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Tumor-targeting pH-sensitive polymeric micelle composition

A technology of polymer glue and composition, which is applied in the direction of drug combination, antineoplastic drugs, and medical preparations of non-active ingredients, etc., which can solve the problems of insufficient drug accumulation and achieve the effect of effectiveness and safety

Inactive Publication Date: 2014-10-29
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the problems of premature drug release from conventional polymer micelles and insufficient drug concentration or drug accumulation at the tumor site

Method used

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  • Tumor-targeting pH-sensitive polymeric micelle composition
  • Tumor-targeting pH-sensitive polymeric micelle composition
  • Tumor-targeting pH-sensitive polymeric micelle composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Synthesis of poly(2-ethyl-2-oxazoline)-polylactic acid (PEOz4300-PLA2700)

[0041] In a three-necked flask equipped with a stirrer, 2-ethyl-2-oxazoline (10g, 150mmol), acetonitrile (40mL), methyl p-toluenesulfonate (0.35g) were added, and at an oil bath temperature of 80°C Under a nitrogen atmosphere, the reaction was stirred for 30 h. After cooling, after adding KOH in methanol solution, the reaction was continued for 4h. The solvent was removed, the residue was dissolved in THF, passed through a silica gel column, the effluent was poured into excess cold ether for precipitation, suction filtered, and vacuum-dried for 12 hours. The lactide was recrystallized three times with ethyl acetate, dried under vacuum at room temperature, and its melting point was determined to be 127°C. Put the obtained PEOz-OH powder into a 100mL round-bottomed flask, add about 70mL of toluene, use a water separator to azeotropically remove water, and stop heating after the volatil...

Embodiment 2

[0042] Example 2 Synthesis of poly(2-ethyl-2-oxazoline)-polylactic acid-poly(2-ethyl-2-oxazoline) (PEOz5000-PLA3000-PEOz5000)

[0043] In a three-necked flask equipped with a stirrer, 2-ethyl-2-oxazoline (10g, 150mmol), acetonitrile (40mL), methyl p-toluenesulfonate (0.47g) were added, and at an oil bath temperature of 80°C Under a nitrogen atmosphere, the reaction was stirred for 30 h. After cooling, after adding KOH in methanol solution, the reaction was continued for 4h. The solvent was removed, the residue was dissolved in THF, passed through a silica gel column, the effluent was poured into excess cold ether for precipitation, suction filtered, and vacuum-dried for 12 hours. The obtained PEOz-OH powder (4g) was dissolved in chlorobenzene (80mL), D, L-lactide (6.3g) and stannous octoate (0.63g) were added under a nitrogen atmosphere, and reacted at 140°C for 24h. The reaction solution was poured into excess diethyl ether for precipitation, filtered, and vacuum-dried at r...

Embodiment 3

[0044] Example 3 Synthesis of polylactic acid-poly(2-ethyl-2-oxazoline)-polylactic acid (PLA2000-PEOz8000-PLA2000)

[0045] 2-Ethyl-2-oxazoline (9.9g) and 1,4-dibromo-2-butene (420mg) were dissolved in acetone (40mL), stirred and refluxed at 100°C for 20h under nitrogen atmosphere. After cooling to room temperature, 0.1 mol / L KOH in methanol solution (40 mL) was added to the reaction flask, and the reaction was continued for 4 h. After passing through a silica gel column, the effluent was poured into excess cold diethyl ether for precipitation, suction filtered, and vacuum-dried for 24 hours. Dissolve the obtained HO-PEOz-OH powder (2g) in chlorobenzene (20mL), add D,L-lactide (0.58g) and stannous octoate (30mg) under a nitrogen atmosphere, and react at 140°C for 24h . The reaction solution was poured into excess diethyl ether to precipitate, filtered, and vacuum-dried at room temperature for 12 hours to obtain the triblock copolymer PLA2000-PEOz8000-PLA2000 of the present i...

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Abstract

The invention belongs to the field of medicinal preparations, and relates to a tumor-targeting pH-sensitive polymeric micelle composition, and especially relates to a pH-sensitive polymeric micelle composition encapsulating a poorly-soluble anti-tumor medicine. The tumor-targeting pH-sensitive polymeric micelle composition is constructed by employing biologically-compatible pH-sensitive amphiphilic block polymer and an amphiphilic polymer connected with a targeting ligand or an antibody in a certain ratio, and the composition encapsulates a poorly-soluble anti-tumor medicine. Experiments prove that the polymeric micelle composition has pH-dependent release characteristic, is accumulated in tumor tissue in a high concentration, has specifically targeting inhibiting effect on growth of tumor cells, and provides a novel carrier and preparation strategy for poorly-soluble anti-tumor medicines.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a tumor-targeting pH-sensitive polymer micelle composition, in particular to a pH-sensitive targeting polymer micelle composition carrying insoluble antitumor drugs. Background technique [0002] At present, most of the commonly used chemotherapeutic drugs for clinical treatment of tumors are hydrophobic drugs. Their solubility in water is very low, and it is difficult to prepare suitable preparations. Various methods are often used to increase their solubility, such as making them into salts, adding co-solvents and Solubilization by low-molecular-weight surfactants, etc. Due to the easy availability of surfactants, solubilization with low-molecular surfactants is often the first choice for clinical use. However, the blood stability of this dosage form is very poor, and the toxic and side effects of auxiliary materials such as low-molecular surfactants are also very larg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K45/00A61K47/34A61P35/00
Inventor 刘艳高雅杰李馨儒周艳霞
Owner PEKING UNIV
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