Compound, nano super-molecular drug carrier and drug containing nano super-molecular drug carrier

A compound and supramolecular technology, applied in the direction of drug combination, preparation for in vivo test, medical preparation of non-active ingredients, etc., can solve the problems of unpredictable photodynamic properties of compounds, complex molecular design manpower and material resources, etc.

Inactive Publication Date: 2018-06-22
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method requires complex molecular design and a lot of manpower and material resources, and the photodynamic performance of the final modified compound is unpredictable

Method used

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  • Compound, nano super-molecular drug carrier and drug containing nano super-molecular drug carrier
  • Compound, nano super-molecular drug carrier and drug containing nano super-molecular drug carrier
  • Compound, nano super-molecular drug carrier and drug containing nano super-molecular drug carrier

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0058] Synthesis process of 1,5,11,17,23,29-pentanitro-31,32,33,34,35-penta(n-dodecyloxy)calix[5]arene:

[0059] 3.97g of 5,11,17,23,29-penta-tert-butyl-31,32,33,34,35-penta(n-dodecyloxy)calix[5]arene (see Arnaud-Neu , F., Fuangswasdi, S., Notti, A., Pappalardo, S. & Parisi, Angew.Chem., Int.Ed.1998, 37, 112-114 and Garozzo, D., et al.Angew.Chem. , Int.Ed.2005, 44, 4892-4896) was dissolved in 119mL of dry dichloromethane and 34.28mL of acetic acid solution, then gradually added 10.28mL of nitric acid dropwise, and stirred at room temperature for 1 to 4 hours. The color of the solution changed from dark purple to orange. Then add 250mL water to the reaction solution and stir for 30 minutes, extract and separate the mixed solution with saturated sodium carbonate solution, saturated saline solution, and water, collect the organic phase, concentrate, dry over anhydrous sodium sulfate, and recrystallize with dichloromethane and methanol , to obtain 1.74 g of 5, 11, 17, 23, 29-pen...

preparation Embodiment 2

[0076] The preparation process of nano supramolecular drug carrier:

[0077] Mix the methanol solution of GC5A-12C with a concentration of 1mmol / L and the chloroform solution of modified polyethylene glycol with a concentration of 1mmol / L in a ratio of 1:1, then remove the solvent in a vacuum, add water, and then heat and sonicate , and finally obtain the nano-supramolecular drug carrier of GC5A-12C with a concentration of 1 mmol / L. The hydrated particle size of the supramolecular nano drug carrier measured by dynamic light scattering is 113nm, and the polydispersity coefficient is 0.17 ( Figure 7 ); the preparation of the TEM sample, the dispersed nano-carrier solution is taken appropriate amount and dripped on the copper grid supported by carbon, dried at room temperature, then vacuum-dried for 24h, and photographed by TEM ( Figure 8 ); the preparation of the SEM sample, the dispersed nano-carrier solution is taken in an appropriate amount and dropped on a silicon wafer, ...

preparation Embodiment 3

[0079] The preparation process of the drug:

[0080] Weigh 2.383g of N-(2-hydroxyethyl)piperazine-N'-2-ethanesulfonic acid (hereinafter referred to as HEPES), and use ultrapure water to prepare 1L of 10mmol / L pH 7.4 buffer solution (hereinafter referred to as HEPES buffer solution). Weigh A1PcS 4 , with 10mmol / L HEPES buffer solution to prepare 1mmol / L AlPcS 4 stock solution, AlPcS was mixed with 10mmol / L pH 7.4 HEPES buffer solution at 25℃ 4 The stock solution is diluted, and the nano-supramolecular drug carrier obtained in Preparation Example 2, AlPcS 4 The final concentration of the nano-supramolecular drug carrier and the nano-supramolecular drug carrier is 2 μmol / L, and the drug with a concentration of 2 μmol / L is obtained after mixing evenly.

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Abstract

The invention provides a compound, a nano super-molecular drug carrier and a drug containing the nano super-molecular drug carrier and belongs to the technical field of nano super-molecular materials.The compound and modified polyethylene glycol are co-assembled to form the nano super-molecular drug carrier and the loading of an anionic photosensitizer is realized; the photosensitizer can be specifically released at a tumor part and targeted imaging and treatment of a solid tumor are realized. The compound is 5,11,17,23,29-pentaguanidyl-31,32,33,34,35-pentaalkoxycalix[5]arene with a specificstructure. The nano super-molecular drug carrier takes the compound with a structural formula shown as a formula (I) and the modified polyethylene glycol as building units. The drug comprises the nanosuper-molecular drug carrier and the anionic photosensitizer loaded on the nano super-molecular drug carrier.

Description

technical field [0001] The invention relates to a compound, a nano-supramolecular drug carrier and a drug containing the nano-supramolecular drug carrier, and belongs to the technical field of nano-supramolecular materials. Background technique [0002] Photodynamic therapy (PDT) is an emerging disease treatment method, which has attracted the attention of the medical field and the majority of scientific researchers because of its good safety and non-invasive characteristics. Photodynamic therapy mainly involves photosensitizers, light and oxygen molecules. First, the photosensitizer gathers around the diseased tissue, and then irradiates the diseased tissue with a suitable light source. After absorbing the energy, the photosensitizer transitions from the ground state to the excited state, and the excited state photosensitizer transfers the energy to the oxygen molecules around the cell, and then a series of events occur. The photochemical reaction produces a large number o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/18A61K47/16A61K41/00A61K49/00A61P35/00C08G65/333
CPCA61K41/0071A61K47/16A61K49/0021A61K49/0054C07C279/18C08G65/33396
Inventor 郭东升
Owner NANKAI UNIV
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