Doxorubicin hydrochloride self-assembled polymer nanoparticle and preparation method thereof

A doxorubicin hydrochloride and polymer technology, which is applied in the field of doxorubicin hydrochloride self-assembled polymer nanoparticles and their preparation, can solve the problems of unstable molecular structure, short plasma half-life, serious toxic and side effects, and reduce adverse reactions As well as toxic side effects, no physiological toxicity, and the effect of reducing toxicity

Active Publication Date: 2017-09-05
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, the existing doxorubicin hydrochloride injection has serious side effects. In addition to myelosuppression, gastrointestinal toxicity and hair loss, it can also cause severe cardiotoxicity, manifested as various arrhythmias, and irreversible myocardial damage can occur when the cumulative amount is large. damage, and the molecular structure is unstable, and the plasma half-life after administration is extremely short, which seriously reduces its curative effect

Method used

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  • Doxorubicin hydrochloride self-assembled polymer nanoparticle and preparation method thereof
  • Doxorubicin hydrochloride self-assembled polymer nanoparticle and preparation method thereof
  • Doxorubicin hydrochloride self-assembled polymer nanoparticle and preparation method thereof

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Embodiment 1

[0024] Embodiment 1 Preparation of doxorubicin hydrochloride self-assembled polymer nanoparticles

[0025] Prescription composition: doxorubicin hydrochloride as the main drug, PLGA as the polymer carrier.

[0026] The specific preparation method is as follows:

[0027] 1) Accurately weigh 0.1 mg of doxorubicin hydrochloride and dissolve it in 1 ml of dimethylsulfoxide (DMSO) to obtain a DMSO solution with a concentration of doxorubicin hydrochloride of 0.1 mg / ml.

[0028] 2) Accurately weigh 1 mg of PLGA and dissolve it in 1 ml of acetonitrile to prepare a PLGA solution with a concentration of 1 mg / ml.

[0029] 3) Precisely pipette 25 μl of doxorubicin hydrochloride solution and add it dropwise to the PLGA solution, and mix well to obtain a co-solution. Take 3ml of deionized water and put it in a beaker. Under the condition of magnetic stirring, slowly add the co-solution dropwise to the deionized water, and keep stirring at room temperature with different stirring speeds o...

Embodiment 2

[0034] Embodiment 2 Preparation of doxorubicin hydrochloride self-assembled polymer nanoparticles

[0035] Prescription composition: doxorubicin hydrochloride as the main drug, PLGA as the polymer carrier.

[0036] The specific preparation method is the same as in Example 1, keeping other conditions constant, the stirring speed is selected at 30r / min, and only changing the solvent type of the PLGA solution in step 2), that is, accurately weighing 1mg PLGA dissolved in 1ml acetonitrile, 1ml acetone, 1ml dichloro A PLGA solution with a concentration of 1 mg / ml was prepared in methane, and the particle size and PDI of the doxorubicin hydrochloride-PLGA self-assembled polymer nanoparticles were measured, and the results are shown in Table 2.

[0037] Table 2

[0038] Organic solvents Particle size / nm PDI acetone 137.68 0.189 Acetonitrile 75.45 0.157 Dichloromethane 168.92 0.367

[0039] As can be seen from Table 2, when the organic solvent ...

Embodiment 3

[0040] Embodiment 3 Preparation of doxorubicin hydrochloride self-assembled polymer nanoparticles

[0041] Prescription composition: doxorubicin hydrochloride as the main drug, PLGA as the polymer carrier.

[0042] Concrete preparation method is the same as embodiment 1, keeps other conditions constant, and stirring speed selects 30r / min, just changes the input amount of doxorubicin hydrochloride in step 1), promptly is 1 by the mass ratio of doxorubicin hydrochloride and PLGA respectively: 25, 1:20, 1:10, and 1:5 ratios were used to feed materials, and the particle size, PDI, and encapsulation efficiency of doxorubicin hydrochloride-PLGA self-assembled polymer nanoparticles were measured, and the results are shown in Table 3.

[0043] table 3

[0044] Doxorubicin hydrochloride: PLGA Particle size / nm PDI Encapsulation Efficiency (EE%) 1:25 98.31 0.189 68.1 1:20 85.72 0.201 73.9 1:10 75.45 0.157 77.6 1:5 80.25 0.142 71.8

[0045...

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Abstract

The invention discloses a doxorubicin hydrochloride self-assembled polymer nanoparticle which is prepared from doxorubicin hydrochloride and an amphipathic high-molecular polymer PLGA (Polylactic-co-Glycolic Acid), wherein the PLGA is formed by two monomers, namely lactic acid (LA) and glycolic acid (GA). The preparation method comprises the following steps: 1) dissolving a drug doxorubicin hydrochloride into a polar organic solvent A so as to obtain a doxorubicin hydrochloride solution; 2) dissolving the PLGA into a polar organic solvent B so as to obtain a PLGA solution; 3) uniformly mixing the doxorubicin hydrochloride solution with the PLGA solution so as to obtain an eutectic solution, dripping the eutectic solution into an aqueous phase under the stirring condition, continuously stirring, and volatilizing the organic solvent; and 4) centrifuging the completely volatilized solution at a high speed by using a centrifugal machine, and collecting the precipitate, thereby obtaining the doxorubicin hydrochloride self-assembled polymer nanoparticle. The prepared product can achieve the effects of reducing the drug toxicity, reducing the administration frequency, improving the drug stability, delaying in-vivo release time of the drug, reducing adverse reactions of the drug, improving the bioavailability and efficacy of the drug and achieving excellent treatment effects.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a doxorubicin hydrochloride self-assembled polymer nanoparticle and a preparation method thereof. Background technique [0002] Doxorubicin (DOX) is a commonly used first-line chemotherapy drug with strong pharmacological activity and broad anti-tumor spectrum. It has significant curative effect on breast cancer, lung cancer and other solid tumors. , Inhibition of nucleic acid synthesis. However, after the intravenous injection of the drug, the side effects are large, and there are adverse reactions such as severe dose-dependent cardiotoxicity and bone marrow suppression, and long-term use of doxorubicin is prone to drug resistance, and the plasma half-life after administration is extremely short, which reduces the curative effect , resulting in a low therapeutic index, which greatly limits the clinical application of doxorubicin hydrochloride. Therefore, a new tumor-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/704A61K47/34A61P35/00
CPCA61K9/5153A61K31/704
Inventor 陈立江张金凤刘宇李丽
Owner LIAONING UNIVERSITY
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