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Multifunctional nanoparticle preparation capable of preventing drug tolerance and preparation method thereof

A multifunctional, nanoparticle technology, applied in antitumor drugs, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve problems such as drug resistance, application limitations, etc., achieve good performance, simple preparation method, good cell toxic effects

Inactive Publication Date: 2014-01-08
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, tumor cells are prone to drug resistance, which limits its application.

Method used

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  • Multifunctional nanoparticle preparation capable of preventing drug tolerance and preparation method thereof
  • Multifunctional nanoparticle preparation capable of preventing drug tolerance and preparation method thereof
  • Multifunctional nanoparticle preparation capable of preventing drug tolerance and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] This example relates to a preparation method of mPEG-PLGA nanoparticle preparation loaded with docetaxel and perifosine.

[0035] The preparation of the new multifunctional nanoparticle preparation loaded with docetaxel and perifo comprises the following steps:

[0036] (1) 2 mg of docetaxel, 2 mg of perifosine, and 20 mg of mPEG-PLGA copolymer were dissolved in dichloromethane as the oil phase;

[0037] (2) Make PVA into a solution with a weight volume concentration of 1% as the water phase;

[0038] (3) Under the condition of an ultrasonic ice bath, add the oil phase to the water phase dropwise to obtain a mixed solution;

[0039] (4) rotary evaporation to remove the organic solvent in the mixed solution obtained in step (3);

[0040] (5) Centrifuge the solution obtained in step (4) at high speed (12,000-50,000 rpm) for 30 minutes to remove free drug and obtain a nanoparticle solution with light blue opalescence;

[0041] (6) The nanoparticle solution was lyophiliz...

Embodiment 2

[0043] This embodiment relates to a preparation method of PEG-PLGA-Fol nanoparticle preparations loaded with docetaxel and perifosine;

[0044] The preparation of the new multifunctional nanoparticle preparation loaded with docetaxel and perifo comprises the following steps:

[0045] (1) Docetaxel 2mg, Perifosine 2mg, mPEG-PLGA-Fol copolymer 20mg dissolved in dichloromethane as the oil phase;

[0046] (2) Make PVA into a solution with a weight volume concentration of 1% as the water phase;

[0047] (3) Under the condition of an ultrasonic ice bath, add the oil phase to the water phase dropwise to obtain a mixed solution;

[0048] (4) rotary evaporation to remove the organic solvent in the mixed solution obtained in step (3);

[0049] (5) Centrifuge the solution obtained in step (4) at high speed (12,000-50,000 rpm) for 30 minutes to remove free drug and obtain a nanoparticle solution with light blue opalescence;

[0050](6) The nanoparticle solution was lyophilized at low t...

Embodiment 3

[0052] This embodiment relates to a kind of mPEG-PLGA-R loaded with docetaxel and perifosine 7 The preparation method of nanoparticle preparation;

[0053] The preparation of the new multifunctional nanoparticle preparation loaded with docetaxel and perifo comprises the following steps:

[0054] (1) Docetaxel 2mg, Perifosine 2mg, mPEG-PLGA-R 7 20 mg of copolymer is dissolved in dichloromethane as the oil phase;

[0055] (2) Make PVA into a solution with a weight volume concentration of 1% as the water phase;

[0056] (3) Under the condition of an ultrasonic ice bath, add the oil phase to the water phase dropwise to obtain a mixed solution;

[0057] (4) rotary evaporation to remove the organic solvent in the mixed solution obtained in step (3);

[0058] (5) Centrifuge the solution obtained in step (4) at high speed (12,000-50,000 rpm) for 30 minutes to remove free drug and obtain a nanoparticle solution with light blue opalescence;

[0059] (6) Freeze-dry the nanoparticle ...

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Abstract

The invention discloses a multifunctional nanoparticle preparation capable of preventing drug tolerance and a preparation method thereof. The preparation method comprises the following steps of: dissolving docetaxel and perifosine and a copolymer in an organic solvent to serve as an oil phase; regarding a PVA solution as an aqueous phase; dripping the oil phase into the aqueous phase at the presence of ultrasound ice-bath to obtain a mixed emulsion; performing reduced pressure distillation to remove the organic solvent; carrying out centrifugal treatment; re-dissolving collected nanoparticle after water-washing; and carrying out vacuum freeze drying to obtain the nanoparticle preparation. The prepared multifunctional nanoparticle preparation has good grain size, good encapsulation efficiency and good drug loading capacity, and can improve cytotoxicity and cell intake amount efficiently.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a drug-resistant multifunctional nanoparticle preparation and a preparation method thereof. Background technique [0002] Targeted nano drug delivery systems can generally be divided into active targeting and passive targeting nano drug delivery systems. An important direction in the research of active targeted drug delivery systems is to use the principle of specific binding between receptors and ligands. Folate is a commonly used active targeting ligand, and folate receptors are overexpressed on the surface of many tumor cell membranes. Based on this special effect, drug carriers combined with folic acid can be introduced into these tumor cells. Cell-penetrating peptides (CPPs) are a class of short peptides, less than 30 amino acids, with strong membrane-penetrating ability, and can transport anti-tumor drugs, polypeptides, nucleic acids or nan...

Claims

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Application Information

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IPC IPC(8): A61K31/685A61K9/19A61K47/34A61P35/00A61K31/337A61K47/32
Inventor 沈琦卜祥媛陈晶晶
Owner SHANGHAI JIAO TONG UNIV
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