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Polyelectrolyte modified graphene oxide anti-cancer drug preparation and preparation method thereof

A technology of anti-cancer drugs and polyelectrolytes, which is applied in the direction of pharmaceutical formulations, anti-tumor drugs, drug combinations, etc., can solve problems affecting the residence time of preparations, space blockage, etc., and achieve enhanced anti-tumor efficacy, delayed release speed, and delayed clearance. Effect

Inactive Publication Date: 2017-11-07
LIAONING UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] After oral administration, most nano drug delivery systems are trapped by the mucus layer due to space obstruction or adhesion, and then cleared within minutes to hours as the mucus layer is renewed, which seriously affects the local residence time of the preparation.

Method used

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  • Polyelectrolyte modified graphene oxide anti-cancer drug preparation and preparation method thereof
  • Polyelectrolyte modified graphene oxide anti-cancer drug preparation and preparation method thereof
  • Polyelectrolyte modified graphene oxide anti-cancer drug preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) GO loaded drug Pingyangmycin (PYM)

[0045] 1. The preparation method comprises the following steps:

[0046] 1) Weigh 200 mg of graphene oxide GO into an EP tube, add 100 mL of PBS buffer, and dissolve it fully by ultrasonication.

[0047] 2) Weigh 100mg of PYM into a beaker filled with 1000mL of distilled water to dissolve.

[0048] 3) Under the condition of magnetic stirring, the PBS solution of GO in the EP tube was dropped into the aqueous solution of PYM in the beaker, and the drug was loaded onto the graphene oxide GO by ultrasound.

[0049] 4) The solution was centrifuged at 10,000 rpm for 20 minutes with a high-speed centrifuge to remove free PYM. The lower precipitate was collected and redissolved to obtain GO-PYM.

[0050] 2. Calculation of encapsulation rate

[0051] The encapsulation efficiency of GO-PYM drug loading system was determined by high performance liquid chromatography.

[0052] 1) The conditions of PYM liquid chromatography are: chromatog...

Embodiment 2

[0097] The synthesis of embodiment 2PAA-CYs / PAH-GO-PYM (PCPGP)

[0098] (1) Synthetic method of PAA-CYs / PAH-GO-PYM

[0099]1) Weigh 200 mg of graphene oxide GO into an EP tube, add 100 mL of PBS buffer, and dissolve it fully by ultrasonication. Weigh 100mg of PYM into a beaker filled with 1000mL of distilled water to dissolve. Under the condition of magnetic stirring, the GO solution in the EP tube was dropped into the beaker of PYM, ultrasonicated for 30 min, and the obtained solution was centrifuged at 10,000 rpm for 20 min in a high-speed centrifuge to remove free PYM. The lower precipitate was collected, reconstituted and lyophilized to obtain GO-PYM.

[0100] 2) Weigh 200mg of GO-PYM and dissolve it in 90mL of distilled water, heat to 45°C, add 78mg of polyallylamine hydrochloride PAH and 1910mg of condensing agent EDC, stir and react, and dialyze the solution for 36h by dialysis to obtain PAH- GO-PYM;

[0101] 3) Dissolve 720mg (0.01mol) of PAA in 10ml of water, adju...

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Abstract

The invention relates to a polyelectrolyte modified graphene oxide anti-cancer drug preparation and a preparation method thereof. The method comprises the following steps: utilizing a charge attracting principle to respectively coat poly allylamine hydrochloride PAH with positive charges, polyacrylic acid PAA with negative charges and cysteine CYs onto a graphene oxide GO surface loaded with an anti-cancer drug and lastly acquiring PAA-CYs / PAH-GO-X. The preparation provided by the invention is coated with two layers of polyelectrolyte, so that the drug can be protected under a strong acidic environment and ultrahigh strong acid resistance stability is represented; the surface is coated with the PAA-CYs, so that the drug preparation is adhered to the inner wall of intestinal tract and a better intestinal absorption effect is achieved; in vitro release and pharmacokinetics prove the preparation has a certain slow release effect; a drug carrier system provided by the invention can effectively promote the orally taken bioavailability of the anti-cancer drug, can be applied to anti-cancer research and has ultrahigh application value for clinical research.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical preparation for oral delivery of anticancer drugs by polyelectrolyte-modified graphene oxide and a preparation method thereof. Background technique [0002] GO is a hydrophilic material, and its surface has hydroxyl, carboxyl and epoxy groups and a large number of oxygen-containing polar groups. It is a hydrophilic material, and the surface-modified GO can be stable in high-salt solution and physiological solution. The carbon atoms in the GO structure form stable chemical bonds with the drug structure, so a large number of bioactive molecules can be adsorbed through π-π conjugation and hydrophobic interactions. Currently, research focuses on the biocompatibility of GO, and the mechanism of the interaction between GO and the body is still in its infancy. The specific physiological mechanism of GO in the body remains to be further studied, especially as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/04A61K47/18A61K47/32A61K31/337A61K31/704A61K38/14A61K31/517A61P35/00
CPCA61K9/0002A61K9/0053A61K31/337A61K31/517A61K31/704A61K38/14A61K47/02A61K47/18A61K47/32
Inventor 刘宇贾德超陈立江吴昊天
Owner LIAONING UNIVERSITY
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