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Intelligent polymethylacrylate drug bearing microsphere with pH response, polymethylacrylate and preparation method and use method thereof

A technology of drug-loaded microspheres and bone cement, used in pharmaceutical formulations, microcapsules, drug delivery, etc., can solve problems such as unsatisfactory antibiotic release curves, limited antibiotic types, and reduced total antibiotic release, and achieve preventive measures. Infectious ability, good bacteriostatic effect, effect of controlling drug release

Active Publication Date: 2020-10-27
BEIJING BONSCI TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 1. The types of antibiotics contained in PMMA are limited, and the antibiotics carried are partially inactivated by the heat release during the bone cement polymerization process;
[0004] 2. The release curve of antibiotics is not satisfactory. Due to the burst release effect, PMMA releases a large amount of antibiotics in a short period of time, and the total amount of antibiotics released in the later period is significantly reduced, and this irregular release curve cannot well meet the requirements for the treatment of infection. Maintain effective antibiotic concentration for a long time

Method used

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  • Intelligent polymethylacrylate drug bearing microsphere with pH response, polymethylacrylate and preparation method and use method thereof
  • Intelligent polymethylacrylate drug bearing microsphere with pH response, polymethylacrylate and preparation method and use method thereof
  • Intelligent polymethylacrylate drug bearing microsphere with pH response, polymethylacrylate and preparation method and use method thereof

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preparation example Construction

[0089] According to a third aspect of the present invention, a method for preparing bone cement is provided, comprising the following steps:

[0090] Mix PMMA, initiator, developer and drug-loaded microspheres according to the proportion to obtain powder;

[0091] Powder and liquid make up bone cement.

[0092] In one embodiment, the preparation method of the drug-loaded microspheres comprises the following steps:

[0093] (A) obtain polyethylene glycol-chitosan graft copolymer and acetyl histidine-chitosan graft copolymer;

[0094] (B) Emulsification and cross-linking of polyethylene glycol-chitosan graft copolymer and acetyl histidine-chitosan graft copolymer in the presence of antibiotics to obtain PEG-chitosan with antibiotics embedded inside sugar-histidine polymer microspheres;

[0095] (C) loading antibiotics on the surface of PEG-chitosan-histidine polymer microspheres with antibiotics embedded inside to obtain drug-loaded microspheres.

[0096] Preferably, step (B...

Embodiment 1

[0106]A bone cement, including powder and liquid; the solid-liquid ratio of the powder and liquid is 2g / ml.

[0107] Powder:

[0108] PMMA: 78%;

[0109] BPO: 2.0%;

[0110] BaSO 4 : 12%;

[0111] Microspheres loaded with antibiotics: 8%;

[0112] liquid:

[0113] MMA: 98%;

[0114] DMPT: 2.0%;

[0115] HQ: 100ppm.

[0116] The preparation method of loading antibiotic microspheres is as follows:

[0117] Preparation of PEG-chitosan powder: 5g chitosan is dissolved in 2% acetic acid (1:5m / v), diluted with 100ml tetramethylethylenediamine hydrochloride and heated at a constant temperature of 35°C, and adjusted The pH of the solution is 5, add 20mg EDC·HCl (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) and 15mg NHS (N-hydroxysuccinimide), after 30min Add 150 mg of carboxyl-terminated polyethylene glycol, stir for 36 hours, and keep the pH at 4-6. The crude product is dialyzed for 4 days and freeze-dried to obtain polyethylene glycol-chitosan powder.

[0...

Embodiment 2

[0123] A bone cement, including powder and liquid; the solid-liquid ratio of the powder and liquid is 2g / ml.

[0124] Powder:

[0125] PMMA: 86%;

[0126] BPO: 1.5%;

[0127] BaSO 4 :8%;

[0128] Microspheres loaded with antibiotics: 4.5%;

[0129] liquid:

[0130] MMA: 99%;

[0131] DMPT: 1.0%;

[0132] HQ: 90ppm.

[0133] Load antibiotic microsphere with embodiment 1.

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Abstract

The invention provides an intelligent polymethylacrylate drug bearing microsphere with pH response, polymethylacrylate and a preparation method and a use method thereof, and relates to the technical field of biomedical materials. The intelligent polymethylacrylate drug bearing microsphere with pH response takes a PEG-chitosan-histidine polymer microsphere as a drug carrier, and the drug includes antibiotics, wherein the antibiotic part is partially embedded inside the PEG-chitosan-histidine polymer microsphere and partially loaded on the surface of the PEG-chitosan-histidine polymer microsphere. The invention solves the problem of sudden release and unsustainable and inefficient release of antibiotics in the antibiotics-loaded polymethylacrylate. In the early stage of implantation, the antibiotics are partially released to play a role of preventing infection. If infection occurs, and becomes serious gradually, the polymethylacrylate continuously releases a large amount of antibiotics at the infection site to achieve the purpose of treating infection. The addition of microspheres not only ensures an antibacterial effect of the polymethylacrylate, but also ensures mechanical properties of the polymethylacrylate within the standard range.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, in particular to an intelligent drug-loaded bone cement microsphere with pH response, bone cement and a preparation method and a use method thereof. Background technique [0002] Bone cement (polymethylmethacrylate, polymethylacrylate, PMMA) is often used in vertebroplasty or joint replacement, because the existence of bone cement implants will weaken the immune system of the human body, in order to avoid the occurrence and spread of infection, so The emergence of antibiotic-containing bone cement is to add antibiotics to the bone cement powder to prevent infection, but there are still obvious disadvantages in the long-term treatment process: [0003] 1. The types of antibiotics contained in PMMA are limited, and the antibiotics carried are partially inactivated by the heat release during the bone cement polymerization process; [0004] 2. The release curve of antibiotics is not sat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L27/16A61L27/20A61L27/54A61L27/50
CPCA61L27/16A61L27/20A61L27/54A61L27/50A61L2430/02A61L2300/232A61L2300/252A61L2300/406A61L2300/602A61L2300/622C08L33/12C08L87/00
Inventor 聂洪涛张凯王璇
Owner BEIJING BONSCI TECH CO LTD
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