Method for preparing nano particles of camptothecin polymeric prodrug amphipathic molecules as well as product and application of nano particles

A technology of amphiphilic molecules and nanoparticles, applied in the field of medicine, can solve problems such as poor solubility and stability

Active Publication Date: 2015-07-22
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Camptothecin is an alkaloid extracted from Camptotheca sinensis, which has good anticancer activity, but poor solubility and stability in water

Method used

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  • Method for preparing nano particles of camptothecin polymeric prodrug amphipathic molecules as well as product and application of nano particles
  • Method for preparing nano particles of camptothecin polymeric prodrug amphipathic molecules as well as product and application of nano particles
  • Method for preparing nano particles of camptothecin polymeric prodrug amphipathic molecules as well as product and application of nano particles

Examples

Experimental program
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Effect test

preparation example Construction

[0075] (4) Preparation of flower-like composite vesicle nanostructures: first dissolve the polymeric prodrug amphiphilic molecule PEG-b-PCPTM in a co-solvent. The co-solvent is pure 1,4-dioxane or a mixed solvent of 1,4-dioxane and other solvents with a total content of not less than 70%. The concentration of the amphiphilic molecule of the polymerized prodrug ranges from 0.1 mg / mL to 1000 mg / mL, and then 4 to 1000 times the volume of water is added, and the total time of dripping water is more than 10 hours. Then, the organic solvent was removed by dialysis. The prepared particles have many small vesicle microstructures and interpenetrating interlaced cavities microstructures. The diameter range of composite vesicle nanoparticles is 500-3000nm.

[0076] E.g, figure 1 PEG based on polymeric prodrug amphiphilic molecule 45 -b-PCPTM 52 (The subscript number "45" represents the degree of polymerization of PEG, and "52" represents the degree of polymerization of CPTM) Four typical ...

Embodiment 1

[0082] Example 1: Reductive response to camptothecin polymerization prodrug amphiphilic molecule PEG 45 -b-PCPTM 52 preparation

[0083] The polyethylene glycol macromolecular chain transfer agent (46mg, 0.02mmol), CPTM (632mg, 1.06mmol) and AIBN (0.33mg, 0.002mmol), 6mL 1,4-dioxane and dimethyl sulfoxide (volume The ratio=1:1) is added to the ampoule to dissolve the mixture. Place the ampoule in liquid nitrogen and freeze it with an oil pump, then seal the ampoule, return to room temperature to melt the reaction mixture, and then freeze and pump the air. The freeze-thaw cycle is repeated three times, and then sealed under vacuum. After stirring the reaction at ℃ for 24h, the polymerization reaction was terminated with liquid nitrogen, the reaction flask was opened, the reaction mixture was precipitated in ether, centrifuged, and then dissolved in chloroform, and AIBN (20 times the equivalent of the macromolecular chain transfer agent) was added at 60℃ The reaction was stirred f...

Embodiment 2

[0087] As described in Example 1, the difference is that the dosage of CPTM is 291.7 mg, 331.9 mg of polymerized prodrug amphiphilic molecule is obtained, and the yield is 98.3%. According to 1 According to H NMR analysis, the degree of polymerization of CPTM is 24, which is expressed as PEG 45 -b-PCPTM 24 , Number average molecular weight M n =15900, the drug load is 50.3%.

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Abstract

The invention relates to a preparation method for different nano particles of reducing response camptothecin polymeric prodrug amphipathic molecules represented in a formula I as well as a product and an application of the nano particles, wherein morphology of a polymeric prodrug amphipathic molecule final assembly can be controlled just by regulating the kind of a solvent and through a way of adding water and regulating a water adding speed, so as to obtain four typical nano structures: spherical structure, disc-shaped structure, flower-shaped compound vesicle and staggered accumulated lamellar nano particles. The nano structures have high drug loading rate (more than 50wt%); compared with the most studied spherical nano particle at present, an assembly of the staggered accumulated lamellar structure is the longest in blood circulation time, followed by the disc-shaped nano particles. In addition, non-spherical particle is greater in tumor cytotoxicity compared with the spherical nano particles. In the formula I, various is independently represent 2 or 3; various Xes independently represent O or NH; R is H, CH3 or CH2CH3; m ranges from 4 to 400; and n ranges from 2 to 300; and number-average molecular weight of the reducing response camptothecin polymeric prodrug amphipathic molecule is 1200-220000.

Description

Technical field [0001] The invention relates to the field of medicine. More specifically, it relates to a method for preparing a hierarchical nanostructure of amphoteric molecule of a camptothecin polymerized prodrug, a product obtained by the method and the use thereof. Background technique [0002] Exploring the hierarchical structure and functions of complex biological systems, such as viral capsids, disc-shaped red blood cells, platelets, etc., has greatly promoted the bionic research of synthetic materials. In the field of biomedicine, synthetic materials are often used as carriers for drugs or imaging reagents. The methods of material structure construction mainly include "top-down" and "bottom-up". method. Among them, the replication (printing) technology of particles in the non-wetting template proposed by DeSimone et al. (Angew.Chem.Int.Ed.2013, 52:6580-6589) and the film stretching technology proposed by Mitragotri et al. (Proc.Natl Acad Sci.USA2007, 104: 11901-11904...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/51A61K47/48A61K31/4745A61P35/00A61K47/60
Inventor 刘世勇胡祥龙
Owner UNIV OF SCI & TECH OF CHINA
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