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Glomerulus-targeted protein nanoparticle pharmaceutical composition and application thereof

A nanoparticle and glomerulus technology, which is applied in the field of medicine, can solve the problems of cumbersome preparation process, in vivo toxicity, cumbersome and complicated methods, etc., and achieve the effect of simple and easy preparation technology, reducing toxic and side effects, and improving therapeutic effect

Active Publication Date: 2016-09-21
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The prior art document CN103690957A discloses a glomerulus-targeted microparticle drug delivery system and its preparation method, although it successfully constructs the kidney glomerulus after modifying the microparticles (liposomes, nanoparticles, micelles) with PEGylated amidines. Ball-targeted microparticle drug delivery system, but there are still many deficiencies in the prior art: first, the prepared microparticle drug delivery system is a cationic microparticle drug delivery system, and there is a risk of in vivo toxicity. A large number of literature reports have confirmed that as a carrier Cationic liposome itself can produce strong cytotoxicity to various cells, and the higher the charge, the greater the toxicity. Obviously, this microparticle drug delivery system has certain defects in safety, which is not conducive to clinical drug use; secondly, this The composition of the microparticle drug delivery system is complicated, the preparation process is cumbersome, and the preparation cost is high, and it is not yet possible for industrialized mass production
Obviously, the protein nanoparticles prepared by this traditional method have poor biodegradability and high toxicity, especially the residual organic solvents such as glutaraldehyde will cause the inactivation of biologically active macromolecules and increase the risk of toxic side effects in the body
Moreover, this method is cumbersome and complicated, and takes a long time, especially the cross-linking curing takes more than 24 hours, and the time cost is high
In summary, the applicant believes that it is not feasible to apply the tripterine pharmaceutical composition with albumin as a pharmaceutical carrier to the glomerulus-targeted drug delivery system

Method used

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  • Glomerulus-targeted protein nanoparticle pharmaceutical composition and application thereof
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  • Glomerulus-targeted protein nanoparticle pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Preparation and characterization of human serum albumin nanoparticle tripterine composition and human serum albumin nanoparticle prednisolone composition by ultrasonic method

[0079] Dissolve tripterine 7mg or prednisolone 20mg and water-insoluble stabilizer soybean oil 50mg in 2mL dichloromethane:ethyl acetate (7:3, V / V), and then distill with 10mL human serum albumin Mix the aqueous solution (2%W / V), in an ice bath, ultrasonic power 500W (3s / 5s) for 8min, and then remove the organic mixed solvent by rotary evaporation under reduced pressure at 37°C to obtain human serum albumin nanoparticles tripterine composition and human serum albumin nanoparticle prednisolone composition. The particle size and potential were measured by a Malvern particle sizer, the morphology was characterized by a transmission electron microscope, and the encapsulation efficiency was determined by a Sephadex column method.

[0080] result:

[0081] As shown in Table 1, the prepared human seru...

Embodiment 2

[0085] Preparation of human serum albumin nanoparticle tripterine composition and human serum albumin nanoparticle prednisolone composition by high pressure homogenization method

[0086] Dissolve tripterine 7mg or prednisolone 20mg in 2mL dichloromethane:ethyl acetate (7:3, V / V), and then mix with 10mL human serum albumin (2%W / V) and water-soluble Solutol HS-15 40mg double-distilled aqueous solution was mixed, and the probe was ultrasonicated 15 times in an ice bath, and the obtained suspension was transferred to a high-pressure homogenizer, and the nanoemulsion was obtained by circulating and homogenizing 15 times in a pressure range of 15000Psi. Under reduced pressure at 37°C, the organic mixed solvent was removed by rotary evaporation to obtain the human serum albumin nanoparticle tripterine composition and the human serum albumin nanoparticle prednisolone composition, with an average particle size of about 100nm and a PDI Both are below 0.2.

Embodiment 3

[0088] Preparation of human serum albumin nanoparticle tripterine composition and human serum albumin nanoparticle prednisolone composition by microfluidic method

[0089] Dissolve tripterine 7mg or prednisolone 20mg and water-insoluble stabilizer medium-chain oil 50mg in 2mL dichloromethane:ethyl acetate (7:3, V / V), and then mix with 10mL human serum albumin (2 %W / V) and water-soluble stabilizer Solutol HS-15 40mg double-distilled aqueous solution mixed, the probe was ultrasonicated 15 times in an ice bath, the obtained suspension was transferred to a high-pressure homogenizer, and circulated within a pressure range of 20000Psi The nanoemulsion was obtained after 15 times of melting, and then the organic mixed solvent was removed by rotary evaporation under reduced pressure at 37°C, and the human serum albumin nanoparticle tripterine composition and the human serum albumin nanoparticle prednisolone composition were obtained. The average particle size is around 90nm, and the P...

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Abstract

The invention provides a glomerulus-targeted protein nanoparticle pharmaceutical composition and an application thereof. The protein nanoparticle pharmaceutical composition is mainly prepared from a protein ingredient, a pharmacological active substance and a stabilizer, and the grain size of the protein nanoparticle pharmaceutical composition ranges from 10nm to 170nm. With the application of the pharmaceutical composition, passive targeted drug delivery of glomerular mesangial cells is achieved, and the aggregation concentration of a drug in a glomerulus is obviously improved or the aggregation duration of the drug in the glomerulus is prolonged, so that the curative effect of the drug is remarkably improved, and meanwhile, the toxic and side effects of the drug on a non-targeted part are greatly reduced.

Description

technical field [0001] The invention relates to a glomerulus-targeted protein nanoparticle pharmaceutical composition and a preparation method and application thereof, belonging to the technical field of medicine. Background technique [0002] Glomerular diseases, including primary and secondary glomerulonephritis, are the main causes of chronic renal failure and end-stage renal disease, and are seriously threatening human health. According to statistics, in my country, glomerular diseases account for 54.4% of the causes of end-stage renal disease, of which glomerulonephritis accounts for 48.1%. Most glomerular diseases are immune-mediated inflammatory diseases. Therefore, immunomodulatory therapy is an important means for the treatment of immune-mediated glomerular inflammatory diseases. Currently, glucocorticoids and immunosuppressants are the main treatments in clinical practice. However, these two drugs have obvious side effects, such as femoral head necrosis and Cushin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K9/14A61K31/56A61K31/573A61P13/12A61P9/00A61P35/00A61P37/06
CPCA61K9/146A61K31/56A61K31/573
Inventor 张志荣龚涛郭玲孙逊
Owner SICHUAN UNIV
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