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Application of aspirin in preparation of platelet targeted drug delivery system

A technology of aspirin and platelets, which is applied in the field of medicinal chemistry, can solve problems such as difficult encapsulation of nanoparticles and drugs, platelet aggregation deformation, and thrombus formation, and achieve the effects of promoting release, preventing thrombus formation, and increasing output rate

Inactive Publication Date: 2020-04-21
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the study of drug loading on nano-platelets, it was found that platelets are extremely prone to aggregation and deformation, which makes it difficult to effectively encapsulate nanoparticles and drugs, and once aggregation occurs, it is easy to form thrombus in vivo

Method used

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  • Application of aspirin in preparation of platelet targeted drug delivery system
  • Application of aspirin in preparation of platelet targeted drug delivery system
  • Application of aspirin in preparation of platelet targeted drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Aspirin inhibits platelet aggregation

[0030] In order to maintain the complete structural shape of platelets during in vitro treatment, avoid activation deformation, and achieve high platelet yield and high drug loading rate during drug loading, platelet activation must be strictly controlled. Select aspirin to inhibit platelet aggregation, and the preparation process is as follows:

[0031] 1. Wash the platelets and adjust the platelet concentration;

[0032] 2. Prepare aspirin solution so that the final concentration of aspirin solution in platelets is 1 ug / ml;

[0033] 3. Co-incubation of platelets and aspirin solution;

[0034] 4. Washing mixed solution;

[0035] The relevant characterization after preparation, the flow diagram and electron microscope picture of the relevant structure are as follows figure 1 and figure 2 , 3 Shown:

[0036] From its flow graph ( figure 1 ) It can be seen that low-concentration aspirin is easier to enter platele...

Embodiment 2

[0038] Embodiment 2: Preparation and drug encapsulation of PLGA nanoparticles

[0039] PLGA is composed of random polymerization of two monomers - lactic acid and glycolic acid. It is a degradable functional polymer organic compound with good biocompatibility, non-toxicity, and good encapsulation and film-forming properties. Widely used in pharmaceuticals, medical engineering materials and modern industrial fields. Prepare PLGA nanoparticles, and encapsulate doxorubicin and new indocyanine green with PLGA nanoparticles to achieve drug stability.

[0040] making process:

[0041] 1. Weigh 80mg of PLGA, dissolve in 1ml of dichloromethane solution, and shake to fully dissolve;

[0042]2. Weigh 10mg of PVA, dissolve in 10ml of ultrapure water, soak overnight, and bathe in a water bath at 60°C for 4 hours;

[0043] 3. Weigh 1mg doxorubicin and new indocyanine green respectively and dissolve in 1ml ultrapure water;

[0044] 4. Place the PVA solution on a magnetic stirrer and sti...

Embodiment 3

[0045] Embodiment 3: Preparation of nano-platelets and encapsulation of PLGA nanoparticles

[0046] making process:

[0047] 1. Platelet preparation after aspirin inhibition. Ultrasonic crushing to obtain a mixed solution of nano-platelets;

[0048] 2. Ultrasonic dispersion and fusion of nanoplatelets and PLGA nanoparticles that have completed drug encapsulation to realize the encapsulation of nanoparticles by platelets;

[0049] 3. Transmission electron microscopy characterization.

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Abstract

The invention discloses application of aspirin in preparation of a platelet targeted drug delivery system. According to the invention, aspirin is utilized to inhibit platelet aggregation in vitro, prevent platelet deformation and maintain a relatively high proportion of complete platelets, so that relatively high encapsulation efficiency of nanoparticles and antitumor drugs is further realized, aneffective antitumor effect is realized, and the use process is safe and efficient.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to the use of aspirin in the preparation of a platelet-targeted drug delivery system. Background technique [0002] Traditional drug delivery systems have many limitations such as limited targeting, low therapeutic index, poor water solubility, and induction of drug resistance. In order to overcome the drawbacks of traditional drug delivery routes, nanoparticle drug delivery systems were designed and used as drug carriers. Nanoparticle-based drug delivery systems have been rapidly developed and are being applied in various fields of biomedicine. Drug nanocarriers based on dendrimers, liposomes, self-assembling peptides, water-soluble polymers, and block copolymer micelles are currently the most widely studied type of drug delivery systems, and some of them are being used in clinical treatments. Especially in cancer treatment, antineoplastic drugs are making use of nano...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/46A61K47/34A61K31/704A61K41/00A61P35/00
CPCA61K9/5146A61K9/5176A61K31/704A61K41/0057A61P35/00A61K2300/00
Inventor 陈宝安沈艳飞栾建凤杜颖戴璐王淑君周芳章美琳
Owner SOUTHEAST UNIV
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