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Double-layer sustained and controlled release nanoparticle and preparation method thereof and application

A nanoparticle and double-layer technology, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, and medical preparations containing active ingredients. Drug delivery carrier and other issues, to achieve the effect of long-term drug circulation, improve drug targeting, and reduce excretion rate

Active Publication Date: 2013-11-06
XINXIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of preparing composite microspheres using chitosan as the outer layer, it is necessary to add the PLGA microsphere solution to the cationic chitosan solution first, and then carry out a crosslinking reaction with chitosan by adding an anionic crosslinking agent, thereby Chitosan is coated on the outer layer of PLGA microspheres, and there are two problems in this method: one, the Zeta potential of the prepared composite microspheres is close to neutral, and microspheres are easily aggregated in the dispersion, which is unfavorable for intravenous administration. Drug carrier; 2. The drugs in the outer layer, especially cytokines, are easy to denature and lose their activity
However, due to the limitations of existing drug carriers, anti-tumor angiogenesis drugs and chemotherapy drugs need to be prepared into different pharmaceutical preparations and administered separately, making it difficult to achieve the best therapeutic effect

Method used

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  • Double-layer sustained and controlled release nanoparticle and preparation method thereof and application
  • Double-layer sustained and controlled release nanoparticle and preparation method thereof and application
  • Double-layer sustained and controlled release nanoparticle and preparation method thereof and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: Preparation of double-layer sustained and controlled release nanoparticles of the present invention

[0055] 1. Preparation of polyethylene glycol monomethyl ether grafted chitosan (mPEG-g-CS)

[0056] (1) Weigh 1 g of chitosan, add it to 10 mL of formic acid solution with a mass concentration of 1.0%, and stir to dissolve it;

[0057] (2) Add 3 g of polyethylene glycol monomethyl ether, stir for 15 minutes, then add 10 mL of formaldehyde solution with a mass concentration of 6.0%, and stir magnetically for 12 hours;

[0058] (3) Transfer to a dialysis bag, dialyze with deionized water for 3 days, and freeze-dry for 12 hours;

[0059] (4) Take the freeze-dried sample, wash it with chloroform, drain it, dissolve it with 0.1mol / L hydrochloric acid, put it into a dialysis bag again, dialyze it with deionized water for 3 days, and freeze-dry it for 24 hours to obtain a white cotton-like mPEG- g-CS sample.

[0060] 2. Preparation of mPEG-g-CS--PLGA bilayer c...

Embodiment 2

[0065] Embodiment 2: Performance determination of the double-layer sustained and controlled release nanoparticles of the present invention

[0066] 1. Determination of the polyethylene glycol grafting rate in mPEG-g-CS

[0067] Dissolve 50 mg of chitosan and 50 mg of mPEG-g-CS with dry constant weight in 25 mL of distilled water, respectively, and prepare sample solutions with a mass concentration of 0.02%; accurately pipette 5 mL of the above solution into a conical flask, and add 0.2 M 2mL of hydrochloric acid solution and a drop of toluidine blue indicator, shake well. Titrate with polyvinyl alcohol potassium sulfate standard solution until the sample solution turns from blue to bright purple, and at the same time take 5mL of distilled water for blank control test. The amino group content was calculated by the following formula (NH 2 %), from which the grafting rate of polyethylene glycol was derived.

[0068] NH 2 % ...

Embodiment 3

[0083] Example 3: Preparation of double-layer sustained and controlled release drug-loaded nanoparticles of the present invention

[0084] (1) Dissolve 100mg of PLGA in 4mL of dichloromethane, add 0.5mL of vincristine sulfate aqueous solution with a concentration of 20mg / mL, and ultrasonically emulsify for 2 minutes under 60W power to form W1 / O type colostrum;

[0085] (2) Stir the W1 / O type colostrum prepared in step (1) into an aqueous polyvinyl alcohol solution with a mass concentration of 1.5% (containing Tween 20 with a mass concentration of 1%), and continue stirring at 200rpm for 4 Hours, form W1 / O / W2 type double emulsion, volatilize organic solvent to solidify, to PLGA nanoparticle solution;

[0086] (3) Take the PLGA nanoparticle solution prepared in step (2), filter it with a 0.8 μm filter membrane, collect the filtrate, centrifuge at a speed of 18000 rpm, collect the nanoparticles, and freeze-dry for 12 hours to obtain solid powder PLGA nanoparticle grain;

[0087...

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Abstract

The invention discloses a double-layer sustained and controlled release nanoparticle and a preparation method thereof and application in preparation of antitumor medicines. The double-layer sustained and controlled release nanoparticle is formed by a lactic acid-glycolic acid copolymer nanoparticle inner core and a polyethylene glycol questin grafting chitosan casing covering an outer layer of the lactic acid-glycolic acid copolymer nanoparticle inner core and can simultaneously load hydrophilic and lipophilic medicines. The drug entrapment rate is high, time-ordered release of inner layer medicines and outer layer medicines can be achieved, the double-layer sustained and controlled release nanoparticle has the effects of sustained release and controlled release, and in addition, the double-layer sustained and controlled release nanoparticle further has the advantages of being controllable in grain size, uniform in particle size distribution, smooth and round in forma and good in stability and dispersibility and the like.

Description

technical field [0001] The invention relates to a sustained and controlled release nanoparticle and its preparation method and application, in particular to a double-layer sustained and controlled release nanoparticle and its preparation method and application. Background technique [0002] As a new type of drug carrier, the nanoparticle drug delivery system can deliver the drug to the lesion in a targeted manner or specifically act on the target cells due to its special size and structure, and can maintain the slow release of the drug and prolong the half-life of the drug. And reduce toxic and side effects, etc., has been widely used in the field of biomedicine. [0003] Lactic acid-glycolic acid copolymer (PLGA) is a polymer organic compound formed by the polymerization of glycolic acid and lactic acid, and is currently considered to be one of the few mature biodegradable biomaterials in vivo. Because PLGA is easy to synthesize, stable in quality, and has the advantages o...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/36A61K47/34A61K31/475A61K31/337A61P35/00C08G81/00A61K47/10
Inventor 陈红丽杨万才刘涌涛鲍永华吕洁丽
Owner XINXIANG MEDICAL UNIV
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