Polymer drug carrier and method for preparing same

Abstract

The invention provides a polymer drug carrier and a method for preparing the same. The polymer drug carrier is provided with a core-shell structure, a core comprises polyethylene glycol-distearoyl phosphoethanolamine nano-micelle, and a shell comprises poly-dopamine. The method includes forming the nano-micelle from polyethylene glycol-distearoyl phosphoethanolamine; forming the poly-dopamine shell on the outside of the nano-micelle to obtain the polymer drug carrier. The polymer drug carrier and the method have the advantages that the core and the shell of the polymer drug carrier comprise biodegradable polymers, accordingly, the polymer drug carrier is good in biocompatibility, and few toxic and side effects can be realized; the particle size of the polymer drug carrier is smaller than 50nm, tumor gathering effects and photo-thermal therapy effects can be realized, and tumor cell killing effects can be realized after near-infrared light irradiates on the polymer drug carrier; drugs can be encapsulated by the nano-micelle of the polymer drug carrier, diversified drugs can be loaded under chemical modification effects of the poly-dopamine, and accordingly the polymer drug carrier has an excellent application prospect in the field of medicine and pharmacology.

Description

technical field

[0001] The invention belongs to the field of drug carriers, and relates to a polymer drug carrier and a preparation method thereof. Background technique

[0002] Polymer micelle was developed as a drug carrier in the 1990s. It is a self-assembled structure formed spontaneously by amphiphilic polymers in aqueous solution. The hydrophilic segments are outside, and the hydrophobic segments are aggregated to form nanomicelles. The diameter is generally 5-50nm, and it has the characteristics of high drug loading capacity, wide drug loading range, good stability, long residence time in the body, and improved drug stability.

[0003] Polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) is a drug carrier material that is degradable in vivo and approved by the U.S. Food and Drug Administration (FDA). It has good biocompatibility and safety. But to make the PEG-DSPE polymer carrier multifunctional, it requires further modification, usually involving comp...

Examples

Embodiment 1

[0040] In this example, the polymer drug carrier is prepared by the following method, which includes the following steps:

[0041] 100mgPEG 2000 -DSPE was dispersed in 5mL methanol, stirred and dissolved, and the organic solvent was removed with a rotary evaporator to form a lipid film. A tris-HCl buffer solution with pH 8.5 was added to the lipid film to form a PEG-DSPE nanomicelle solution, wherein the concentration of the PEG-DSPE nanomicelle was 2 mg / mL.

[0042] 20 mg of dopamine hydrochloride was added to the above PEG-DSPE nanomicelle solution, and the reaction vessel was opened and stirred for 24 hours to obtain a polymer drug carrier with a core-shell structure.

Embodiment 2

[0044] 100mgPEG 2000 -DSPE was dispersed in 6mL aqueous solution, ultrasonically stirred until dissolved, and tris-HCl buffer solution was added to adjust the pH value to 8.5 to form a PEG-DSPE nanomicelle solution, and the concentration of PEG-DSPE nanomicelle was 15mg / mL.

[0045] Add 150 mg of dopamine hydrochloride to the above PEG-DSPE nanomicelle solution, stir and react for 12 hours under the condition that the opening of the reaction vessel is in convection with the outside air, to obtain a polymer drug carrier with a core-shell structure.

Embodiment 3

[0047] 100mgPEG 2000 -DSPE was dispersed in 10 mL of tris-HCl buffer solution with a concentration of 10 mmol / L to form a PEG-DSPE nanomicelle solution with a concentration of 10 mg / mL.

[0048] Add 10 mL of tris-HCl buffer solution (concentration 10 mmol / L, pH 8.0) dissolved with 150 mg of dopamine hydrochloride to the above-mentioned PEG-DSPE nanomicelle solution, stir and react for 48 h under the condition that the opening of the reaction vessel is in convection with the outside air, A polymeric drug carrier with a core-shell structure was obtained.

technical field

[0001] The invention belongs to the field of drug carriers, and relates to a polymer drug carrier and a preparation method thereof. Background technique

[0002] Polymer micelle was developed as a drug carrier in the 1990s. It is a self-assembled structure formed spontaneously by amphiphilic polymers in aqueous solution. The hydrophilic segments are outside, and the hydrophobic segments are aggregated to form nanomicelles. The diameter is generally 5-50nm, and it has the characteristics of high drug loading capacity, wide drug loading range, good stability, long residence time in the body, and improved drug stability.

[0003] Polyethylene glycol-distearoylphosphatidylethanolamine (PEG-DSPE) is a drug carrier material that is degradable in vivo and approved by the U.S. Food and Drug Administration (FDA). It has good biocompatibility and safety. But to make the PEG-DSPE polymer carrier multifunctional, it requires further modification, usually involving comp...

Examples

Embodiment 1

[0040] In this example, the polymer drug carrier is prepared by the following method, which includes the following steps:

[0041] 100mgPEG 2000 -DSPE was dispersed in 5mL methanol, stirred and dissolved, and the organic solvent was removed with a rotary evaporator to form a lipid film. A tris-HCl buffer solution with pH 8.5 was added to the lipid film to form a PEG-DSPE nanomicelle solution, wherein the concentration of the PEG-DSPE nanomicelle was 2 mg / mL.

[0042] 20 mg of dopamine hydrochloride was added to the above PEG-DSPE nanomicelle solution, and the reaction vessel was opened and stirred for 24 hours to obtain a polymer drug carrier with a core-shell structure.

Embodiment 2

[0044] 100mgPEG 2000 -DSPE was dispersed in 6mL aqueous solution, ultrasonically stirred until dissolved, and tris-HCl buffer solution was added to adjust the pH value to 8.5 to form a PEG-DSPE nanomicelle solution, and the concentration of PEG-DSPE nanomicelle was 15mg / mL.

[0045] Add 150 mg of dopamine hydrochloride to the above PEG-DSPE nanomicelle solution, stir and react for 12 hours under the condition that the opening of the reaction vessel is in convection with the outside air, to obtain a polymer drug carrier with a core-shell structure.

Embodiment 3

[0047] 100mgPEG 2000 -DSPE was dispersed in 10 mL of tris-HCl buffer solution with a concentration of 10 mmol / L to form a PEG-DSPE nanomicelle solution with a concentration of 10 mg / mL.

[0048] Add 10 mL of tris-HCl buffer solution (concentration 10 mmol / L, pH 8.0) dissolved with 150 mg of dopamine hydrochloride to the above-mentioned PEG-DSPE nanomicelle solution, stir and react for 48 h under the condition that the opening of the reaction vessel is in convection with the outside air, A polymeric drug carrier with a core-shell structure was obtained.

Images