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Preparation of a drug-loaded cinnamaldehyde-dextran polymer self-assembled nanoparticle and its antitumor application

A kind of technology of glucan and cinnamaldehyde, which is applied in the fields of high molecular polymer and its synthesis and application

Active Publication Date: 2020-03-10
WENZHOU MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a kind of cinnamaldehyde-dextran polymer, self-assembled nanoparticles, drug-loaded complex and its preparation and application. key, not only improve the problem of poor bioavailability of cinnamaldehyde, improve the drug effect, but also the formed polymer can be self-assembled to form nanoparticles, which has drug loading capacity, and has the effect of pH-targeted release in the tumor environment

Method used

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  • Preparation of a drug-loaded cinnamaldehyde-dextran polymer self-assembled nanoparticle and its antitumor application
  • Preparation of a drug-loaded cinnamaldehyde-dextran polymer self-assembled nanoparticle and its antitumor application
  • Preparation of a drug-loaded cinnamaldehyde-dextran polymer self-assembled nanoparticle and its antitumor application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 polymer

[0029] (1) Dissolve cinnamaldehyde (5g, 1eq), trimethyl orthoformate (18.07g, 4.5eq) and pyridinium p-toluenesulfonate (1.89g, 0.2eq) in an appropriate amount of methanol, at 60°C , Reaction 3h. with saturated NaHCO 3 Quenched reaction, extracted three times with EA (ethyl acetate), combined organic layers, MgSO 4 Dry and spin dry under reduced pressure to obtain cinnamon acetal (6.45 g, 95%), which is directly carried out to the next reaction.

[0030] (2) The obtained cinnamon acetal (6.4g, corresponding to 2 equivalents of each hydroxyl group of dextran monomer), dextran (0.872g, MW=20,000), pyridinium p-toluenesulfonate (0.202 g, corresponding to each hydroxyl group of dextran monomer 0.05 equivalent), dissolved with DMSO (10ml), added activated Molecular sieve, N 2 Protected, reacted in an anhydrous and oxygen-free environment, heated at 60°C, and reacted for 60h. The molecular sieves were removed by suction filtrati...

Embodiment 2

[0033] (1) Weigh 5 mg of the polymer obtained in Example 1 and dissolve it with 1 ml of DMSO, drop it into PBS under high-speed stirring, and stir for 2 minutes to fully self-assemble and form nanoparticles. Then DLS detects its particle size, the particle size result is as follows figure 2 As shown in A, the size of nanoparticles formed by self-assembly is about 182.3nm, and its PDI value is 0.225, and the comprehensive evaluation is GOOD.

[0034] (2) Take the self-assembled nanoparticle solution, dilute it with water to 0.125mg / ml, then slowly drop it on the copper grid of the transmission electron microscope, dry it in an oven at 25°C, and then observe it under the transmission electron microscope. The result is as follows figure 2 As shown in B, nanoparticles of about 200 nm are formed.

[0035](3) Take 5 mg of cinnamaldehyde-dextran polymer, dissolve it in 1 ml of DMSO, shake for 2 minutes, and shake evenly. The DMSO solution is dropped into the PBS solution which is...

Embodiment 3

[0039] Take 5 mg of cinnamaldehyde-dextran polymer and dissolve it with 0.5 ml DMSO, and weigh 2 mg of HCPT (10-hydroxycamptothecin) and dissolve it with 0.5 ml DMSO. Mix the two evenly, drop them into 20ml of PBS that is stirring at high speed with a rubber dropper, stir for 4 hours, then dialyze in ultrapure water with a 3.5kd dialysis bag, change the water every 4 hours, and dialyze for 24 hours. Liquids are freeze-dried. The amount of drug loaded was judged by the standard curve of camptothecin. It can be detected that the entrapment rate of camptothecin is about 54%, and the entrapment amount is 0.216mg / mg. It can be seen that the nanoparticle has the ability to load drugs.

[0040] Performance Determination of Drugs for Targeted Release:

[0041] Take 3ml of the dialyzed solution (into a 1000KD dialysis bag, dialyze in 50ml of PBS (pH7.4, 5.0) at 37°C with stirring, and take out 0.3 ml (take three in parallel), measure the OD values ​​of cinnamaldehyde and CPT at 295...

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Abstract

The invention discloses nanoparticles self-assembled from amphipathic molecules which are prepared from cinnamaldehyde and glucan by the aid of acetal bond. The problems of unstable in-vivo metabolismand low bioavailability of cinnamaldehyde are solved greatly, and the formed nanoparticles have pH responsiveness and drug loading capability, and by means of loading for an anti-tumor drug 10-hydroxycamptothecine, the problems of poor water solubility, severe toxic and side effects and the like of 10-hydroxycamptothecine are solved. The nano-polymers are connected with the loaded drug, the two drugs are combined for application, so that ROS (reactive oxygen species) level of tumor cells is improved synergistically, and the tumor cells are killed. The nature of the nanoparticles is verified with multiple means such as nuclear magnetism, DLS, TEM and the like, a drug release experiment is carried out by simulating the tumor environment, and it is proved that the nanoparticles have pH targeted drug release effect definitely.

Description

technical field [0001] The invention relates to a high-molecular polymer and its synthesis and application. The high-molecular polymer is used for the modification of the drug cinnamaldehyde, can self-assemble to form nanoparticles, and has pH responsiveness. According to the loading capacity of nanoparticles, 10-hydroxycamptothecin, an anti-tumor drug, is loaded to form a drug targeting tumor release. The two play a synergistic effect and have a good effect. purpose of application. Background technique [0002] Colorectal cancer is a common clinical malignant tumor, ranking third among digestive tract tumors in my country, and its incidence rate is still showing a trend of increasing significantly. At present, the clinical treatment of colorectal cancer is mainly based on surgery, combined with radiotherapy and chemotherapy. Chemotherapy is an effective method commonly used in the treatment of colorectal cancer. It can reduce postoperative recurrence, improve clinical eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/02A61K47/61A61K47/69A61K9/14A61K31/11A61K31/4745A61P35/00
CPCA61K9/146A61K31/11A61K31/4745C08B37/0006A61K2300/00
Inventor 赵承光郑素清赵承伟梁广蔡跃飘周尔全张露露蔡雄张远洁郑海伦曹伟兰
Owner WENZHOU MEDICAL UNIV
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