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Multifunctional nano-drug carrier, preparation method thereof and drug-loading composition

A nano-drug carrier and multi-functional technology, which is applied in the direction of pharmaceutical formulations, liposome delivery, medical preparations of non-active ingredients, etc., can solve the problems of difficult control of degradation rate and cycle, poor water solubility, etc., to reduce toxic side effects, The effect of reducing the frequency of administration and improving the therapeutic effect

Active Publication Date: 2021-01-26
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the strong hydrogen bonding between amino acid molecules, etc., its water solubility is poor, the degradation rate and cycle in the body are difficult to control, and it is easy to be recognized and cleared by the immune system in the body, etc.

Method used

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  • Multifunctional nano-drug carrier, preparation method thereof and drug-loading composition
  • Multifunctional nano-drug carrier, preparation method thereof and drug-loading composition
  • Multifunctional nano-drug carrier, preparation method thereof and drug-loading composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0120] Polyethylene glycol monomethyl ether polyaspartic acid polyselenomethionine block copolymer (mPEG 45 -Pasp2-PMet(Se) 2 )Synthesis

[0121] Weigh 0.1g mPEG-NH 2 (0.05 mmol, Mn=2000) was vacuum-dried in a vacuum oven for 4 hours, and then dissolved in 3 ml of dried DMF to be used as a macroinitiator. Weigh 25mg of newly prepared benzyl L-aspartate NCA (BLA-NCA) (0.1mmol) and dissolve it in 1ml of ultra-dry DMF, then mix the two reaction solutions with a syringe, place under nitrogen atmosphere, and stir the reaction 24h. After the reaction, 22.3 mg of newly prepared seleno-L-methionine NCA (0.1 mmol) was weighed and dissolved in 1 ml of ultra-dry DMF, added to the above mixed reaction solution, and the reaction was continued with stirring. After 24 hours, the reaction was complete. The tri-block polymer was settled in ice anhydrous isopropyl ether, centrifuged, freeze-dried, and dried in a vacuum oven for 24 hours to obtain the product polyethylene glycol monomethyl ...

Embodiment 2

[0123] Polyethylene glycol monomethyl ether polyaspartic acid polyselenomethionine block copolymer (mPEG 45 -PAsp 2 -PMet(Se) 4 )Synthesis

[0124] Weigh 0.1g mPEG-NH 2 (0.05 mmol, Mn=2000) was vacuum-dried in a vacuum oven for 4 hours, and then dissolved in 3 ml of dried DMF to be used as a macroinitiator. Weigh 25 mg of newly prepared L-benzyl-aspartate NCA (0.1 mmol) and dissolve it in 1 ml of ultra-dry DMF, then mix the two reaction solutions with a syringe, place under nitrogen atmosphere, and stir for 24 h. After the reaction, 44.6 mg of newly prepared seleno-L-methionine NCA (0.2 mmol) was weighed and dissolved in 1 ml of ultra-dry DMF, added to the above mixed reaction solution, and the reaction was continued with stirring. After 24 hours, the reaction was complete. The tri-block polymer was settled in ice anhydrous isopropyl ether, centrifuged, freeze-dried, and dried in a vacuum oven for 24 hours to obtain the product polyethylene glycol monomethyl ether polyasp...

Embodiment 3

[0126] Polyethylene glycol monomethyl ether polyaspartic acid polyselenomethionine block copolymer (mPEG 45 -PAsp 2 -PMet(Se) 6 )Synthesis

[0127] Weigh 0.1g mPEG-NH 2 (0.05 mmol, Mn=2000) was vacuum-dried in a vacuum oven for 4 hours, and then dissolved in 3 ml of dried DMF to be used as a macroinitiator. Weigh 25 mg of newly prepared L-benzyl-aspartate NCA (0.1 mmol) and dissolve it in 1 ml of ultra-dry DMF, then mix the two reaction solutions with a syringe, place under nitrogen atmosphere, and stir for 24 h. After the reaction, weigh 66.9g of newly prepared seleno-L-methionine NCA (0.3mmol) and dissolve it in 1ml of ultra-dry DMF, add it to the above mixed reaction solution, and continue to stir the reaction. After 24 hours, the reaction was complete. The tri-block polymer was settled in ice anhydrous isopropyl ether, centrifuged, freeze-dried, and dried in a vacuum oven for 24 hours to obtain the product polyethylene glycol monomethyl ether polyaspartate benzyl este...

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Abstract

The invention relates to a multifunctional nano-drug carrier, a preparation method thereof and a drug-loading composition, and belongs to the technical field of biomedical drug carriers and sustained-release drug carriers. The nano-drug carrier is formed by self-assembling a poly-seleno-amino acid amphiphilic block copolymer with a structure shown in the following formula, wherein n is more than or equal to 22 and less than or equal to 454, x is more than or equal to 2 and less than or equal to 50, y is more than or equal to 2 and less than or equal to 50, and n, x and y are integers. The nano-drug carrier provided by the invention can load drug molecules to prepare a sustained-release and controlled-release drug delivery system, and can be used for drug delivery in various modes, and theloaded drug can be released from the delivery system in a sustained-release and controlled-release mode according to needs, so that the drug delivery frequency is reduced, the treatment effect is improved, and the toxic and side effects of the drug are reduced. Compared with the prior art, the nano-drug carrier provided by the invention has the advantages of a common amino acid nano-drug carrier,has a plurality of biological functions of selenium, and is a novel multifunctional nano-drug carrier.

Description

technical field [0001] The invention relates to the technical field of biomedical drug carriers and slow-release materials, in particular to a multifunctional nano-medicine carrier, a preparation method thereof, and a drug-loaded composition. Background technique [0002] Drug carriers are mainly natural or synthetic polymer materials, which are chemically bonded, physically adsorbed or packaged with drug molecules in different forms to form a drug control system, which can be used without reducing the efficacy of the original drug molecule and suppressing its side effects. Through a series of physical, chemical and biological controls, the timing, positioning and quantitative release of drugs can be realized to help enhance their curative effect. Drug carrier systems have been used in various routes of administration, including injection, oral administration, and transdermal absorption. There are many types of drug carriers. Nano-drug carriers refer to a new type of carrie...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/127A61K47/34A61K45/00C08G69/10C08G69/40
CPCA61K9/1075A61K9/1273A61K47/34A61K45/00C08G69/10C08G69/40
Inventor 吴海强许晨舒徐盼王亦男欧阳娜尚琦
Owner SHENZHEN UNIV
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