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Total bufadienolides solid lipid nanoparticle drug delivery system for injection and preparation method thereof

A technology of solid lipid nanometer and total bufolide, which is applied to the digestive system, medical formulas, medical preparations of non-effective ingredients, etc., can solve problems such as poor intravenous infusion, redness and swelling at the infusion site, and improve biological Utilization, reducing vascular irritation, and ensuring drug safety

Active Publication Date: 2015-10-28
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the course of clinical application, vascular irritation adverse reactions such as poor intravenous infusion, redness and swelling at the infusion site, and pain in the vein often occur.

Method used

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  • Total bufadienolides solid lipid nanoparticle drug delivery system for injection and preparation method thereof
  • Total bufadienolides solid lipid nanoparticle drug delivery system for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～10

[0065] Examples 1-10 This example mainly describes the hot and high-pressure homogenization method. The components specified in Table 1 were prepared according to the following steps to obtain bufolide solid lipid nanoparticles of different embodiments.

[0066] (1) Heating the total toad toad lactone extract, lipid material and fat-soluble emulsifier to melting at the temperature shown in Table 2, to dissolve or disperse in the lipid to obtain a melt as an oil phase;

[0067] (2) Disperse the water-soluble emulsifier, antioxidant, and glucose in 100ml of water for injection to form a uniform water phase;

[0068] (3) Mix and stir the oil phase obtained in (1) and the water phase obtained in (2) at the temperature and rotating speed shown in Table 2 until uniform colostrum is formed;

[0069] (4) Transfer the colostrum prepared in (3) to a milk homogenizer, homogenize in a high-pressure milk homogenizer, and rapidly cool to room temperature or below to obtain total bufolide s...

Embodiment 11

[0078] The physical and chemical properties of the total bufolide solid lipid nanoparticles prepared in Examples 1-10 above were taken.

[0079] Take an appropriate amount of total bufotoxin solid lipid nanoparticle suspension, dilute it with water, then drop it on the copper grid covered with carbon film, stain with 2.0% sodium phosphotungstate negative staining solution, and observe the nanoparticles under a transmission electron microscope form and take photos.

[0080] As a result, the nanoparticles were observed under the electron microscope as spherical solid particles with uniform particle size and no aggregation and adhesion phenomenon.

Embodiment 12

[0082] The total bufolide solid lipid nanoparticles in the above-mentioned Examples 1-10 were taken to measure the encapsulation efficiency and drug loading capacity.

[0083] Total bufolide solid lipid nanoparticles and free drug were separated by sephadex glucose gel column chromatography, and the encapsulation efficiency was determined. Draw 1 ml of the nanoparticle suspension onto the column, and use distilled water as the elution medium for elution. Collect the eluate with opalescent part, quantitatively absorb this part of the eluate, add methanol to dissolve the nanoparticles; take another 1 ml of nanoparticle suspension, add methanol to dissolve. The encapsulation efficiency and drug loading were determined by HPLC.

[0084] The particle size, encapsulation efficiency and drug loading of total bufolide solid lipid nanoparticles measured in Examples 11-12 are shown in the following table:

[0085] table 3

[0086] Example Particle size (nm) Encapsulation...

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Abstract

The invention belongs to the field of pharmaceutical preparation, and relates to a total bufadienolides solid lipid nanoparticle drug delivery system for injection and a preparation method thereof. Total bufadienolides solid lipid nanoparticles are composed of the components in parts by weight: 0.1-2 parts of total bufadienolides with therapeutically effective amount, 0.5-20 parts of a lipid material, 0.5-15 parts of a lipid soluble emulsifier, 0.5-10 parts of a water soluble emulsifier, 0.002-2.5 part of an antioxidant, 0.1-25 parts of sugar and a proper amount of water for injection. The total bufadienolides solid lipid nanoparticles for injection allow the total bufadienolides to be wrapped in a lipoid nucleus, increase the solubility of the total bufadienolides, reduce the irritation, avoid degradation or leakage of the drug, can achieve targeting effect, controlled release and other effects, and have the advantages of stable physical and chemical properties and the like.

Description

technical field [0001] The invention relates to a total bufolide nano-preparation, in particular to a total bufolide solid lipid nanoparticle delivery system for injection and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Total bufolides are a class of C-24 steroids or their glycosides connected with an α-pyrone ring (αpyrone) at the C-17β position. The main medicinal ingredient with anticancer activity. Total bufotalin mainly contains resibufogenin, cinobufagin, bufalin, bufotalin, and bufotalin-3-semisuberic acid Esters (Gamabufotalin-3-hydrogen Suberate), bufalin-3-succinyl arginate, cinobufotalin-3-succinyl arginate and other lactone components. Studies have shown that total bufotoxin has obvious anti-tumor effects, and can also transform tumor cells into normal cells (induce tumor cell differentiation), induce tumor cell apoptosis, inhibit tumor cell angiogenesis, and reduce tumor metastasis, etc. ....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K35/65A61K47/14A61P35/00A61P1/16A61P31/20
Inventor 何勇高永好吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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