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Vincristine-PEG-PLGA segmented copolymer nanoparticle, its preparation method and use

A -PEG-PLGA, block copolymer technology, applied in the field of medicine, can solve the problems of toxicity, low efficiency and complex preparation procedures of degradants, and achieve the effects of reducing toxic side effects, prolonging time and increasing compliance

Inactive Publication Date: 2011-11-09
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it has the following disadvantages: low efficiency of encapsulating hydrophobic drugs, sudden release of drugs, complex preparation procedures and toxic degradation products
However, these drug-loading methods have deficiencies in different aspects, and there is still a long way to go to clinical practice.

Method used

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  • Vincristine-PEG-PLGA segmented copolymer nanoparticle, its preparation method and use
  • Vincristine-PEG-PLGA segmented copolymer nanoparticle, its preparation method and use
  • Vincristine-PEG-PLGA segmented copolymer nanoparticle, its preparation method and use

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Embodiment Construction

[0024] The vincristine-PEG-PLGA block copolymer nanoparticle of the invention is prepared by encapsulating vincristine in PEG-PLGA.

[0025] Wherein, vincristine adopts its sulfate-vincristine sulfate (VCR).

[0026] The ratio of vincristine and PEG-PLGA is as follows:

[0027]Vincristine: PEG-PLGA block copolymer = 1:10-1:1000.

[0028] The preparation of PEG-PLGA block copolymer nanoparticles can adopt emulsification solvent evaporation method, precipitation method, ultrasonic method, solid dispersion-hydration method, solvent evaporation-solid melt dispersion method, thin film dispersion method, solvent evaporation method, etc.

[0029] Such as:

[0030] 1. The emulsified solvent evaporation method adopts the single emulsion method

[0031] The PEG-PLGA block copolymer is added to the mixed organic solvent of dichloromethane and acetone containing the model drug to form the oil phase, and the oil phase is added to the water phase composed of emulsifier and deionized wate...

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Abstract

The invention provides a vincristine-PEG-PLGA segmented copolymer nanoparticle for incorporating vincristine into PEG-PLGA segmented copolymer, also provides a method for preparing the nanoparticle by emulsification-solvent evaporation method and other methods, and use of the nanoparticle in preparing anticancer drug. The nanoparticle provided by the invention can improve the solubility of drugs effectively; can avoid dose dumping and incomplete release to allow the drug to release slowly; can reduce the abilities of RES to identificate and phagocytose nanoparticle, so as to realize the targeted release of the drug in tissues and organs out of the reticuloendothelial system; can reduce toxic and side effect, increase biocompatibility, prolong the circulation time of the drug in the blood; and can increase the compliance of the patients.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a vincristine-PEG-PLGA block copolymer nanoparticle, a preparation method and application. Background technique [0002] Leukemia is one of the most common malignant tumors, which seriously threatens human life and health. Although current treatment methods include chemotherapy, radiation therapy, bone marrow transplantation and supportive therapy, antineoplastic drug therapy is still the most effective therapy. At present, there are five categories that are most widely used: antimetabolites, antitumor antibiotics, alkylating agents, plant components, and others. The corresponding drugs include methotrexate, doxorubicin, cyclophosphamide, and vinca Sim and L-asparaginase etc. [1]. Most of them are limited in clinical application due to their poor specificity, significant toxic and side effects on normal tissues and organs in conventional therapeutic doses, intolerance by patients and hi...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/475A61K47/34A61P35/00A61P35/02
Inventor 张阳德张浩伟廖明媚刘殿奎汪建荣齐贵新谢薇
Owner CENT SOUTH UNIV
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