Multifunctional nano-drug composition and preparation method thereof

A nano-drug, multi-functional technology, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of single treatment method, poor treatment effect, inability to solve drug tolerance problems, etc., to improve treatment efficiency, load high dose effect

Active Publication Date: 2016-01-13
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the nanoparticle pharmaceutical compositions obtained by the currently disclosed preparation methods of nanoparticle pharmaceutical compositions are nanoparticle pharmaceutical compos...

Method used

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  • Multifunctional nano-drug composition and preparation method thereof
  • Multifunctional nano-drug composition and preparation method thereof
  • Multifunctional nano-drug composition and preparation method thereof

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preparation example Construction

[0032] The embodiment of the present invention also provides a preparation method of the above-mentioned multifunctional nanomedicine composition, which includes the following steps:

[0033] S01: the monomethoxy polyethylene glycol-polylactic acid-glycolic acid block copolymer (mPEG-PLGA) and / or polyethylene glycol-polylactic acid-glycolic acid block copolymer (PEG-PLGA) The polymer covalently bonded to the porphyrin compound is dissolved in the first water-immiscible organic solvent to obtain a modified porphyrin polymer solution;

[0034] S02: adding the aqueous solution of the hydrophilic drug to the polymer solution of the modified porphyrin, emulsifying, and obtaining colostrum;

[0035] S03: adding a surfactant and the hydrophobic drug dissolved in a second organic solvent to the colostrum, sonicating, removing the organic solvent under reduced pressure, and then centrifuging and washing to obtain the product.

[0036] Above-mentioned preparation method, wherein:

[0...

Embodiment 1

[0082] Mix 100 nmol of mPEG-PLGA, 50 nmol of protoporphyrin, 50 nmol of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, 25 nmol of 4-(dimethylamino)pyridine and 50 μL of N,N-Diisopropylethylamine was mixed in 10 mL of anhydrous dichloromethane, reacted at room temperature under argon protection for 48 hours, the product was dialyzed for 24 hours, and freeze-dried to obtain the mPEG-PLGA-porphyrin carrier;

[0083]Dissolve 20mgmPEG-PLGA-porphyrin in 1mL dichloromethane, add 0.2mL doxorubicin hydrochloride aqueous solution (7.5mg / mL), mix and sonicate for 3min, then add 2mL 2% polyvinyl alcohol aqueous solution, vortex and mix well , 0.2 mL of paclitaxel (5 mg / mL) dissolved in dichloromethane was added, and after ultrasonic emulsification for 8 min, the mixture was slowly added into 10 mL of 0.3% polyvinyl alcohol and stirred for 10 min. Evaporate under reduced pressure with a rotary evaporator to remove dichloromethane in the solution, centrifuge at 13,000 rpm for 10 min, and th...

Embodiment 2

[0085] 100 nmol of mPEG-PLGA, 100 nmol of chlorin e6, 50 nmol of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, 25 nmol of 4-(dimethylamino)pyridine and 50 μL of triethylamine in 10 mL of anhydrous Mix in dichloromethane, react at room temperature for 48 hours under the protection of argon, dialyze the product for 48 hours, and freeze-dry to obtain mPEG-PLGA-chlorin e6.

[0086] Dissolve 20 mg of mPEG-PLGA-chlorin e6 in 1 mL of dichloromethane, add 0.2 mL of doxorubicin hydrochloride aqueous solution (5 mg / mL), mix and sonicate for 5 min, then add 10 mL of 2% polyvinyl alcohol aqueous solution, and vortex Mix evenly, add 0.2mL paclitaxel (5mg / mL) dissolved in dichloromethane, then ultrasonic emulsify for 8min, evaporate under reduced pressure with a rotary evaporator to remove dichloromethane in the solution, centrifuge at 13000rpm for 10min, and then use deionized Centrifugal washing with water to obtain the multifunctional nano drug composition.

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Abstract

The invention provides a multifunctional nano-drug combination and a preparation method thereof. The combination comprises a carrier and active ingredients loaded on the carrier, wherein the carrier is a polymer formed by mPEG-PLGA and/or PEG-PLGA and a porphyrin compound through covalent-bond connection, and the active ingredients include hydrophobic and hydrophilic drugs. Preferentially, the carrier and the active ingredients loaded on the carrier form particles with the nano size of 50-1000 nm. The multifunctional nano-drug combination has photo-thermal effect so that the treatment efficiency can be improved based on traditional chemotherapy in combination with photo-thermal therapy, and the multifunctional nano-drug combination can be applied to cancer therapy drugs.

Description

technical field [0001] The invention belongs to the field of nanobiological medicine, and in particular relates to a multifunctional nanomedicine composition and a preparation method thereof. Background technique [0002] Nano-drug delivery system refers to the drug delivery system formed by drugs and nano-carriers with a particle size ranging from 1 to 1000 nm, including nanospheres, nanocapsules, nanoparticles and nanoliposomes. Compared with other drug carriers, the nano-drug delivery system has significant advantages: (1) ultra-small volume, which can pass through the smallest capillaries in the human body, and is not easily cleared by phagocytic cells, prolonging the residence time in the circulatory system; (2) ) reach target sites such as the liver, spleen, lung, bone marrow, and lymph where the reticuloendothelial system is concentrated; (3) can penetrate the interstitial space and be absorbed by cells, which is conducive to transdermal absorption and intracellular d...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K9/16A61K31/704A61K47/34A61P35/00A61K31/337
Inventor 聂广军吴雁苏世帅
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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