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

10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation

A technology of hydroxycamptothecin and liposome preparation, which is applied in the directions of liposome delivery, medical preparations containing active ingredients, organic active ingredients, etc., can solve the difficulty of fusion and freeze-drying, and the speed of liposome removal is slowed down , large particle size of liposomes, etc., to increase blood circulation time, improve needle adaptability, and reduce toxicity

Inactive Publication Date: 2005-08-10
FUDAN UNIV
View PDF6 Cites 13 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention is characterized in that it uses PEGylated lipids to modify liposomes. On the one hand, it can solve the problems of traditional liposomes with large particle size, poor stability, easy leakage, fusion and freeze-drying difficulties; on the other hand, it can make lipids The surface of the plastid is modified by PEG to form a three-dimensional "conformation cloud", which prevents the recognition of opsonins in the blood and the adsorption of plasma proteins, and reduces the phagocytosis of liposomes by the reticuloendothelial system, thereby enabling the removal of liposomes The speed is slowed down, and the residence time in the blood is prolonged, which is conducive to its entry into the tumor tissue, and enhances its penetration and retention of the tumor tissue (EPR effect), so as to achieve tumor targeting and synergistic attenuation

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
  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation
  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation
  • 10-hydroxy camptothecin long cyclic liposome and its freeze aried preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] 10-hydroxycamptothecin 1g, phospholipid 50g, cholesterol 15g, polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) 5g, dissolved in chloroform:methanol (2:1), rotary evaporation to remove organic The solvent was vacuum-dried, added into a solution of trehalose and sucrose water (1:1) dissolved in 100 g, hydrated for 30 min, and treated with ultrasonic waves to obtain a long-circulating liposome solution of 10-HCPT.

Embodiment 2

[0026] Dissolve 2 g of 10-hydroxycamptothecin, 50 g of phospholipids, 10 g of cholesterol, and 10 g of polyethylene glycol-polycaprolactone (PEG-PCL) in chloroform:methanol (2:1), remove the organic solvent by rotary evaporation, and vacuum After drying, add 100g of trehalose solution, hydrate for 30 minutes, and process it with a high-pressure homogenizer to obtain a long-circulation liposome solution of 10-HCPT.

Embodiment 3

[0028] Dissolve 4 g of 10-hydroxycamptothecin, 50 g of phospholipids, 20 g of cholesterol, and 8 g of polyethylene glycol-polyglycolide lactide (PEG-PLGA) in dichloromethane:ethanol (2:1), and rotate to evaporate Remove the organic solvent, dry in vacuum, add 70g of mannose and sucrose in water (1:1) solution, hydrate for 30min, and process with a high-pressure homogenizer to obtain a long-circulating liposome solution of 10-HCPT.

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

A long-cycle lipoid of 10-hydroxyamptothecin and its freeze dried medicine for treating cancer are prepared from lecithin, PEG modified bipid, cholesterol, mycose or cane sugar, alcohol and dichloromethane.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to 10-hydroxycamptothecin long-circulation liposome, a freeze-dried preparation of the long-circulation liposome and a preparation method thereof. Background technique [0002] 10-hydroxycamptothecin (Hydrocamptothecin, HCPT) is a trace alkaloid with the strongest anti-cancer effect among similar anti-tumor monomers extracted from camphor tree chinensis in the 1960s and 1970s. It is an S-phase specific anti-cancer drug . Systematic pharmacological research. Its anti-cancer mechanism is to inhibit Topo I. It is mainly used clinically in ascites-type liver cancer, head and neck cancer, gastric cancer, bladder cancer and leukemia. The toxic reactions of HCPT are mainly manifested in the inhibition of urinary system, digestive system and hematopoietic function. etc., but its toxicity is significantly lower than that of camptothecin, especially the urinary system reaction is les...

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
IPC IPC(8): A61K9/127A61K31/475A61P35/00
Inventor 施斌裴元英
Owner FUDAN 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