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Hypocrellin B nanoparticle and preparation method thereof

A kind of Bamboo Rhododendron B, nanoparticle technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve problems such as direction transfer, and achieve the effect of good dispersibility, uniform morphological rules, and improved water solubility.

Active Publication Date: 2015-12-09
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0009] The Chinese patent "Preparation Method of Water-Soluble Hypocretin Titanium Dioxide Nanoparticles" has developed a titanium dioxide-based hypocretin nanoparticle that improves stability and singlet oxygen yield, but the titanium dioxide used in the patent is in After intravenous injection into the human body, it is difficult to be completely metabolized and eliminated by the human body, and there are certain safety hazards
However, the nanoparticles prepared by this patent are mainly passively targeted in vivo, and it is difficult to achieve active targeted delivery of drugs

Method used

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  • Hypocrellin B nanoparticle and preparation method thereof
  • Hypocrellin B nanoparticle and preparation method thereof
  • Hypocrellin B nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Optimization of preparation conditions of Hypocretin B nanoparticles

[0037] 1. Investigation of preparation method

[0038] Rotary evaporation method, dialysis method and rotary evaporation dialysis method are used to prepare nanoparticles respectively. The solution of medicine and nanomaterials is added dropwise into water by rotary evaporation method, and the micellar solution is obtained by stirring at a certain speed. In the dialysis method, drugs and nanomaterials are directly loaded into dialysis bags, and micellar solutions are obtained through dialysis. The rotary dialysis evaporation method combines the two, the rotary evaporation method is the same as the above, the rotary evaporation solution is put into a dialysis bag, and dialyzed in water to obtain a micellar solution.

[0039] The nanoparticles prepared by different methods were observed by transmission electron microscope, and the results are shown in Table 1.

[0040] Table 1 The influ...

Embodiment 2

[0058] Embodiment 2: Preparation of blank nanoparticles

[0059] Accurately weigh 30 mg of the PEG-PLA mixture, dissolve it in 2 ml of organic solvent acetone or tetrahydrofuran, and prepare a 15 mg / ml organic solvent. In another 50ml beaker, add 20ml of ultrapure water, and under the condition of magnetic stirring at a certain speed (magnetic stirrer 2 gear, about 660rpm / min), use a 2ml injection needle to inject the organic solution containing nanomaterials at a rate of 20- Drop into pure water drop by drop at a speed of 30 drops / min, continue to stir for 2 hours, let it stand overnight at 4°C, then put the liquid into a dialysis bag (molecular weight cut-off 3500kDa), and then put it into a beaker filled with 1L ultrapure water During dialysis, the water was changed at 1h, 5h, 8h, 12h, 24h, 48h and 72h, and the organic solution was dialyzed out to obtain a milky white micellar solution.

[0060] The transmission electron microscope picture of the blank nanoparticle prepare...

Embodiment 3

[0061] Embodiment 3: Preparation of Hypocretin B Nanoparticles

[0062] Weigh polymer PEG-PLA27mg, weigh polymer folate-PEG-PLA3mg, make the ratio of the polymer with folic acid account for 10% of the total polymer, under dark conditions, accurately weigh hypocrellin B (HB) 1mg. Dissolve the accurately weighed HB and polymer with 1ml and 1ml of organic solvent tetrahydrofuran respectively, vibrate until completely dissolved, and then mix the two. Ultrasonic for 2-3min under 30-40W ultrasonic power, so that the drug organic solution and the polymer organic solution are evenly mixed, so as to prepare a drug-polymer organic solution with uniform concentration. Add 20ml of water into a 50ml beaker, and drop the organic solution into the pure water drop by drop at a speed of 25 drops / min under the condition of a certain speed of magnetic stirring (magnetic stirrer 2, about 660rpm / min). Continue to stir for 2 hours after completion to prevent micelles from sticking together, and l...

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Abstract

The invention discloses a preparation method of a hypocrellin B nanoparticle. The preparation method includes: (1), dissolving a carrier polymer in an organic solution to obtain a solution A with the concentration of 10-20mg / ml; (2), dissolving hypocrellin B in an organic solution to obtain a solution B with the concentration of 1-2mg / ml; (3), evenly mixing the solution A with the solution B according to a volume ratio of (1-14):1 to obtain a drug polymer organic solution with the uniform concentration; (4), dripping the drug polymer organic solution prepared in the step (3) in water while stirring, and performing standing for 12-24 hours to obtain a micellar solution, wherein the volume ratio of the drug polymer organic solution to the water is 1:(10-30); (5), transferring the micellar solution into a dialysis bag, putting the dialysis bag in water for dialysis, and dialyzing the organic solution to obtain the hypocrellin B nanoparticle. The hypocrellin B nanoparticle prepared according to the method is spherical and regular morphologically, high in dispersity, uniform and not sticky when being observed by a transmission electron microscope.

Description

technical field [0001] The invention relates to a hypocrellin B nanoparticle and a preparation method thereof. Background technique [0002] Photodynamic therapy (Photodynamic therapy, PDT) is a treatment method with good application prospects. It refers to a treatment method in which the photosensitizer is irradiated by a sensitizing light source to cause a photosensitive chemical reaction to generate active oxygen, thereby destroying the diseased tissue. The photosensitizer itself can selectively gather in the diseased tissue, and the irradiation light source can be limited to the diseased part during treatment to achieve double selection. The advantage of PDT is that it can selectively kill diseased tissue, has low toxicity, can be applied repeatedly, and can also be used in combination with surgery and other treatments. Applying PDT to the treatment of tumors is also a hot spot now. [0003] Photosensitizers are an important part of photodynamic therapy. Hypocretin B...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/14A61K47/22A61P35/00
Inventor 宋坤孔北华鲁再君李钊苑存忠
Owner SHANDONG UNIV QILU HOSPITAL
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