Sodium cholate-polymer nanometer composite drug carrier

A nanocomposite and polymer technology, applied in the fields of biomedicine and nanoscience, can solve the problem of unclear distinction between hydrophilic groups and hydrophobic parts, and achieve the effect of simple preparation method and strong operability

Inactive Publication Date: 2017-10-13
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the hydrophobic tails of common amphiphilic molecules are located in the micelle core, while the hydrophobic rings of bile salts have strong rigidity. On the one hand, it makes the distinction between hydrophilic groups and hydrophobic parts unclear. In the micelle, some hydrophobic groups may still be exposed to the water environment, while the hydrophilic groups are located inside the micelles

Method used

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  • Sodium cholate-polymer nanometer composite drug carrier
  • Sodium cholate-polymer nanometer composite drug carrier
  • Sodium cholate-polymer nanometer composite drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1. Preparation of a drug carrier with tunable polymer micelle morphology

[0030] 1. The mass ratio of amphiphilic block copolymer (polyethylene glycol-polylactic acid) to sodium deoxycholate is 100:5, weigh sodium deoxycholate and add it to 5ml of dimethyl sulfoxide (DMSO), stir for 1h, make it fully dissolved.

[0031] 2. Weigh 10 mg of doxorubicin hydrochloride (DOX HCL) and add it to the above solution, add 1 ml of triethylamine to remove the hydrochloride of DOX HCL, make it insoluble in water, stir overnight to make triethylamine and DOX fully react . 40 mg of polyethylene glycol-polylactic acid was added, and the polymer was dissolved by stirring.

[0032] 3. Transfer the above mixed solution to a dialysis bag (molecular weight cut-off is 8-14kDa), dialyze in 500 mL of deionized water for 2 days, and change the water every 6h to remove the DMSO dialyzed. The compound drug carrier solution can be obtained. The transmission electron microscope observation resul...

Embodiment 2

[0034] 1. Preparation of a drug carrier with tunable polymer micelle morphology

[0035] 1. The mass ratio of block copolymer (polyethylene glycol-polylactic acid) to sodium deoxycholate is 100:10. Weigh sodium deoxycholate and add it to 5ml of dimethyl sulfoxide (DMSO), and stir for 1h to make it Fully dissolved.

[0036] 2. Weigh 10 mg of doxorubicin hydrochloride (DOX HCL) and add it to the above solution, add 1 ml of triethylamine to remove the hydrochloride of DOX HCL, make it insoluble in water, stir overnight to make triethylamine and DOX fully react . 40 mg of polyethylene glycol-polylactic acid was added, and the polymer was dissolved by stirring.

[0037] 3. Transfer the above mixed solution to a dialysis bag (molecular weight cut-off is 8-14kDa), dialyze in 500 mL of deionized water for 2 days, and change the water every 6h to remove the DMSO dialyzed. The compound drug carrier solution can be obtained.

[0038] The particle size distribution results of the obta...

Embodiment 3

[0040] 1. Preparation of a drug carrier with tunable polymer micelle morphology

[0041] 1. The mass ratio of block copolymer (polyethylene glycol-polylactic acid) to sodium deoxycholate is 100:20, weigh sodium deoxycholate and add it to 5ml of dimethyl sulfoxide (DMSO) and stir for 1h to make it Fully dissolved.

[0042] 2. Weigh 10 mg of doxorubicin hydrochloride (DOX HCL) and add it to the above solution, add 1 ml of triethylamine to remove the hydrochloride of DOX HCL, make it insoluble in water, stir overnight to make triethylamine and DOX fully react . 40 mg of polyethylene glycol-polylactic acid was added, and the polymer was dissolved by stirring.

[0043]3. Transfer the above mixed solution to a dialysis bag (molecular weight cut-off is 8-14kDa), dialyze in 500 mL of deionized water for 2 days, and change the water every 6h to remove the DMSO dialyzed. The compound drug carrier solution can be obtained.

[0044] 2. In vitro release experiments

[0045] 2 mL of DO...

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Abstract

The present invention relates to a sodium cholate-polymer nanometer composite drug carrier, which is formed by compounding an amphiphilic block copolymer, sodium cholate and at least a hydrophobic drug encapsulated in a carrier, wherein the shape of the drug carrier can be regulated by the sodium cholate material so as to regulate the drug release behavior. The present invention further provides a preparation method and applications of the drug carrier having the regulated shape. According to the present invention, the drug carrier has the good drug controlled-release function, can provide the high drug loading amount, and further has characteristics of effective drug encapsulation, drug side effect reducing, and drug utilization rate improving.

Description

technical field [0001] The invention belongs to the field of biomedicine and nano science, in particular to a sodium cholate-polymer nano composite drug carrier. Background technique [0002] Amphiphilic block polymers can form nanomicelles of various morphologies through self-assembly in solvents. Regarding the morphology of polymer micelles, there are mainly spherical, cylindrical (short rod-like and worm chain-like), plate-like and vesicles. The dominant factor for the formation and change of different morphologies is the free energy of micelles. The free energy of the system is subject to the balance between the following three forces: one is the extension of the nucleating segment; the other is the surface tension between the inner segment and the solvent, that is, the interfacial energy; the third is the interfacial energy between the shell segments mutual exclusion. The magnitude and change of the free energy of the system essentially determine the morphology of bl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K45/00A61K47/34A61K47/28A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K45/00A61K47/28A61K47/34
Inventor 谭庆刚储艳艳
Owner TONGJI UNIV
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