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Preparation method and application of targeted co-supported drug delivery system nano-particles based on polylactic-co-glycolic acid

A technology of glycolic acid copolymer and delivery system, which is applied in the field of medicine, can solve problems such as no public reports, and achieve huge economic and social benefits and good use effects

Inactive Publication Date: 2014-03-12
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So how to realize the targeted co-loaded drug delivery system based on PLGA copolymer, and realize the application in brain tumor targeted therapy drugs, there is no public report so far

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (1), the preparation of chitosan-angiopep-2 polymer, the method is:

[0037] a. Add 20 mg of chitosan into 8 mL of acetic acid solution with a volume concentration of 20%, ultrasonically dissolve it at a power of 500 W for 30 minutes, and adjust the pH value to 6.0 with 5M (5mol / L) NaOH solution to obtain a chitosan solution;

[0038] b. Add 5 mg of 3-maleimide propionic acid-N-hydroxysuccinic acid imide ester to the chitosan solution, and react under nitrogen protection at 30°C and 100r / min magnetic stirring for 48 hours. After the reaction is completed, the reaction The solution was placed in a dialysis bag with a molecular weight cut-off of 8kD-14kD and dialyzed in 1000mL PBS for 60h to remove unreacted 3-maleimide propionic acid-N-hydroxysuccinimidyl ester to obtain a dialysate;

[0039] c. Weigh 5 mg of Angiopep-2 and dissolve it in 20 mL of ultrapure water, add 10 mg of Traut's reagent, sonicate for 1 hour at a temperature of 50°C, so that the end of Angiopep-2 ha...

Embodiment 2

[0042] Synthesis of chitosan-angiopep-2 polymer

[0043] 1) Weigh 20mg of chitosan, add 8mL of 20% acetic acid solution, dissolve with 500W ultrasonic, adjust the pH to 6.0 with 5M NaOH;

[0044] 2) Add 5 mg of N-hydroxysuccinimide 3-maleimide propionate to the above chitosan solution, heat at 30°C under nitrogen protection, and react with magnetic stirring at 100 r / min for 48 hours. After the reaction is completed, The reaction solution was placed in a dialysis bag with a molecular weight cut-off of 8kD-14kD and dialyzed in 1000mL PBS to remove unreacted N-hydroxysuccinimidyl 3-maleimide propionate, and dialyzed for 60h;

[0045] 3) Take out the solution in the dialysis bag, add Angiopep-2 whose end is cysteine ​​(a cysteine ​​is added to the carboxyl end when synthesizing Angiopep-2), heat and stir under nitrogen protection to make it fully react, Angiopep -2 Modified chitosan was placed in a dialysis bag with a molecular weight cut-off of 8kD-14kD and dialyzed in 1000mL PB...

example 3

[0047] Preparation of targeting PLGA nanoparticles co-loaded with doxorubicin hydrochloride and EGFR siRNA

[0048] 1) Weigh 100mg of PLGA (polylactide: glycolide = 50:50, molecular weight 17kD), dissolve in 10mL acetone to prepare PLGA stock solution (10mg / mL), weigh 15mg of doxorubicin hydrochloride, dissolve in In 5mL of methanol, obtain doxorubicin hydrochloride stock solution (3mg / mL);

[0049] 2) Weigh 1g of bovine serum albumin, add it into 100mL of RNase-free aqueous solution with a pH value of 6, after it is completely dissolved, add 62.5mg of chitosan-Angiopep-2, dissolve it completely by ultrasonic, and use it as the water phase;

[0050] 3) Take 5mL doxorubicin hydrochloride stock solution, add it to 10mL PLGA stock solution (10mg / mL), sonicate for 1min, as the oil phase, add 60mL water dropwise to the oil phase at a speed of 1mL / min under stirring (100rpm) Phase, and then probe ultrasound (power 200W, working time 3s, intermittent time 6s, working times 20 times)...

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Abstract

The invention relates to a preparation method and application of targeted co-supported drug delivery system nano-particles based on polylactic-co-glycolic acid (PLGA), which can effectively solve the problem of preparing the targeted co-supported drug delivery system nano-particles based on polylactic-co-glycolic acid, and realizes the application in cerebral tumor targeted treatment medicines. The method comprises the following steps: connecting Angiopep-2 by utilizing the reactive amino group on chitosan: reacting chitosan with 3-maleimidopropionic acid N-hydroxysuccinimide to enable the amino terminal of chitosan to have maleimide; reacting with terminal-sulfhydrylated Angiopepe-2 to obtain a chitosan-angiopep-2 polymer. The polymer can be applied to preparation of a PLGA-based targeted co-supported drug delivery system. The method is stable and reliable, the product has a good using effect, small-molecular chemical drugs and genetic drugs can be delivered at the same time, or a fluorescent probe can pass through a blood brain barrier and enters the brain while chemotherapeutic drugs are delivered, and targeted cerebral tumor treatment can be synergized or targeted cerebral tumor treatment and diagnosis can be integrated into a whole.

Description

technical field [0001] The invention relates to medicine, in particular to a preparation method and application of nanoparticles of a targeted co-loaded drug delivery system based on polylactic acid-glycolic acid copolymer. Background technique [0002] Polylactic-co-glycolic acid copolymer (poly lactic-co-glycolic acid, PLGA, or polylactide-glycolide copolymer), is polymerized from two monomers - lactic acid and glycolic acid. The degraded functional polymeric organic compound has good biocompatibility, non-toxicity, good encapsulation and film-forming properties, and is widely used in pharmaceuticals, medical engineering materials and modern industrial fields. In the United States, PLGA has passed FDA certification and has been officially included in the United States Pharmacopoeia as a pharmaceutical excipient. It has become one of the favored carrier materials in recent years and is widely used in the fields of drug carriers and medical bioengineering materials. eventu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K48/00A61K47/42A61K47/34A61K49/00A61K9/14A61P35/00
Inventor 王蕾郝永伟张云赵亚林孟德辉李懂史进进张振中
Owner ZHENGZHOU UNIV
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