Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of protein nanoparticle for in vivo delivery of pharmacologically active agent

A pharmacologically active, nanoparticle technology, applied in the field of protein nanoparticles, can solve problems such as loss of protein activity and inability to deliver in vivo

Active Publication Date: 2011-05-11
NANJING UNIV +1
View PDF6 Cites 58 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical purpose of the present invention is to provide a method for preparing protein nanoparticles for in vivo delivery of pharmacologically active substances, to solve the problem that some pharmacologically active substances cannot be delivered in vivo due to their hydrophobic properties, and the protein activity after forming nanoparticles lost problem

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of protein nanoparticle for in vivo delivery of pharmacologically active agent
  • Preparation method of protein nanoparticle for in vivo delivery of pharmacologically active agent
  • Preparation method of protein nanoparticle for in vivo delivery of pharmacologically active agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1. Preparation of paclitaxel-albumin nanoparticles

[0076] 100 mg HSA was dissolved in 10 mL pH6 phosphate buffer containing 0.5 mg / mL EDTA and 0.05 M mercaptoethanol, and the reaction was continued at 55°C for two hours. After the end, the protein was precipitated and washed with 5% trichloroacetic acid, and 1.6 mL of 10 mg / mL paclitaxel (dissolved in ethanol) solution into the pellet, mix for 2 minutes, add 50 mL of 0.08 M phosphate buffer and stir to dissolve the mixture. The obtained suspension is transparent, and the average particle size of the drug-loaded particles is 80-200 nm (BIC 90plus Particle Size Analyzer). The encapsulation efficiency of paclitaxel was determined by a reversed-phase C18 column, the mobile phase was acetonitrile: water (60:40), and the detection wavelength was 227 nm. HPLC analysis showed that the encapsulation efficiency of paclitaxel in this experiment was over 90%.

[0077] In the experiment, TCA can also be replaced by ot...

Embodiment 2

[0078] Example 2. Preparation of paclitaxel-albumin nanoparticles

[0079] 100 mg HSA was dissolved in 50 mL pH7.4 TRIS buffer, in a 37°C water bath, 350 μL 2-mercaptoethanol was added, the reaction lasted for 10 minutes, and 2 mL 10 mg / mL paclitaxel (dissolved in ethanol) was added. After 30 min, samples were dialyzed against pH 7.4 TRIS buffer for 24 h and the resulting samples were lyophilized for 48 h. The resulting lyophilized block sample can be easily redissolved into the original solution with water or saline, and the particle size of the nanoparticles remains unchanged. After lyophilization, the particle size mainly distributed in the range of 80-200 nm (BIC 90plus Particle Size Analyzer). HPLC analysis showed that the encapsulation efficiency of paclitaxel in this experiment was over 90%.

Embodiment 3

[0080] Example 3. Preparation of paclitaxel-albumin nanoparticles

[0081] 100 mg of paclitaxel was dissolved in 10 mL of pH 4.8 buffer solution, placed in an ice-water bath for 30 minutes, then 7.5 mL of 0°C pre-cooled acetone was added dropwise, and the ice bath was continued for 1 hour. Centrifuge to collect the precipitate, add 1 mL of 10 mg / mL paclitaxel (dissolved in acetone) to the precipitate, ultrasonically mix, add 50 mL of normal saline, and stir magnetically to form a suspension. Particle size analysis was carried out with BIC 90plus Particle Size Analyzer, and the result was 150-220 nm. The freeze-dried sample could be reconstituted, and the drug loading was 8.34% according to HPLC analysis.

[0082] Additional experiments show that glycine, mannitol, lactose and trehalose can all be used as lyoprotectant, and the particle size obtained by using lactose as lyoprotectant is the smallest.

[0083]During the preparation, we investigated different buffers (water, ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention provides a preparation method of protein nanoparticles for in vivo delivery of pharmacologically active agents, wherein the methods are to encase pharmaceutically active agents into proteins or peptides to form nanoparticles by unfolding the protein, and subsequently refolding or assembling the protein to produce a pharmacologically active agent encased within a protein nanoparticle.

Description

technical field [0001] The invention relates to a method for preparing protein nanoparticles for delivering pharmacologically active substances in vivo, and belongs to the field of in vivo delivery of pharmacologically active substances and their clinical applications. Specifically, the present invention is a method for encapsulating pharmacologically active substances into proteins by unfolding and refolding or self-assembling methods of proteins and polypeptides to form nanoparticles. Background technique [0002] Intravenous administration can quickly and directly act on the body. In order to reduce the side effects of intravenous administration, one of the effective methods is to encapsulate pharmacologically active substances into micron or nanoscale particles. On the one hand, the intravenously injected particles can release the pharmacologically active substances slowly and prolong the half-life of the pharmacologically active substances; on the other hand, the targe...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/42A61K31/337A61P35/00
CPCA61K9/5138A61K9/5192A61K31/337A61K9/19A61P35/00
Inventor 胡一桥吴锦慧丁大伟汤晓雷袁阿虎
Owner NANJING UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com