Self-assembled nanoparticles having glucose sensitivity and temperature sensitivity and preparation method of nanoparticles

A nanoparticle and sensitive technology, applied in the field of self-assembled nanoparticles and its preparation, can solve the problems of poor water solubility and unsuitable drug-carrying system, and achieve the effects of no toxic and side effects, good clinical application value, and simple operation.

Inactive Publication Date: 2016-11-09
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are patents for microgels combined with temperature and glucose-sensitive NVCL and 4-vinylphenylboronic (VPBA). However, the above-mentioned microgels have a disadvantage, that is, their water solubility is very poor, and may not be suitable for for drug delivery systems

Method used

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  • Self-assembled nanoparticles having glucose sensitivity and temperature sensitivity and preparation method of nanoparticles
  • Self-assembled nanoparticles having glucose sensitivity and temperature sensitivity and preparation method of nanoparticles
  • Self-assembled nanoparticles having glucose sensitivity and temperature sensitivity and preparation method of nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) Weigh 100mg of AAPBA and 1000mg of NVCL; add 1mg of AIBN at the same time, mix all the above materials and dissolve in 1mL of DMF, fill with nitrogen, 70°C, and react for 8h to generate p(NVCL-co-AAPBA).

[0045] (2) Weigh 10mg of p(NVCL-co-AAPBA), dissolve it in 10mL of ultrapure water, and rotate it for 3 hours at a low speed of 300r / min to form p(NVCL-co-AAPBA )Nanoparticles.

[0046] (3) Accurately weigh 2 mg of p(NVCL-co-AAPBA), and characterize it with a Fourier transform infrared instrument, such as figure 2 shown. AAPBA presents 6 main characteristic peaks, respectively the absorption peak of C=O (1660cm -1 ), the absorption peak of C=C (1620cm -1 ), the absorption peak of O-B-O (1352cm -1 ) and the absorption peak of B-O (1014cm -1 ), the absorption peak of the benzene ring is located at 1555cm -1 to 1610cm -1 between, while the benzene ring is at 698cm -1 and 791cm -1 There is also a faint absorption peak. Between p(NVCL) and p(NVCL-co-AAPBA), t...

Embodiment 2

[0049] Basic properties of the nanoparticles obtained in Example 1.

[0050] (1) Weigh multiple portions of 1mg p(NVCL-co-AAPBA) and dissolve them in aqueous glucose solutions with different concentrations (0g / mL, 1g / mL, 2g / mL, 3g / mL) Solution (pH values ​​are 5.5, 6.0, 6.5, 7.0, 7.5, 8.0, 8.5) and solutions at different temperatures (12 degrees to 37 degrees, measured every 5 degrees), after rotating at a low speed for 10 hours, use DLS to measure the particle size. path. in, Figure 5 is the particle size change of the obtained p(NVCL-co-AAPBA) nanoparticles in different glucose concentrations; Figure 6 is the particle size change of the obtained p(NVCL-co-AAPBA) nanoparticles in aqueous solutions of different pH values; Figure 7 is the particle size change of the obtained p(NVCL-co-AAPBA) nanoparticles at different temperatures.

[0051] (2) Put a drop of the aqueous solution of p(NVCL-co-AAPBA) nanoparticles on the copper grid, observe its morphology and characterist...

Embodiment 3

[0053] Drug-loading characteristics of the nanoparticles obtained in Example 1.

[0054] (1) Dissolve 1mg of insulin and 10mg of p(NVCL-co-AAPBA) in 10mL of aqueous solution, and rotate it for 3 hours at a low speed of 300r / min to complete, then calculate the drug loading rate and encapsulation rate, such as Figure 8 shown.

[0055] (2) Place the p(NVCL-co-AAPBA) nanoparticles coated with insulin at 0mg / mL, 1mg / mL, 2mg / mL and 3mg / mL glucose concentration, in an aqueous solution with a pH value of 7.4, and the temperature is set at 37 degrees Celsius, examine its release characteristics within 120h, such as Figure 9 shown.

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Abstract

The invention relates to self-assembled nanoparticles having glucose sensitivity and temperature sensitivity and a preparation method of nanoparticles. The nanoparticles consist of the following components: 3-acrylamidophenylboronic acid AAPBA and N-vinylcaprolactam NVCL. The preparation method comprises the following steps: mixing the AAPBA, the NVCL and an initiating agent, and dissolving an obtained mixture in a solvent; in an anaerobic condition, conducting a reversible addition reaction, so that a polymer p (NVCL-co-AAPBA); and dissolving the polymer in ultra-pure water, and conducting rotating at 300r/min for 3h, so that the self-assembled nanoparticles having glucose sensitivity and temperature sensitivity are obtained. The method disclosed by the invention is simple and rapid in reaction; the nanoparticles can be used for encapsulating insulin, and the drug-release rate of the encapsulated insulin can be changed along with the increase in glucose concentration; therefore, the nanoparticles have a good practical value.

Description

technical field [0001] The invention belongs to the field of preparation of nanoparticles, in particular to a self-assembled nanoparticle with glucose sensitivity and temperature sensitivity and a preparation method thereof. Background technique [0002] Diabetes has become one of the most serious diseases affecting human health. At present, the only effective treatment is daily subcutaneous injection of insulin. Insulin can regulate blood sugar levels well, but it cannot adjust blood sugar changes according to glucose concentration. In addition, excessive insulin injection can lead to hypoglycemia, and severe cases can lead to death of patients. Therefore, it is necessary to design an intelligent drug delivery system that automatically regulates insulin secretion according to the glucose concentration in the body. In recent years, glucose-sensitive materials have been extensively studied and reported. Concanavalin, glucose oxidase and phenylboronic acid system are the three...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/50A61K47/32A61P3/10
CPCA61K38/28A61K9/5026
Inventor 朱利民武俊紫吴焕玲李赫宇周开春
Owner DONGHUA UNIV
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