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Composite drug carried microsphere, minocycline hydrochloride nano controlled-release composite drug carried microsphere system and preparation method thereof

A technology of minocycline hydrochloride and drug-loaded microspheres, which is applied in the field of medicine, can solve the problems of increased cytotoxicity, decreased drug-loading rate, and poor hydrophilicity, and achieves a simple and quick preparation process, reduced toxicity, and strong antibacterial activity. Effect

Inactive Publication Date: 2012-05-30
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] 1) Poor hydrophilicity;
[0012] 2) The PLGA terminal chain contains carboxyl groups and is negatively charged, thus increasing the cytotoxicity of the carrier itself
[0013] Conventional liposomes prepared from traditional lecithin and cholesterol (Chol) are coated on the outer surface of PLGA drug-loaded microspheres to form a composite drug-loading system, which neutralizes the negative charge of PLGA to a certain extent and increases its Hydrophilic, but at the same time brings the defects of a significant increase in particle size and a decrease in drug loading rate

Method used

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  • Composite drug carried microsphere, minocycline hydrochloride nano controlled-release composite drug carried microsphere system and preparation method thereof
  • Composite drug carried microsphere, minocycline hydrochloride nano controlled-release composite drug carried microsphere system and preparation method thereof
  • Composite drug carried microsphere, minocycline hydrochloride nano controlled-release composite drug carried microsphere system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Raw material mass ratio is as follows:

[0055] PLA-b-PGA:PVA=1:2

[0056] PEG-OQCMC:OQCMC=1:2

[0057] Total copies of PEG-OQCMC and OQCMC: Chol=2:1

[0058] Cationic polymer liposomes: PLGA microspheres = 1:1

[0059] (1) Pour 5ml of PVA solution with a concentration of 40mg / ml into a beaker, perform ultrasonication with an ultrasonic cell pulverizer with a power of 200W, add 5ml of a PLA-b-PGA solution with a concentration of 20mg / ml, and continue ultrasonication. Uniform opalescent liquid can be stopped, so as to prepare PLGA microspheres. After magnetic stirring for 24 hours, wash with distilled water at least three times, and vacuum freeze-dry.

[0060] (2) Weigh 10 mg PEG-OQCMC, 20 mg OQCMC, and 15 mg Chol, and dissolve them in 4 ml of dichloromethane. The mixture was placed in an eggplant-shaped bottle, and was rotated at 35° C. on a rotary evaporator at a rotational speed of 50 r / min, and at the same time, a nitrogen stream was passed into the rotary evapo...

Embodiment 2

[0063] Raw material mass ratio is as follows:

[0064] PLA-b-PGA:PVA=1:1

[0065] PEG-OQCMC:OQCMC=1:1

[0066] Total copies of PEG-OQCMC and OQCMC: Chol=4:1

[0067] Cationic polymer liposomes: PLGA microspheres = 2:1

[0068] (1) Pour 5ml of PVA solution with a concentration of 20mg / ml into a beaker, perform ultrasonication with an ultrasonic cell pulverizer at a power of 110W, add 5ml of a PLA-b-PGA solution with a concentration of 20mg / ml, and continue ultrasonication. Uniform opalescent liquid can be stopped, so as to prepare PLGA microspheres. After magnetic stirring for 24 hours, wash with distilled water at least three times, and vacuum freeze-dry.

[0069] (2) Weigh 20mg PEG-OQCMC, 20mgOQCMC, 10mgChol, and dissolve in 4ml dichloromethane. The mixture was placed in an eggplant-shaped bottle, and was rotated at 40° C. on a rotary evaporator at a rotational speed of 45 r / min, and at the same time, nitrogen flow was passed into the rotary evaporator for protection. A...

Embodiment 3

[0072] Raw material mass ratio is as follows:

[0073] PLA-b-PGA:PVA=1:1.5

[0074] PEG-OQCMC:OQCMC=2:1

[0075] Total copies of PEG-OQCMC and OQCMC: Chol=2.5:1

[0076] Cationic polymer liposomes: PLGA microspheres = 1.4:1

[0077] (1) Pour 5ml of PVA solution with a concentration of 30mg / ml into a beaker, perform ultrasonication with an ultrasonic cell pulverizer at a power of 150W, add 5ml of a PLA-b-PGA solution with a concentration of 20mg / ml, and continue ultrasonication. Uniform opalescent liquid can be stopped, so as to prepare PLGA microspheres. After magnetic stirring for 24 hours, wash with distilled water at least three times, and vacuum freeze-dry.

[0078] (2) Weigh 20 mg PEG-OQCMC, 10 mg OQCMC, and 12 mg Chol, and dissolve them in 4 ml of dichloromethane. The mixture was placed in an eggplant-shaped bottle, and was rotated at 32° C. on a rotary evaporator at a rotational speed of 55 r / min, and at the same time, nitrogen flow was passed into the rotary evapo...

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Abstract

The invention relates to a composite drug carried microsphere, a minocycline hydrochloride nano controlled-release composite drug carried microsphere system and a preparation method thereof. A drug carried system with a nuclear shell structure is formed by embedding minocycline hydrochloride inside a poly D,L-lactide-co-glycolic acid polymer microsphere and covering a cationic polymeric liposome prepared from O-QACMC modified by polyethylene glycol, O-QACMC and cholesterol outside the poly D, L-lactide-co-glycolic acid polymer microsphere; and the composite drug carried microsphere system covered and carried with the minocycline hydrochloride has the grain diameter ranging from 340 nm to 400 nm and positive surface Zeta electric potential. The composite drug carried microsphere system canbe remained in a water solution for at least 2 months, has high entrapment rate reaching larger than 90 percent on drugs and strong drug carrying capacity reaching 9 percent. The minocycline hydrochloride nano controlled-release composite drug carried microsphere system has the characteristics of uniform and controllable grain diameter, good preparation stability, simple preparation process, highdrug carrying rate, favorable controlled release function, and the like, and is suitable for batch production.

Description

technical field [0001] The invention relates to a novel composite drug-loaded microsphere, a minocycline hydrochloride sustained-release composite drug-loaded microsphere system and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Carboxymethyl chitosan is a water-soluble chitosan derivative, which contains negatively charged carboxyl groups and positively charged amino groups in its molecule, and is an amphoteric polymer; chitosan quaternary ammonium salt has excellent The mucosal permeability, high zeta potential and can be used as a gene carrier are favored by researchers, and carboxymethyl chitosan is quaternized with dimethyloctadecylglycidyl ammonium chloride Preparation of carboxymethyl chitosan quaternary ammonium salt will endow chitosan quaternary ammonium salt with better antibacterial properties. At the same time, the introduction of long-chain alkyl quaternary ammonium salts on carboxymethyl chitosan can...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/36A61K31/65A61P31/04A61K47/28
Inventor 常津苏文雅王汉杰胡秀凤廖振宇
Owner TIANJIN UNIV
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