Glaucocalyxin A-carrying bilirubin albumin nanoparticles and preparation method and application thereof

A technology of albumin nanoparticles and cyanine A, which is applied in the direction of non-active ingredients of polymer compounds, powder delivery, drug combination, etc., to achieve the effect of improving poor water solubility and good application prospects

Inactive Publication Date: 2016-07-27
上海泰申医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, there is no report on the application of cerulein A albumin nanoparticles in the solubilization, sustained release and targeting of drugs.

Method used

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  • Glaucocalyxin A-carrying bilirubin albumin nanoparticles and preparation method and application thereof
  • Glaucocalyxin A-carrying bilirubin albumin nanoparticles and preparation method and application thereof
  • Glaucocalyxin A-carrying bilirubin albumin nanoparticles and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Organic phase preparation: disperse the cerulein A drug (13.33%) in the organic phase;

[0053] Water phase preparation; adjust the pH to 4.0 with deionized water, add albumin (1%) to fully dissolve;

[0054] Slowly inject the organic phase into the water phase while dispersing at high shear (32000rpm, 5min) to obtain colostrum;

[0055] The colostrum was subjected to high-pressure homogenization (8000psi, 8 times) to obtain uniformly dispersed cyanine-loaded albumin nanoparticles;

[0056] The obtained cyanine-loaded albumin nanoparticles were vacuum rotary evaporated at 40° C. for 60 minutes to remove the organic phase; the cyanine-loaded albumin nanoparticles were filtered through a 0.22 μm carbonate sterile filter.

[0057] The nanoparticle suspension was measured by a Malvern particle size analyzer, and its average particle diameter was 84.77±2.050nm, its Zeta potential was -17.73±3.772, its encapsulation efficiency was 22.69%, and its stability was less than 48h. ...

Embodiment 2

[0059] Organic phase preparation: disperse the cerulein A drug (26.66%) in the organic phase;

[0060] Water phase preparation; adjust the pH to 4.0 with deionized water, add albumin (1%) to fully dissolve;

[0061] Slowly inject the organic phase into the water phase while dispersing at high shear (32000rpm, 5min) to obtain colostrum;

[0062] The colostrum was subjected to high-pressure homogenization (16000psi, 16 times) to obtain uniformly dispersed scutellarin-loaded albumin nanoparticles;

[0063] The obtained cyanine-loaded albumin nanoparticles were vacuum rotary evaporated at 40° C. for 60 minutes to remove the organic phase; the cyanine-loaded albumin nanoparticles were filtered through a 0.22 μm carbonate sterile filter.

[0064] The nanoparticle suspension was measured by a Malvern particle size analyzer, and its average particle diameter was 121.07±31.13nm, its Zeta potential was -21.20±2.514, its encapsulation efficiency was 39.68%, and its stability was less th...

Embodiment 3

[0066] Organic phase preparation: disperse the cerulein A drug (40%) in the organic phase;

[0067] Water phase preparation; adjust the pH to 4.0 with deionized water, add albumin (1%) to fully dissolve;

[0068] Slowly inject the organic phase into the water phase while dispersing at high shear (32000rpm, 5min) to obtain colostrum;

[0069] The colostrum was subjected to high-pressure homogenization (24000psi, 24 times) to obtain uniformly dispersed scutellarin-loaded albumin nanoparticles;

[0070] The obtained cyanine-loaded albumin nanoparticles were vacuum rotary evaporated at 40° C. for 60 minutes to remove the organic phase; the cyanine-loaded albumin nanoparticles were filtered through a 0.22 μm carbonate sterile filter.

[0071] The nanoparticle suspension was measured by a Malvern particle size analyzer, and its average particle diameter was 191.77±19.25nm, its Zeta potential was -20.1±0.860, its encapsulation efficiency was 53.23%, and its stability was less than 4...

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Abstract

The invention relates to the field of pharmaceutical preparations, in particular to glaucocalyxin A-carrying bilirubin albumin nanoparticles, a preparation method thereof and application of the nanoparticles in breast cancer treatment.The prepared glaucocalyxin A-carrying bilirubin albumin nanoparticles can overcome the defects that glaucocalyxin A is poor in water solubility and is quickly removed in a body and difficult to administrate through the characters of slow releasing and targeting of albumin nanoparticles.The glaucocalyxin A-carrying bilirubin albumin nanoparticles have very good application prospects in aspects of medicine solubilizing, slow releasing, targeting and the like.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a santrin-loaded albumin nanoparticle, a preparation method thereof, and an application in treating breast cancer. Background technique [0002] Glaucocalyxin A (GLA) is a natural kaurene-type diterpene compound, which has various biological activities such as antibacterial, anticoagulant, antioxidant, immunosuppressive, and cardiovascular protection. In recent years, more and more studies have shown that cyanine A has anti-cancer effects such as breast cancer, liver cancer, uterine cancer, and lung cancer. [0003] However, cyanine A has poor water solubility, difficulty in administration, and rapid metabolism in the body. For example, it can be metabolized into hydroxyl or dihydroxy products in liver microsomes, and can be metabolized into isomerized products in bile, so it takes a long time to grow up. Dosage is required to produce a therapeutic effect. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/122A61K47/42A61P35/00
CPCA61K9/146A61K31/122
Inventor 钟延强孙笃新王强迟晴晴张翮张国庆
Owner 上海泰申医药科技有限公司
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