelle system to reach 35% (w/w), and Vitamin E-TPGS in the mixed micelle system has a P-gp efflux inhibition biologic function, and can efficiently reverse the multidrug resistance of tumors in order to improve the tumor treatment effect. The mixed micelle does not contain Tween80 or ethanol; and compared with commercial paclitaxel injections, the above preparation provided by the invention has the advantages of no allergy of commercial preparations, reduction of toxic side effects, and increase of the safety of clinic application.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to polymer micelles carrying paclitaxel, in particular to a polymer micelles carrying paclitaxel for treating tumors and a preparation method thereof. and improve the therapeutic effect of drug-resistant tumors. Background technique [0002] The prior art discloses paclitaxel (Paclitaxel, PTX), which is a diterpene compound of a taxene ring extracted from the trunk and bark of Taxus yew, with a molecular formula of C 47 h 51 NO 14 , the molecular weight is 853.91Da, and the structural formula is as follows: [0003] [0004] Paclitaxel is currently the first-line broad-spectrum anti-tumor drug, and its curative effect is remarkable. Studies have shown that paclitaxel promotes the polymerization of spindle tubulin, inhibits depolymerization, and maintains the stability of tubulin, thereby inhibiting the mitosis process of tumor cells, thereby playing an anti-tumor role. effe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K31/337A61P35/00
Inventor 沙先谊范卓洋
Owner FUDAN UNIV
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