Poly(2-cyanoacrylic acid) as well as preparation method and application thereof
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A technology of cyanoacrylic acid and cyanoacrylate, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as poor biocompatibility and easy allergies , to achieve the effect of improving curative effect and reducing side effects
Active Publication Date: 2019-12-03
DALIAN HEYUAN MEDICAL DEVICES
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There are sulfonic acid groups in DC-Bead, the biocompatibility is not good, and it is easy to cause allergies
Method used
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Embodiment
[0057] Embodiment 1 --- the preparation of poly(2-cyanoacrylic acid)
[0058] (1) Formulation: n-butyl α-cyanoacrylate
[0059] Normal saline, sesame oil, Tween-80, Span-20, absolute ethanol
[0060] Dissolve n-butyl α-cyanoacrylate in refined pyrogen-free sesame oil to form 10 mL of a 30% oil solution of n-butyl α-cyanoacrylate, and disperse in 0.25% Tween-80 with a pH value of 4.0 and Span-20 in normal saline solution. Then adjust the pH value to 7.8 to initiate the polymerization of n-butyl α-cyanoacrylate, centrifuge the precipitate after 12 hours, wash the precipitate with absolute ethanol and repeat the centrifugation for 5 times, and disperse the precipitate in 50ml of absolute ethanol, Add sodium hydroxide, selectively hydrolyze the ester bond and retain the cyano group, evaporate under reduced pressure to remove absolute ethanol, then mix with 100mL distilled water, centrifuge at 8000rpm for 20 minutes, discard the supernatant, shake and wash with water, and centrif...
Embodiment 3
[0084] Example 3---Preparation of poly(2-cyanoacrylic acid) drug-loaded embolic microspheres
[0087] Take 1 mL of blank embolization microspheres, mix with an equal volume of 2 mg / mL doxorubicin 1 / 15M isotonic phosphate buffer with pH value 7.4, shake for 15 minutes, pour off the remaining doxorubicin solution, and then use pH 7.4 After washing with 1 / 15M isotonic phosphate buffer solution, the doxorubicin-loaded embolization microspheres for tumor arterial embolization are obtained.
[0090] Take 1 mL of blank embolization microspheres, mix with an equal volume of 10 mg / mL gentamicin 1 / 15M isotonic phosphate buffer with a pH value of 7.4, shake for 5 minutes, pour off the remaining gentamicin solution, and then use pH 7.4 1 / 15M isotonic phosphate buffer solution to obtain gentamicin-loaded embolization microspheres that re...
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Abstract
The invention relates to poly(2-cyanoacrylic acid) as well as a preparation method and application thereof, and belongs to the fields of medicine and chemical industry. The method comprises the following steps: firstly, preparing an alpha-cyanoacrylate polymer, and selectively hydrolyzing ester bonds of the polymer under alkaline conditions to obtain the poly(2-cyanoacrylic acid). The poly(2-cyanoacrylic acid) is dispersed into water to form negatively charged microspheres, so that novel blank embolism microspheres are obtained, the particle sizes of the blank embolism microspheres can be adjusted in a micrometer range, and the blank embolism microspheres have a deformation function to pass through blood vessels with specific morphology, and can tightly embolize the blood vessels to avoidectopic embolism due to shedding; and the blank embolism microspheres and a positively-charged drug are combined to obtain novel drug-loaded embolism microspheres, the novel drug-loaded embolism microspheres use a polymer carboxyl group to actively load the positively-charged drug by adopting the principle of charge reversal, and can directly release the drug in localized pathological tissue, thedrug rarely flows through a whole body, so that the local effect of the drug on the pathological tissue is improved, and the toxic and side effects of the drug on the whole body are reduced.
Description
technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to poly(2-cyanoacrylic acid) and its preparation method and application. Background technique [0002] It is generally believed that intravascular embolism should be avoided, but if some blood vessels can be partially embolized selectively, good therapeutic effects can be received. In recent years, due to the development of medical technology, people have been able to inject vascular occlusive agents (Vascular Occlusive Agent) into relevant arteries through inserted catheters to treat some diseases, especially for some diseases that are difficult to control with surgery or drugs, such as tumors or gastric fundus Varicose veins. This technique is medically known as selective vascular embolization. Transcatheter arterial embolization was first used in the 1970s to treat prostatic bleeding after prostate biopsy or transurethral prostatectomy and refractory hematuria of p...
Claims
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