Polymer micelle coated with insoluble antitumor drug and preparation method of polymer micelle

An anti-tumor drug and polymer glue technology is applied in the field of polymer micelles encapsulating insoluble anti-tumor drugs and its preparation, which can solve the problems of no significant accumulation, avoid phagocytosis, enhance passive targeting ability, improve The effect of bioavailability

Inactive Publication Date: 2019-06-21
INNER MONGOLIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

No significant accumulation after multiple doses

Method used

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  • Polymer micelle coated with insoluble antitumor drug and preparation method of polymer micelle
  • Polymer micelle coated with insoluble antitumor drug and preparation method of polymer micelle
  • Polymer micelle coated with insoluble antitumor drug and preparation method of polymer micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Mix 10mgplla1092-mpeg4000-plla1092 triblock polymer, 1mg dasatinib, and 10mL methanol, and ultrasonically dissolve the carrier material and drug for 10min in a water bath to obtain a uniform mixed solution; place the obtained mixed solution in a rotary evaporator , 45°C rotary steaming for 30min, vacuum drying overnight to obtain a light yellow film; after the obtained film was swelled at 37°C for 15min, 10mL of 37°C deionized water was added for hydration, stirred for 30min, filtered through a 0.22μm microporous filter The dasatinib-plla1092-mpeg4000-plla1092 mixed micelle preparation was obtained by membrane filtration sterilization.

Embodiment 2

[0037] Mix 20mg of plla1092-mpeg4000-plla1092 triblock polymer, 2mg of dasatinib and 4mL of tetrahydrofuran, and ultrasonically dissolve the carrier material and drug for 10 minutes in a water bath to obtain a uniform mixed solution; place the obtained mixed solution in a rotary evaporator Rotary steam at 45°C for 30min, and vacuum dry overnight to obtain a light yellow film; after swelling the obtained film at 37°C for 15min, add 10mL of 37°C deionized water for hydration, stir for 30min, and use 0.22μm micro The dasatinib-plla1092-mpeg4000-plla1092 mixed micelle preparation was obtained by filtering and sterilizing through a pore filter membrane.

Embodiment 3

[0039] Mix 40mg of plla1092-mpeg4000-plla1092 triblock polymer, 4mg of dasatinib and 10mL of methanol, and ultrasonically dissolve the carrier material and drug for 10 minutes in a water bath to obtain a uniform mixed solution; place the obtained mixed solution in a rotary evaporator Rotary steam at 45°C for 30min, and vacuum dry overnight to obtain a light yellow film; after swelling the obtained film at 37°C for 15min, add 10mL of deionized water at 37°C for hydration, stir for 30min, and use a 0.22μm microporous The dasatinib-plla1092-mpeg4000-plla1092 mixed micelle preparation was obtained by filter membrane filtration sterilization.

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Abstract

The invention discloses a polymer micelle coated with an insoluble antitumor drug. A plla1092-mpeg4000-plla1092 triblock polymer is taken as a carrier of the polymer micelle, dasatinib is coated in ahydrophobic core plla of plla1092-mpeg4000-plla1092, and the mass ratio of the dasatinib to the plla1092-mpeg4000-plla1092 triblock polymer is 10: 1. According to the invention, the solubility of thedasatinib can be effectively increased, and phagocytosis of a reticuloendothelial system in vivo can be avoided, so that the circulation time of the dasatinib in blood is prolonged, and the bioavailability of the dasatinib is effectively improved; and meanwhile, a plla1092-mpeg4000-plla1092 vector can enhance the passive targeting capability and improve the antitumor effect of the dasatinib.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a polymer micelle carrying insoluble antitumor drugs and a preparation method thereof. Background technique [0002] Dasatinib, chemical name: N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]- 2-Methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide. The product name is Sprycel, which is a receptor tyrosine kinase inhibitor developed by Bristol-Myers Squibb. In mid-2006, it was approved by the US FDA first. Dasatinib can treat adult chronic leukemia and leukemia treatment failure or Patients with intolerance have a good therapeutic effect, and it can also be used to treat adult chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia who are resistant or intolerant to imatinib. [0003] The structural formula of Dasatinib is C 22 h 26 ClN 7 o 2 S, molecular weight: 487.16, structural formula is as follows: [0004]...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K31/506A61P35/02
Inventor李瑞娟顾艳丽王小凤刘佳张烨
OwnerINNER MONGOLIA MEDICAL UNIV