Drug-loading nano-micelles, and preparation method and application thereof

A drug-loading nanometer and micelle technology, which is applied in the field of nanomedicine, can solve the problems of biomembrane permeability toxicity, low drug loading or gene efficiency, etc., and achieves the effects of simple and easy preparation method and easy operation and promotion.

Active Publication Date: 2013-02-13
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned drug-loading systems generally have biomembrane permeabi

Method used

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  • Drug-loading nano-micelles, and preparation method and application thereof
  • Drug-loading nano-micelles, and preparation method and application thereof
  • Drug-loading nano-micelles, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0027] This embodiment also provides a method for preparing an amphiphilic triblock copolymer, comprising the following steps:

[0028] Step S110: Using polyethylene glycol derivatives as initiators, synthesizing linear triblock copolymers comprising polyethylene glycol derivatives, side chain-protected polylysine and polyleucine by NCA ring-opening polymerization , wherein one end of the side chain-protected polylysine is connected to polyethylene glycol derivatives through an amide bond, and the other end is connected to polyleucine through a peptide bond, and the molecular weight of the polyethylene glycol derivative is 2000, and the side chain The degree of polymerization of the protected polylysine is 10-200, and the degree of polymerization of polyleucine is 10-200.

[0029] The details are as follows: dissolve polyethylene glycol derivatives with a molecular weight of 2000 in an organic solvent at a concentration range of 1-100 mg / mL, heat to 30-50 °C under nitrogen pro...

example 1

[0044] Example 1, the preparation of carboxypolyethylene glycol-polylysine-polyleucine triblock copolymer

[0045] After the polymerization tube was evacuated, it was filled with nitrogen protection, and 0.5g of NH with a molecular weight of 2000 2 -PEG-COOH was dissolved in 20mL of DMF and added to the polymerization tube, according to the LysZ-NCA monomer and CH 3 O-PEG-NH 2 The molar ratio of the LysZ-NCA monomer is added in a ratio of 10:1, and the constant temperature reaction is carried out under nitrogen protection for 24 hours, and then the Leu-NCA monomer and CH 3 O-PEG-NH 2 Add the Leu-NCA monomer with a molar ratio of 40:1, and continue the constant temperature reaction for 48 hours under nitrogen and protection. After the reaction, add 20 times the volume of ether in the reaction system to precipitate, filter, and dry to obtain PEG-PLysZ-PLeu3 block copolymers.

[0046] Dissolve the PEG-PLysZ-PLeu polymer obtained above in trifluoroacetic acid at 0°C, add HBr / H...

example 2

[0048] The amphiphilic tri-block copolymer is the carboxypolyethylene glycol-polylysine-polyleucine tri-block copolymer prepared in Example 1.

[0049] Prepare a docetaxel solution with a concentration range of 0.5 mg / ml and an amphiphilic triblock copolymer solution with a concentration range of 2 mg / ml, mix 100 μl of the docetaxel solution with 1 ml of the amphiphilic triblock copolymer solution, A mixed solution was obtained.

[0050] Add 1ml of ultrapure water dropwise to the mixed solution, then place the resulting mixed solution in a dialysis bag with a molecular cut-off of 3500, and dialyze in 2000ml of ultrapure water at room temperature for 24 hours to obtain a polymer composite containing docetaxel body.

[0051] Prepare a Bcl-2 siRNA diethyl pyrocarbonate aqueous solution with a concentration of 100 μg / ml, mix 0.5 μg of the polymer complex containing docetaxel with 1 μl of Bcl-2 siRNA diethyl pyrocarbonate aqueous solution at room temperature, Static and co-incuba...

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Abstract

The invention relates to drug-loading nano-micelles, and a preparation method and an application thereof. According to the to drug-loading nano-micelles, a polyethylene glycol derivative-polylysine-polyleucine amphiphilic triblock copolymer is adopted as a carrier, and self-assembly is carried out in a water solution, such that nano-micelles with a three-layer structure transferring gene and medicine are formed. With the hydrophobic effect between polyleucine, the copolymer forms a core of the micelles in water, such that a hydrophobic medicine docetaxel is entrapped. With polylysine, the nano-micelles are positively charged, such that negatively charged anti-apoptotic protein small interfering RNA can be bonded. Polyethylene glycol is used for protecting the stability of the nano-micelles loading the medicines and gene, and a cycle time of the nano-micelles in vivo is prolonged. The nano-micelles are used for loading both an anti-apoptotic protein small interfering RNA gene medicine and a docetaxel medicine, such that the gene treatment medicine and the chemotherapeutic medicine cooperates in treating cancer, and a synergetic effect of the two medicines can be developed. Therefore, a direction is provided for better treatment of breast cancer.

Description

technical field [0001] The invention relates to the field of nanomedicine, in particular to a drug-loaded nano-micelle and its preparation method and application. Background technique [0002] Traditionally, a variety of delivery systems that can simultaneously carry genes and chemotherapy drugs have been developed. For example, Meng et al. used mesoporous silica nanoparticles to connect polyethyleneimine (PEI) and simultaneously carried P-glycoprotein small interfering RNA (Pgp siRNA) and doxorubicin, which effectively enhanced the uptake of drug-resistant tumor cells to doxorubicin and induced apoptosis; Cao et al. synthesized a diblock copolymer to jointly load Bcl-2siRNA and doxorubicin, Effectively inhibit the growth of liver cancer cells. However, the above-mentioned drug-loading systems generally have biomembrane permeability and toxicity problems, and the efficiency of loading drugs or genes is not high. Contents of the invention [0003] Based on this, it is nec...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K48/00A61K31/337A61K47/34A61P35/00
Inventor 蔡林涛郑翠芳邓吉喆龚萍郑明彬易虎强
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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