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Cisplatin nano-micelle prodrug and preparation method thereof

A nanomicelle and prodrug technology, which is applied in the field of cisplatin nanomicelle prodrug and its preparation, can solve the problems affecting the passive targeting effect, and achieve the effect of optimizing the active targeting effect and optimizing the passive targeting effect

Inactive Publication Date: 2011-03-30
SHANGHAI NAT ENG RES CENT FORNANOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Kataoka et al. assembled cisplatin and polyethylene glycol-polyglutamic acid (PEG-b-Glu) diblock copolymers into nanomicelles, and the drug loading was greatly improved, up to about 30%. Micellar drugs have good therapeutic effects on solid tumor models in nude mice, showing good clinical application prospects (Nobuhiro Nishiyama, Souichiro Okazaki, Horacio Cabral, Masaki Miyamoto, Yukio Kato, Yuichi Sugiyama, Kazuto Nishio, Yasuhiro Matsumura, and Kazunori Kataoka , Cancer Research, 63 (2003) 8977-8983; Nobuhiro Nishiyama, Masayuki Yokoyama, Takao Aoyagi, Teruo Okano, Yasuhisa Sakurai, and Kazunori Kataoka, Langmuir, 15 (1999) 377-383), but the micellar particle size is below 30nm, Affect passive targeting effect

Method used

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  • Cisplatin nano-micelle prodrug and preparation method thereof
  • Cisplatin nano-micelle prodrug and preparation method thereof
  • Cisplatin nano-micelle prodrug and preparation method thereof

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Embodiment 1

[0045] Embodiment 1 prepares the cisplatin nanomicelle prodrug containing cisplatin 28%, the chemical structure of this cisplatin nanomicelle prodrug is as follows:

[0046]

[0047] Where: a=5, b=95, x=45, m=0, FA is folic acid.

[0048] Such as figure 1 As shown, the micelle particle size of the cisplatin nanomicelle prodrug is 89nm, a number of polyethylene glycol 1 with a molecular weight of 1000-4000 is attached to the outside of the micelle, and at the end of the polyethylene glycol 1 With folic acid molecule 2 attached.

[0049] This embodiment is prepared through the following steps:

[0050] The first step, synthesis of FA-PEG-NH 2 :

[0051] 1.1) Take NH 2 -PEG-NH 2 (Mw2K, 1.0g, 0.5mmol), folic acid (FA, 0.22g, 0.5mmol), N, N-dicyclohexylcarbodiimide (DCC, 0.12g, 0.6mmol) were dissolved in 10mL dimethyl sulfoxide ( DMSO),

[0052] 1.2) Add 20 μL of pyridine, at room temperature, N 2 Protection stirring reaction 48h. The reaction solution was diluted with...

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Abstract

The invention discloses a cisplatin nano-micelle prodrug and a preparation method thereof in the technical field of nano medicaments. The cisplatin nano-micelle prodrug comprises the following compositions in percentage: 5 to 30 percent of cisplatin and 95 to 70 percent of macromolecular carrier modified by folic acid. The chemical structure of the cisplatin nano-micelle prodrug is as follows: wherein a and b are respectively integers more than or equral to 10 and less than or equal to 60; x is an integer more than or equal to 23 and less than or equal to 92; FA is the folic acid, and m=0, 1 or 2. The cisplatin nano-micelle prodrug is a cisplatin nano-micelle drug carrier system which has narrow particle size distribution, can perform long-acting circulation in blood,and has double targeting effects on lung cancer tissues and adjustable drug release rate so as to improve the water-solubility and the drug-loading rate of the cisplatin, and simultaneously reduce the toxic and side effects of the cisplatin to the utmost.

Description

technical field [0001] The invention relates to a medicine in the technical field of medicine and a preparation method thereof, in particular to a cisplatin nanomicelle prodrug and a preparation method thereof. Background technique [0002] Cisplatin (cis-dichlorodiamminoplatinum, CDDP) is a cycle non-specific drug that can combine with DNA to form cross-links, thereby destroying the replication function of DNA and inhibiting cell division. Clinical practice has proved that cisplatin has the characteristics of broad anti-cancer spectrum, strong effect, synergistic effect with various anti-tumor drugs, and no cross-drug resistance. It is one of the most commonly used drugs in current combination chemotherapy and is widely used in ovarian cancer, Cervical cancer, testicular cancer, breast cancer, esophageal cancer, non-small cell lung cancer and gastric cancer, etc. However, the low water solubility of cisplatin, severe gastrointestinal reactions, bone marrow suppression, and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K9/00A61K33/24A61K35/00A61K47/54A61K47/69
Inventor 余家会唐晓星沈新程何丹农黄进
Owner SHANGHAI NAT ENG RES CENT FORNANOTECH