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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 poor targeting, difficult hydrophilicity, and weak stability, and achieve the effects of strong targeting, easy use, and good compatibility

Active Publication Date: 2012-07-25
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, weak stability, poor targeting, hydrophilicity and difficulty in preparing high-drug-loading dosage forms are problems that have not been solved.

Method used

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  • 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] like 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 ] dis...

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).

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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

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Application Information

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Patent Type & Authority Patents(China)
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
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