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Preparation of surface hydrazide functionalized polyvinyl alcohol microspheres

A technology of polyvinyl alcohol microspheres and functionalization, which is applied in the direction of medical preparations containing active ingredients, organic active ingredients, antineoplastic drugs, etc., can solve the problems of high microsphere hardness, small swelling, safety hazards, etc., and achieve Improved biocompatibility and safety, improved stability, and reduced leakage

Active Publication Date: 2018-05-08
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The traditional method of preparing polyvinyl alcohol microspheres is through the emulsification method, using small molecule cross-linking agents such as formaldehyde or glutaraldehyde, but the obtained microspheres have high hardness, low swelling and poor elasticity; Agents, such as formaldehyde and glutaraldehyde are highly toxic, and there are residues in the microspheres, which have a certain degree of safety hazard when used as biological materials

Method used

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  • Preparation of surface hydrazide functionalized polyvinyl alcohol microspheres
  • Preparation of surface hydrazide functionalized polyvinyl alcohol microspheres
  • Preparation of surface hydrazide functionalized polyvinyl alcohol microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The synthesis of bisaldehyde-based polyethylene glycol: PEG200 (10 grams, 50mmol) is dissolved in the mixed solvent of 360 milliliters of anhydrous dimethyl sulfoxide and 40 milliliters of chloroform, acetic anhydride (58ml, 600mmol) is added to above-mentioned solution Stir well, and react at room temperature (25°C) for 10 hours. The mixture was then poured into 1500 ml of ether to precipitate. The precipitate was dissolved with chloroform and reprecipitated with ether, and the operation was repeated twice. After vacuum drying, a viscous liquid was obtained to obtain bisaldehyde polyethylene glycol, PEGCHO-200.

Embodiment 2

[0021] Change PEG200 into PEG400, PEG1000, and PEG2000 respectively, and the rest of the operations are the same as in Example 1.

Embodiment 3

[0023] Preparation of polyvinyl alcohol microspheres: polyvinyl alcohol (grade: 1750) and crosslinking agent (bisaldehyde-based polyethylene glycol PEGCHO-200) were respectively 10:3, 10:5, 10:7 according to the mass ratio , 10:9 dissolved in deionized water, mixed the above aqueous solution with paraffin oil according to the water / oil ratio of 1:4, added 3% span80, and stirred at high speed to prepare a reverse phase suspension system. Prepare a 1:1 hydrochloric acid solution, slowly add it dropwise to the above suspension system, and promote the crosslinking of polyvinyl alcohol through the diffusion of hydrogen protons to the water phase. After 8 hours of reaction, filter, soak and wash the microspheres with deionized water repeatedly, and vacuum dry to obtain microspheres with a diameter distribution between 100 microns and 650 microns.

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Abstract

First, synthesize a macromolecular cross-linking agent (dialdehyde-based polyethylene glycol), then mix polyvinyl alcohol, macromolecular cross-linking agent aqueous solution and paraffin oil by endogenous method, stir at high speed to prepare a reverse phase suspension system, and then Hydrochloric acid solution is added dropwise, the diffusion of hydrogen protons to the water phase promotes the cross-linking of polyvinyl alcohol, and microspheres with diameters ranging from 100 microns to 650 microns are prepared. Using dimethylaminopyridine (DMAP) as a catalyst, the hydroxyl groups on the surface of polyvinyl alcohol microspheres (CPVA) reacted with succinic anhydride (SA), and then the carboxyl groups were esterified and reacted with hydrazine hydrate to prepare the surface Polyvinyl alcohol microspheres with hydrazide functional groups. The functional grouped microsphere has good strength and swelling property, adjustable size, good loading capacity for doxorubicin, and can be released slowly under acid stimulation. At the same time, the microsphere has good biocompatibility and has the prospect of being used as a drug carrier.

Description

technical field [0001] The invention relates to the preparation of pH-responsive covalently loaded doxorubicin polyvinyl alcohol microspheres, belonging to the technical field of biological materials and sustained release. Background technique [0002] Microspheres with a diameter of hundreds of microns can be used as a drug formulation for the treatment of inoperable liver cancer in the middle and advanced stages. Through selective arterial cannulation, the microspheres are injected into the target tissue, and the blood supply artery of the tumor is blocked, so as to achieve the purpose of treating liver cancer. Polyvinyl alcohol is a water-soluble polymer material. Animal experiments show that it is completely harmless, non-toxic, non-irritating, and has good biocompatibility. It can be used as a drug sustained-release carrier material to prepare targeted microspheres . [0003] Ordinary embolic microspheres require a long cycle in the process of treating cancer, and ord...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08J7/12C08J3/24A61K47/59A61K9/16A61K31/704A61P35/00
Inventor 倪才华张猛李旺张亚南王洁
Owner JIANGNAN UNIV