Multifunctional nano-drug carrier of targeted lactoferrin receptor, preparation method of multifunctional nano-drug carrier and drug-loading composition comprising multifunctional nano-drug carrier

A nano-drug carrier, lactoferrin technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulations, etc., can solve the problems of difficult control of degradation rate and cycle, poor water solubility, difficult to achieve targeted delivery, etc., to reduce toxic side effects, Reduce the frequency of dosing and improve the effect of drug efficacy

Pending Publication Date: 2021-11-09
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strong hydrogen bonding between amino acids, etc., this type of drug carrier material has disadvantages such as poor water solubility, difficulty in controlling the degradation rate and cycle in vivo, and difficult to achieve targeted delivery.

Method used

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  • Multifunctional nano-drug carrier of targeted lactoferrin receptor, preparation method of multifunctional nano-drug carrier and drug-loading composition comprising multifunctional nano-drug carrier
  • Multifunctional nano-drug carrier of targeted lactoferrin receptor, preparation method of multifunctional nano-drug carrier and drug-loading composition comprising multifunctional nano-drug carrier
  • Multifunctional nano-drug carrier of targeted lactoferrin receptor, preparation method of multifunctional nano-drug carrier and drug-loading composition comprising multifunctional nano-drug carrier

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0056] An embodiment of the present invention provides a method for preparing a multifunctional nano-drug carrier targeting lactoferrin receptors as described above, which includes the following steps:

[0057] S10, providing nano micelles;

[0058] S11, get lactoferrin and disperse it in the buffer, add 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDCI) and N-hydroxysuccinimide (NHS ), followed by stirring and activation treatment at room temperature in the dark;

[0059] S12, remove the unreacted EDCI and NHS in the reaction solution after the activation treatment, and then disperse in the buffer solution to obtain an activated lactoferrin dispersion;

[0060] S13. Add the nanomicelles to the activated lactoferrin dispersion, and react under stirring;

[0061] S14. Purifying the post-reaction system to obtain a multifunctional nano drug carrier targeting lactoferrin receptors;

[0062] Wherein, the nanomicelle is an amino-modified nanomicelle (that is, the ...

Embodiment 1

[0086] Preparation of nanospherical micelles

[0087] Take 10mg mPEG 45 -PV 2 -PMet(Se) 2 (P=0.28) and 10mg NH 2 -PEG 45 -PV 2 -PMet(Se) 2 (P=0.28) was completely dissolved in 2mL DMSO, oscillated to mix the polymer evenly to obtain a polymer solution; then 5mL of deionized water was added dropwise to it, and stirred for 2 hours to obtain a solution; the obtained solution was directly added to the intercepted In a dialysis bag with a molecular weight of 2000DA, dialyze in 2L deionized medium at room temperature for 7 days, change the water once a day, and then use a water phase filter head to filter (pore size 450nm) the liquid in the dialysis bag to filter out macromolecular precipitation and aggregated micellar particles , to obtain the target product nano-spherical micelles.

Embodiment 2

[0089] Preparation of nanorod micelles

[0090] Take 10mg mPEG 45 -PV 2 -PMet(Se) 4 (P=0.46) and 10mg NH 2 -PEG 45 -PV 2 -PMet(Se) 4 (P=0.46) was completely dissolved in 2 mL of dichloromethane, and a uniform film was formed by rotary evaporation in an eggplant-shaped flask, and the residual organic solvent was removed by vacuuming overnight. Add 5mL double-distilled water into an eggplant-shaped bottle, hydrate at 60°C for 1 hour, oscillate and mix well, and ultrasonically in a water bath to obtain a nanorod-shaped micellar dispersion, centrifuge at 3000r / min for 30min, remove large aggregated particles, and freeze-dry the supernatant , to obtain the target product nanorod micelles.

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Abstract

The invention relates to a multifunctional nano-drug carrier of a targeted lactoferrin receptor, a preparation method of the multifunctional nano-drug carrier and a drug-loading composition comprising the multifunctional nano-drug carrier. The multifunctional nano-drug carrier is prepared by self-assembling a poly-seleno-amino acid amphiphilic block copolymer with a structure as shown in the following formula and then modifying the self-assembled poly-seleno-amino acid amphiphilic block copolymer with lactoferrin, where n is smaller than or equal to 454 and greater than or equal to 22, x is smaller than or equal to 50 and greater than or equal to 2, y is smaller than or equal to 50 and greater than or equal to 2, and n, x and y are all integers. The drug carrier disclosed by the invention can be used for loading drug molecules to prepare a sustained-release and controlled-release targeted drug delivery system, and can be used for directionally delivering the drug molecules to a diseased region so as to reduce the drug delivery frequency, improve the treatment effect and the like. When having the advantages of common amino acid drug carriers, the drug carrier not only has various biological functions of selenium, but also has specificity of the targeted lactoferrin receptor, is a novel targeted multifunctional drug carrier, and is suitable for research, development and clinical application of drug carriers of various drugs for various diseases related to lactoferrin receptor abnormality.

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 drug carrier targeting lactoferrin receptors, a preparation method and a drug-loaded composition. Background technique [0002] The human body has a very complex physiological environment. Drugs need to go through multiple obstacles from ingestion to exert their effects. Often only a small part of the drugs can exert their efficacy in the end, seriously affecting the therapeutic effect, and at the same time causing toxic and side effects. How to enhance the utilization rate and safety of drugs is of great significance for improving the therapeutic effect of diseases and human health. In recent years, researches on different types of drug carriers have been highly valued. [0003] Drug carriers are mainly natural or synthetic polymer materials, which are chemically bonded, physically adsorbed or packaged with drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K47/62A61K47/64A61K47/69A61K33/04A61K45/06A61P3/02A61P25/28A61P25/16
CPCA61K47/60A61K47/62A61K47/644A61K47/6907A61K47/6925A61K47/6921A61K33/04A61K45/06A61P3/02A61P25/28A61P25/16A61K2300/00
Inventor 吴海强许晨舒李晨阳欧阳娜王亦男熊炜李霞
Owner SHENZHEN UNIV
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