Unlock instant, AI-driven research and patent intelligence for your innovation.

A long-circulation nano lipid carrier of doxorubicin derivatives and its preparation method

A nano-lipid carrier and derivative technology, which is applied in drug combination, pharmaceutical formula, liquid delivery, etc., can solve the problems of lack of sustained release effect, poor dissolution of preparations in vitro, short action time in vivo, etc., and prolong the circulation time in the body , Bioavailability improvement, effect of improving drug loading and encapsulation efficiency

Inactive Publication Date: 2015-08-19
SHANDONG UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The water-insoluble nature of Amoitone B makes its formulation poor in vitro dissolution, which seriously affects its absorption and distribution in the body, reduces its bioavailability, is easily metabolized by the liver, has a short biological half-life, and poor curative effect, which limits its clinical application.
[0006] CN102579373A discloses a nanocrystalline preparation of doxorubicinone derivatives to improve its solubility and dissolution rate, but it does not have a sustained release effect and the in vivo action time is short
Although it is a conventional technical means to make drugs into nano-lipid carriers, it is not easy to develop a preparation with long circulation, controllable drug release, good curative effect, good stability, low toxicity and good biocompatibility. Need to repeatedly explore the conditions and pay a lot of creative work

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
  • A long-circulation nano lipid carrier of doxorubicin derivatives and its preparation method
  • A long-circulation nano lipid carrier of doxorubicin derivatives and its preparation method
  • A long-circulation nano lipid carrier of doxorubicin derivatives and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 prepares Amoitone B long circulation nano lipid carrier

[0042] Proceed as follows:

[0043]Dissolve 10mg of Amoitone B, 70mg of PEG (40) stearate, 100mg of stearic acid, 40mg of oleic acid, and 200mg of soybean lecithin in 5ml of acetone, and heat to 75°C to completely dissolve to form an organic phase;

[0044] Dissolve 188250mg of poloxamer in 10ml of water for injection, and heat to 75°C to completely dissolve to form the water phase;

[0045] Inject the organic phase into the water phase at a temperature of 75°C and a stirring speed of 1000 r / min, and stir for 2.5 hours to completely volatilize the organic phase to obtain colostrum;

[0046] Pour the colostrum into 25ml of water at 0-2°C, and stir in an ice bath for 2 hours at a rotational speed of 1000r / min to obtain the Amoitone B long-circulation nano-lipid carrier.

Embodiment 2

[0047] Embodiment 2 prepares Amoitone B long circulation nano lipid carrier

[0048] Proceed as follows:

[0049] Dissolve 10 mg of Amoitone B, 80 mg of PEG (40) stearate, 80 mg of glyceryl monostearate, 40 mg of medium-chain triglycerides, and 150 mg of soybean lecithin into 5 ml of ethanol, and heat to 80°C to completely dissolve to form an organic phase;

[0050] Dissolve 188200mg of poloxamer in 15ml of water for injection, heat to 80°C to dissolve completely, and form the water phase;

[0051] Inject the organic phase into the water phase at a temperature of 80°C and a stirring speed of 1200 r / min, and stir for 3 hours to completely volatilize the organic phase to obtain colostrum;

[0052] Pour colostrum into 20ml of water at 0-2°C, and stir in an ice bath at a rotational speed of 1200r / min for 2 hours to obtain Amoitone B long-circulation nano-lipid carrier.

[0053] After diluting with water, observe its morphology with a H-7000 transmission electron microscope, as s...

Embodiment 3

[0054] Embodiment 3 prepares Amoitone B long circulation nano lipid carrier

[0055] Proceed as follows:

[0056] Dissolve 30 mg of Amoitone B, 250 mg of PEG (40) stearate, 250 mg of glyceryl monostearate, 100 mg of oleic acid, and 250 mg of lecithin in 10 ml of ethanol, and heat to 75°C to completely dissolve to form an organic phase;

[0057] Dissolve 300mg of sodium lauryl sulfate in 20ml of water for injection, heat to 75°C to dissolve completely, and form the water phase;

[0058] Inject the organic phase into the water phase at a temperature of 75°C and a stirring speed of 1000 r / min, and stir for 4 hours to completely volatilize the organic phase to obtain colostrum;

[0059] Pour the colostrum into 20ml of water at 0-2°C, and stir in an ice bath for 4 hours at a rotational speed of 1000r / min to obtain the Amoitone B long-circulation nano-lipid carrier.

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 an amoitone derivative long-circulation nanometer lipid carrier which comprises the following main components: crude medicine Amoitone B, polyoxyethylene glycol bisstearate, solid lipid material, liquid lipid material, fat-soluble emulsifier, water-soluble emulsifier and injection water. The preparation method of the amoitone derivative long-circulation nanometer lipid carrier is an emulsion evaporating-low temperature curing method. The amoitone derivative long-circulation nanometer lipid carrier prepared by the preparation method has a slow release function in the body, is capable of effectively prolonging the in-vivo retention time of the medicine and improving the bioavailability of the medicine, has higher encapsulation efficiency and medicine carrying amount and a grain size of about 200nm, and can be passively targeted to a liver tissue, so that the toxic and side effects of the Amoitone B are lowered. Moreover, the amoitone derivative long-circulation nanometer lipid carrier is good in biocompatibility, easy to degrade, good in stability and capable of improving body tolerance and patient compliance.

Description

technical field [0001] The invention relates to a long-circulation nano-lipid carrier of adriamycin derivatives and a preparation method thereof. Background technique [0002] Orphan receptor Nur77 (also known as TR3, NGFI-B, TIS1 or NAK-1) is a product of an immediate early gene and is one of the important members of the orphan nuclear receptor subfamily NR4A, which can be stimulated by nerve growth factor, platelet growth Factors, serum, and epidermal growth factor are induced to express, and play a vital role in various biological processes, involving cell proliferation, metabolism, mutation, and apoptosis. Nur77 is often overexpressed in tumor cells, such as gastric cancer, lung cancer, pancreatic cancer, colon cancer, ovarian cancer, etc. It plays an extremely important regulatory role in inhibiting the growth of tumor cells and is a potential target for the treatment of related diseases. [0003] Ascosporine B (cytosporone B, Csn-B) is a natural product extracted from...

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 Patents(China)
IPC IPC(8): A61K9/19A61K9/10A61K31/216A61K47/34A61P35/00
Inventor 张典瑞栾晶晶郝蕾蕾李彩云郭和坚张连茹徐庆妍胡志钰
Owner SHANDONG UNIV
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com