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Preparation method for surface-laminated and self-assembled doxorubicin hydrochloride copolymer nano-particles

A technology of doxorubicin hydrochloride and self-assembly, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, drug combinations, etc., and can solve the problems of low drug utilization, poor targeting, and large toxic and side effects And other issues

Active Publication Date: 2017-03-15
JIANGSU HEALTH VOCATIONAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The object of the present invention is to overcome the poor targeting of doxorubicin hydrochloride (DOX) drugs, the shortcomings of large toxic and side effects; to overcome the low drug availability of doxorubicin hydrochloride PLGA nanoparticles and the release process due to their surface lipophilic properties There are obvious disadvantages of sudden release

Method used

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  • Preparation method for surface-laminated and self-assembled doxorubicin hydrochloride copolymer nano-particles
  • Preparation method for surface-laminated and self-assembled doxorubicin hydrochloride copolymer nano-particles
  • Preparation method for surface-laminated and self-assembled doxorubicin hydrochloride copolymer nano-particles

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Embodiment 1

[0015] A preparation method of surface laminated self-assembled doxorubicin hydrochloride copolymer nanoparticles, which contains the following steps:

[0016] 1) Preparation of lactic acid-glycolic acid copolymer nanoparticles loaded with doxorubicin hydrochloride: Accurately weigh 1 mg of doxorubicin hydrochloride, completely dissolve it in 250 μL of deionized water as the inner aqueous phase; accurately weigh 50 mg of PLGA, and dissolve in 2 mL of The mixed solution of methyl chloride and acetone (v / v=1:1) was shaken and dissolved as the organic phase; the inner water phase was added to the organic phase dissolved in PLGA, and ultrasonically emulsified and dispersed in an ice bath for 6-10 minutes to form colostrum (W / O); add colostrum into the solution containing 0.5% emulsifier F68, shake rapidly and uniformly, ultrasonically emulsify and disperse in ice bath for 12min, and form double emulsion (W / O / W); add 0.3%F68 continuous phase 15mL, room temperature Under low-speed ...

Embodiment 2

[0020] A preparation method of surface laminated self-assembled doxorubicin hydrochloride copolymer nanoparticles, which contains the following steps:

[0021] 1) Preparation of lactic acid-glycolic acid copolymer nanoparticles loaded with doxorubicin hydrochloride: the preparation method is the same as in Example 1.

[0022] 2) Layer-by-layer self-assembly of natural polyelectrolyte chitosan and alginic acid on the surface of DOX-PLGA NPs: prepare ALG solution (2mg / mL) containing 0.5M NaCl. Add 2 mL of DOX-PLGA NPs solution to the centrifuge tube, and add 4 mL of chitosan solution (2 mg / mL) containing 0.5 M NaCl at the same time, incubate in a water bath at 37 °C for 20 min, then centrifuge at high speed to remove the supernatant, and wash; use 2 mL of deionized Resuspend nanoparticles in water, add ALG solution (2mg / mL) containing 0.5M NaCl, absorb in constant temperature water bath for the same time and then centrifuge at high speed. In this way, a double-layer cycle is co...

Embodiment 3

[0024] A preparation method of surface laminated self-assembled doxorubicin hydrochloride copolymer nanoparticles, which contains the following steps:

[0025] 1) Preparation of lactic acid-glycolic acid copolymer nanoparticles loaded with doxorubicin hydrochloride: the preparation method is the same as in Example 1.

[0026] 2) Self-assembly of natural polyelectrolyte chitosan and alginic acid on the surface of DOX-PLGA NPs: add 2 mL of DOX-PLGA NPs solution to the centrifuge tube, and add 4 mL of chitosan solution (2 mg / mL, 0.5 M NaCl), incubated in a water bath at 37°C for 20 minutes, then centrifuged at high speed to remove the supernatant, and washed; resuspended nanoparticles in 2 mL of deionized water, added 4 mL of ALG solution (2mg / mL, 0.5M NaCl), and adsorbed the same in a water bath at 37°C Centrifuge at high speed after time. In this way, a double-layer cycle is completed, and the above operation is repeated until one double-layer is adsorbed.

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Abstract

The invention relates to the technical field of a pharmaceutical preparation and specifically relates to surface-laminated and self-assembled doxorubicin hydrochloride copolymer nano-particles and a preparation method thereof. According to the invention, a multiple emulsion-solvent evaporation process is adopted for preparing doxorubicin hydrochloride-loaded lactic acid-glycolic acid copolymer nano-particles, and then natural hydrophilic polyelectrolyte chitosan and alginic acid are selected for laminating and self-assembling on the surfaces of the nano-particles. The self-assembled nano-particles prepared according to the invention have particle sizes within the scope of 100-300nm and are uniformly distributed; the burst release of the medicine can be reduced, and the release time of the medicine can be prolonged; the nano-particles are slowly released under a physiological pH value, so that the nano-particles are beneficial to anti-tumor application; and the nano-particles have certain long circulation effects and excellent market prospects.

Description

technical field [0001] The invention relates to a method for preparing surface laminated self-assembled doxorubicin hydrochloride copolymer nanoparticles, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Doxorubicin (DOX) is a glycoside antibiotic with anthracyclines produced by Streptomyces actinomycetes. Its chemical structure has lipophilic anthracyclines, and the six-membered ring side chain has one Hydrophilic amino sugar, the structural formula is shown in formula I. Doxorubicin, as a non-specific anticancer drug for tumor cell cycle, can be directly embedded between the DNA base pairs of tumor cells at each stage, and electrostatically binds to the DNA minor groove region, irreversibly destroys the tertiary structure of DNA, interferes with other Transcription process, inhibition of mRNA and DNA synthesis, and then cause cell death or stagnation in S phase, G2 phase, showing strong anticancer activity. As the broad-spect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/36A61K31/704A61P35/00
CPCA61K9/5153A61K9/5161A61K31/704
Inventor 刘元芬郑春丽何新怡李洁丽
Owner JIANGSU HEALTH VOCATIONAL COLLEGE
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