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

Target nano lipid core micelle used for carrying docetaxel, and preparation method and applications thereof

A technology of docetaxel and nano-lipid, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, capsule delivery, etc., can solve problems that have not yet been seen, and achieve good social benefits and obvious sustained release effect, enhance the effect of treatment

Inactive Publication Date: 2014-01-15
SHANGHAI UNIV OF T C M
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In foreign patents, there are RGD-mediated magnetic nanoparticles of anti-tumor drugs (US7329638); RGD-mediated pH-sensitive or temperature-sensitive nanoparticles (US7371781); RGD-mediated perfluoronanoparticles for tumor imaging ( US7566442) and RGD-mediated cationic polymer nanoparticles (US2009142842A1) and other patents, but there have been no reports on RGD peptide-mediated lipid core micellar drug delivery systems using amphiphilic polymers as carrier materials

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
  • Target nano lipid core micelle used for carrying docetaxel, and preparation method and applications thereof
  • Target nano lipid core micelle used for carrying docetaxel, and preparation method and applications thereof
  • Target nano lipid core micelle used for carrying docetaxel, and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] At room temperature: Weigh 80 mg of PEG-DSPE and 2 mg of mal-PEG-DSPE and dissolve them in 7.8 mL of chloroform; weigh 2.05 mg of docetaxel and dissolve them in 1 mL of methanol; mix them well and then rotate them in a water bath at 38°C for 30 min; Freeze-dry at -45°C for 24 hours; hydrate with 8 mL of HBS (pH=7.4), shake for 10 minutes, then add 8 mL of HBS (pH=7.4) for dilution; filter with a 0.22 μm filter membrane to obtain loaded docetaxel Nano-lipid core micelle solution (unmodified);

[0034] Weigh 0.45 mg of RGD cyclic peptide and prepare a solution of about 0.3 mg / mL with 1.5 mL of HBS (pH=7.4); take 6 mL of the above-mentioned nano-lipid core micelles solution loaded with docetaxel, and stir under 1000 rpm magnetic force, Add 1 mL of RGD peptide solution dropwise; after the addition, continue to stir for 12 hours to obtain the targeted nano-lipid core micelles solution (modified by RGD) loaded with docetaxel.

[0035] 1. Morphological observation of the prep...

Embodiment 2

[0085] At room temperature: weigh 90mg of PEG-PE and 1.5mg of mal-PEG-PE and dissolve in 9mL of chloroform, weigh 3.05mg of docetaxel and dissolve in 1.5mL of methanol; mix the two and then spin evaporate in a water bath at 38°C for 30min ; freeze-dry at -45°C for 24 hours; hydrate with 8 mL of HBS (pH=7.4), shake for 10 min, then add 8 mL of HBS (pH=7.4) for dilution; Nano-lipid nucleus micellar solution of paclitaxel (unmodified);

[0086] Weigh 0.3 mg of RGD chain peptide and prepare a solution of about 0.3 mg / mL with 1 mL of HBS (pH=7.4); take 6 mL of the nano-lipid core micelle solution carrying docetaxel, and put it under magnetic stirring at 1000 rpm. Add 0.8 mL of RGD peptide solution dropwise; after the addition, continue to stir for 12 hours to obtain the targeted nano-lipid core micelles solution (modified by RGD) loaded with docetaxel.

Embodiment 3

[0088] At room temperature: weigh 80mg of PEG-DOPE and 1mg of mal-PEG-DOPE and dissolve in 7.8mL of chloroform, weigh 2.25mg of docetaxel and dissolve in 1.1mL of methanol; mix the two together and spin evaporate in a water bath at 38°C for 30min; Lyophilize at -45°C for 24 hours; hydrate with 8 mL of HBS (pH=7.4), shake for 10 min, then add 8 mL of HBS (pH=7.4) for dilution; filter with a 0.22 μm filter membrane to obtain the loaded polyene Paclitaxel nano lipid core micelles solution (unmodified);

[0089] Weigh 0.3 mg of RGD chain peptide and prepare a solution of about 0.3 mg / mL with 1 mL of HBS (pH=7.4); take 6 mL of the nano-lipid core micelle solution carrying docetaxel, and put it under magnetic stirring at 1000 rpm. Add 0.6 mL of RGD peptide solution dropwise; after the addition, continue to stir for 12 hours to obtain the targeted nano-lipid core micelles solution (modified by RGD) loaded with docetaxel.

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

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a target nano lipid core micelle used for carrying docetaxel, and a preparation method and applications thereof. The target nano lipid core micelle is obtained by RGD peptide surface modification of a nano lipid core micelle used for carrying docetaxel; the nano lipid core micelle used for carrying docetaxel is prepared via thin-film hydration method of a polyethylene glycol polymer with methoxyl end groups, a polyethylene glycol polymer with maleimide end groups and docetaxel. It is confirmed by experiment results that: the target nano lipid core micelle is of a uniform spherical shape, is composed of discontinuous nanoparticles, is small in particle size and uniform in distribution, is capable of changing pharmacokinetics characteristics of docetaxel, and possesses obvious sustained release effect, excellent compatibility with blood plasma, and no obvious toxicity on cells. In addition, the preparation method is simple, is suitable for scale production, and possesses relatively promising clinical application prospect and high social benefits.

Description

technical field [0001] The invention relates to a targeted nano-lipid core micelle carrying docetaxel, a preparation method and application thereof, and belongs to the technical field of targeted drug delivery. Background technique [0002] Docetaxel (Docetaxel), also known as Docetaxel, Docetaxel (trade name: Taxotere, Taxotere), is a compound synthesized from paclitaxel, a compound extracted from the needles of Taxus berry, and then undergoes structural modification. It is a white powdery solid, hardly soluble in water. This product is a new type of taxane anti-tumor drug. Its anti-tumor mechanism is the same as that of paclitaxel, which is through the formation of non-functional microtubule bundles, destroying mitosis and cell proliferation, but its activity is about twice that of paclitaxel, which is higher than that of existing drugs. The most effective single-agent chemotherapy drug for the treatment of metastatic breast cancer and non-small cell lung cancer (Breast C...

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): A61K9/51A61K9/14A61K47/34A61K47/16A61K31/337A61P35/00A61K47/10
Inventor 奉建芳胡凯莉陈王彦刘梅
Owner SHANGHAI UNIV OF T C M
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