Nanoparticle for embedding medicinal Adriamycin as well as preparation method and application thereof

A nanoparticle and doxorubicin technology, which is applied in the direction of drug combination, pharmaceutical formula, and preparations for in vivo tests, etc., can solve the problems of cumbersome preparation process, high cost, and short sustained release time, and achieve broad application prospects and low cost. Low, long-term sustained-release effect

Inactive Publication Date: 2010-07-28
HUNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The stability of polymer nanoparticles has been improved, but there is still the shortcoming of short sustained release time, and in order to achieve simultaneous imaging and treatment, two steps are required to synthesize gold nanoparticles and embed doxorubicin molecules, the preparation process is cumbersome and the cost is relatively high. high

Method used

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  • Nanoparticle for embedding medicinal Adriamycin as well as preparation method and application thereof
  • Nanoparticle for embedding medicinal Adriamycin as well as preparation method and application thereof
  • Nanoparticle for embedding medicinal Adriamycin as well as preparation method and application thereof

Examples

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Embodiment 1

[0042] a kind of like image 3 The nanoparticle embedding drug doxorubicin of the present invention is shown, the nanoparticle is a core-shell structure in which the core is embedded in the shell, wherein the core is the embedded drug doxorubicin, and the material for the shell is silicon dioxide , the shell surface is modified with carboxyl groups.

[0043] The preparation method of nanoparticles embedding drug doxorubicin of the present embodiment comprises the following steps:

[0044] (1) Embedding doxorubicin in the silica matrix: Mix 7.5mL cyclohexane, 1.8mL surfactant Triton X-100 and 1.6mL n-hexanol, add Add 500 μL of 10 mg / mL sodium fluoride solution as the dispersed phase, stir well to form an inverse microemulsion; add 80 μL of 0.05 mol / L doxorubicin solution and 100 to 200 μL orthosilicate ethyl ester to the inverse microemulsion , the DOX-SiNP microemulsion system was obtained after 24 hours of reaction;

[0045] (2) Modification of functional groups: Use the s...

Embodiment 2

[0051] A nanoparticle embedding the drug doxorubicin of the present invention, the nanoparticle is the carboxyl group on the surface of the nanoparticle prepared in Example 1 and Aptamer molecules with tumor cell targeting function are grafted.

[0052] The nanoparticles embedded with drug doxorubicin in this example were prepared by EDC / NHS cross-linking method: first, the DOX-COOH-SiNP prepared in Example 1 was washed by centrifugation with sterilized water once, and then ultrasonically dispersed in DOX-COOH-SiNP solution was obtained in sterilized MES buffer; then 100 μL of 35 mg / mL NHS, 100 μL of 12 mg / mL EDC, 50 μL of 10 μM sgc8c were added to 1 mL of 10 mM / L MES buffer (pH5.5) DNA and 250 μL 8mg / mL DOX-COOH-SiNP solution were shaken in a shaker at room temperature for 3 hours, and finally washed twice with 0.1mM PBS (pH 7.2) at 14000rpm to complete the Aptamer with CEM cell targeting The molecule sgc8c was modified onto the surface of DOX-COOH-SiNP to prepare the nanopar...

Embodiment 3

[0061] A nanoparticle of the present invention embedding drug doxorubicin, the nanoparticle is a core-shell structure in which a shell embeds a core, wherein the core is embedded drug doxorubicin, and the material for the shell is silicon dioxide, The shell surface is modified with amino groups. The difference between the preparation method of this drug-embedded nanoparticle and Example 1 is only that the silylating agent N-(propyltrimethoxysilane)-ethylenediamine-triacetate sodium in Example 1 is replaced by N-( β-aminoethyl)-γ-aminopropyltriethoxysilane, and all the other steps are the same as in Example 1.

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Abstract

The invention belongs to the technical field of composite medicine materials as well as a preparation method and application thereof, more particularly discloses a nanoparticle for embedding medicinal Adriamycin. The nanoparticle has a core-shell type structure with an inner core embedded by an outer shell, wherein the inner core is embedded medicinal adriamycin, and the material for the outer shell is silicon dioxide; and the preparation method of the nanoparticle comprises the following steps of: evenly mixing cyclohexane, a surfactant and n-hexylalcohol, adding a sodium fluoride solution into the mixed solution after being evenly mixed to form a reverse-phase microemulsion; adding adriamycin and tetraethoxysilane into the reverse-phase microemulsion, and reacting to obtain a nanoparticle microemulsion system for embedding the adriamycin; adding a silylanization reagent containing functional groups into the microemulsion system, stirring for reacting, adding ethanol and demulsifying, centrifuging and then preparing the nanoparticle for embedding the medicinal adriamycin and modifying the functional groups. The nanoparticle embedding for the adriamycin has good stability, good biocompatibility, long slow-release time, large drug-loading rate, high medicine packaging rate, and the like, and has application prospect in the fields of tumor imaging and treatment.

Description

technical field [0001] The invention relates to a composite medical material and its preparation and application, in particular to a drug-embedded granular material and its preparation and application. Background technique [0002] Since the 1960s, doxorubicin has been the most frequently used chemotherapeutic drug in clinical practice. Its mechanism of action is mainly: the anthracycline planar structure of doxorubicin molecule is inserted into the double-stranded structure of DNA molecule to inhibit DNA replication and RNA transcription, thereby inhibiting tumor growth. Doxorubicin is characterized by broad anticancer spectrum and high chemotherapy index, but it has side effects such as bone marrow suppression, nausea, vomiting, stomatitis, hair loss, high fever, bleeding symptoms, phlebitis and skin pigmentation, and there is dose dependence Cardiotoxicity (manifested as various arrhythmias), myocardial necrosis and even congestive heart failure will occur when the cumul...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/704A61K49/00A61K47/04A61K47/24A61P35/00
Inventor 王柯敏海罗何晓晓倪晓琪石慧羊小海
Owner HUNAN UNIV
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