Composite drug-loading sustained release microsphere system entrapped with quantum dots and preparation method of composite drug-loading sustained release microsphere system

A technology of drug-loaded microspheres and quantum dots, applied in the field of medicine, can solve the problems of poor hydrophilicity, difficult gene carrier, and difficult multi-functional modification, and achieve the effect of good stability and simple preparation process

Active Publication Date: 2012-07-04
JIANGSU ZODIAC MARINE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PLGA, as a drug carrier, has certain defects: (1) poor hydrophilicity; (2) the surface functional groups of PLGA microspheres are few, making it difficult to carry out multifunctional modification; (3) the surface of PLGA microspheres is negatively charged, making it difficult to use Gene carrier

Method used

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  • Composite drug-loading sustained release microsphere system entrapped with quantum dots and preparation method of composite drug-loading sustained release microsphere system
  • Composite drug-loading sustained release microsphere system entrapped with quantum dots and preparation method of composite drug-loading sustained release microsphere system
  • Composite drug-loading sustained release microsphere system entrapped with quantum dots and preparation method of composite drug-loading sustained release microsphere system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation process of composite drug-loaded microspheres. The anticancer drug used is water-soluble drug epirubicin, and the quantum dots used are red cadmium selenide quantum dots with a particle diameter of 10 nanometers. The mass proportioning of raw materials is as follows:

[0031] PLGA:PVA=1:2;

[0032] PLGA: epirubicin: quantum dots=60:5:1;

[0033] RGD-OQLCS:Chol=2:1;

[0034] Polymer lipid film: PLGA drug-loaded microspheres = 1:1.

[0035] (1) Weigh 5 mg of epirubicin and dissolve it in 1 mL of distilled water, and set aside; weigh 60 mg of PLGA and place it in a small beaker, add 3 mL of dichloromethane to dissolve it completely, add 1 mg of quantum dots, and use an ultrasonic cell pulverizer at 50W Ultrasound at high power. Add epirubicin aqueous solution to the small beaker during ultrasonication, and continue ultrasonication until a uniform water-in-oil emulsion is formed;

[0036] (2) Pour the sonicated solution in the small beaker into a beaker fi...

Embodiment 2

[0042] Preparation process of composite drug-loaded microspheres. The anticancer drug used is paclitaxel, an oil-soluble drug, and the quantum dots used are green cadmium selenide quantum dots with a particle diameter of 5 nanometers. The mass proportioning of raw materials is as follows:

[0043] PLGA:PVA=1:1;

[0044] PLGA: paclitaxel: quantum dots = 30:8:5;

[0045] RGD-OQLCS:Chol=4:1;

[0046] Polymer lipid film: PLGA drug-loaded microspheres = 4:1.

[0047] (1) Weigh 30mg of PLGA and place it in a small beaker, add 3mL of dichloromethane to dissolve it completely, add 5mg of quantum dots and 8mg of paclitaxel, so that the quantum dots are evenly dispersed, and the paclitaxel is completely dissolved;

[0048] (2) Pour the solution in the small beaker into a beaker filled with 10 mL of PVA solution with a concentration of 3 mg / mL, and use an ultrasonic cell pulverizer to perform ultrasound at a power of 100 W until a uniform emulsion is formed;

[0049] (3) Stir with a...

Embodiment 3

[0054] Preparation process of composite drug-loaded microspheres. The anticancer drug used is vincristine, a water-soluble drug, and the quantum dots used are red cadmium selenide quantum dots with a particle diameter of 7 nanometers. The mass proportioning of raw materials is as follows:

[0055] PLGA:PVA=1:1.5;

[0056] PLGA: vincristine: quantum dots=100:10:3;

[0057] RGD-OQLCS:Chol=3:1;

[0058] Polymer lipid film: PLGA drug-loaded microspheres = 2.5:1.

[0059] (1) Weigh 5 mg of vincristine and dissolve it in 1 mL of distilled water for use; weigh 50 mg of PLGA and place it in a small beaker, add 3 mL of dichloromethane to dissolve it completely, add 1.5 mg of quantum dots, and use an ultrasonic cell pulverizer at 200W Ultrasound at high power. Add vincristine aqueous solution to the small beaker during the ultrasonication process, and continue ultrasonication until a uniform water-in-oil emulsion is formed;

[0060] (2) Pour the sonicated solution in the small bea...

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Abstract

The invention relates to a composite drug-loading sustained release microsphere system entrapped with quantum dots and a preparation method of the composite drug-loading sustained release microsphere system. The quantum dots and an anti-cancer medicament are entrapped in a polylactic-co-glycolic acid microsphere, and a cationic macromolecular liposome prepared from arginine-glycine-aspartic acid (RGD) peptide-modified octadecyl-quaternized lysine modified chitosan and cholesterol is coated outside the polylactic-co-glycolic acid microsphere to form a core-shell drug-loading microsphere system. The composite drug-loading microsphere system entrapped with the quantum dots and the anti-cancer medicament has the particle size being between 300 and 400nm, positive surface Zeta potential and high stability, and can be stored for at least two months after being freeze-dried. The composite drug-loading sustained release microsphere system entrapped with the quantum dots and the anti-cancer medicament has the characteristics of uniform and controllable particle size, high stability, RGD peptide modification on surface, simple preparation process and the like, and is suitable for batch production.

Description

technical field [0001] The invention relates to a sustained-release composite drug-loaded microsphere system loaded with quantum dots and anticancer drugs and a preparation method thereof, belonging to the technical field of drugs. Background technique [0002] Polylactic acid-glycolic acid copolymer (PLGA) is formed by random polymerization of lactic acid and glycolic acid. It is a degradable functional polymer organic compound with good biocompatibility and biodegradability, non-toxic, good It has excellent encapsulation and film-forming properties and is widely used in pharmaceuticals, medical engineering materials and modern industrial fields. Because of its safety, reliability, good biocompatibility, and controllable biodegradability, it has shown important and broad application prospects in drug controlled release and surgical anastomosis repair. [0003] PLGA has the following advantages as a slow-release microsphere drug carrier: (1) non-toxic, it can be degraded in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/36A61K47/02A61P35/00
Inventor 常津王亮亮王生苏文雅王汉杰
Owner JIANGSU ZODIAC MARINE BIOTECH
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