Cisplatin precursor medicine as well as preparation method thereof, and core-shell nano-particle as well as preparation method thereof

A prodrug and nanoparticle technology, applied in the field of nanomedicine, can solve the problems of difficult hydrophilicity, poor targeting, and weak stability, and achieve the effects of strong targeting, good compatibility, and easy use

Active Publication Date: 2011-05-18
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
View PDF0 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, weak stability, poor targeting, hydrophilicity and difficulty in pre

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
  • Cisplatin precursor medicine as well as preparation method thereof, and core-shell nano-particle as well as preparation method thereof
  • Cisplatin precursor medicine as well as preparation method thereof, and core-shell nano-particle as well as preparation method thereof
  • Cisplatin precursor medicine as well as preparation method thereof, and core-shell nano-particle as well as preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] Such as figure 1 Shown, the preparation method of above-mentioned cisplatin prodrug, comprises the steps:

[0031] Step S110: carry out hydroxylation reaction of cisplatin and hydrogen peroxide to generate c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ]. details as follows:

[0032] Weigh a certain amount of cisplatin and dissolve it in distilled water, add 5 to 10 times the molar amount of cisplatin in H 2 o 2 , react at 40-60 degrees Celsius for 3-6 hours to generate c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ]. Preferably, after the reacted mixture is recrystallized, it is washed successively with cold distilled water, ethanol and ether, and the purified c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ].

[0033] Step S120: c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ] react with hexanoic anhydride to generate structural formula as c, c, t-[Pt(NH 3 ) 2 Cl 2 (O 2 CCH 2 CH 2 CH 2 CH 2 CH 3 ) 2 ] of cisplatin prodrugs. details as follows:

[0034] c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ] ...

Embodiment 1

[0057] Embodiment 1. Preparation of cisplatin prodrug:

[0058] Weigh 0.20 g of cisplatin and dissolve it in 5 mL of distilled water, add 5 times the molar amount of H 2 o 2 , after 3 hours of reaction at 50 ° C, a light yellow precipitate was produced, which was c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ]. After recrystallization, wash with cold distilled water, ethanol and ether successively, and dry to obtain purified c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ].

[0059] Weigh 0.70g c, c, t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ] dissolved in 10mL dimethyl sulfoxide, then added 0.90g hexanoic anhydride, stirred at room temperature for 24 hours, then added distilled water to precipitate a bright yellow precipitate, collected the precipitate by centrifugation, and washed the precipitate 3 times with ether to obtain purified c , c, t-[Pt(NH 3 ) 2 Cl 2 (O 2 CCH 2 CH 2 CH 2 CH 2 CH 3 ) 2 ].

Embodiment c

[0060] The present embodiment c, c, t-[Pt (NH 3 ) 2 Cl 2 (O 2 CCH 2 CH 2 CH 2 CH 2 CH 3 ) 2 ] with a yield of 43%. Product use 1 Characterized by H NMR, the solvent was DMSO-d 6, the chemical shifts are: 6.40-6.13 (S, 6H), 2.13-2.07 (t, J=8Hz, 4H), 2.13-2.07 (m, 4H), 1.25-1.19 (m, 4H), 1.17-1.09 ( m, 8H), 0.93-0.89 (t, J=8Hz, 6H).

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
Diameteraaaaaaaaaa
Login to view more

Abstract

The invention relates to a cisplatin precursor medicine, of which a structural formula is c,c,t-[Pt(NH3)2Cl2(O2CCH2CH2CH2CH2CH3)2]. The cisplatin precursor medicine molecule contains a -O2CCH2CH2CH2CH2CH3 group which has stronger hydrophobicity and better stability, and is easy to pack to be prepared into a nanometer dosage form of high drug load. Meanwhile, the -O2CCH2CH2CH2CH2CH3 group is easily reduced into cisplatin in an organism to act to cancer cells. In addition, the invention also relates to a preparation method of the cisplatin precursor medicine, and a core-shell nano-particle containing the same as well as a preparation method thereof.

Description

【Technical field】 [0001] The invention relates to the field of nanomedicine, in particular to a cisplatin prodrug and a preparation method thereof, and also to a core-shell nanoparticle containing the cisplatin prodrug and a preparation method thereof. 【Background technique】 [0002] The two main types of nanocarriers represented by polymer nanoparticles and nanoliposomes can efficiently encapsulate and transport drugs, and have become a research hotspot for scientists from all over the world. Polymer-phospholipid hybrid nanoparticles have the advantages of good biocompatibility, biodegradability and low toxicity of degradation products, easy target-controlled release, and easy surface functionalization, etc., and are increasingly favored. [0003] Cisplatin is a kind of complex platinum-based chemotherapeutic drug widely used clinically. The action site of cisplatin is the purine or pyrimidine base of DNA. It has the advantages of broad anti-cancer spectrum, strong effect,...

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): A61K31/282C07F15/00A61K9/14A61K47/24A61K47/34A61P35/00
Inventor 蔡林涛郑明彬龚萍贾冬雪郑翠芳
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap