Dual drug-loading composite microsphere and preparation method thereof

A technology of composite microspheres and double drug loading, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problem of excessive drug release and mechanical loss, and is not suitable for lipophilic drugs. Carriers, quality control and other issues, to achieve good biocompatibility and degradability, good biocompatibility, and increase compatibility

Inactive Publication Date: 2010-03-03
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the deficiencies of natural chitosan microspheres are: due to the different sources of each batch, there are differences in raw materials; too fast drug release and premature loss of mechanics caused by too fast degradation; and it is not suitable as a carrier for lipophilic drugs; Difficult to control quality etc.

Method used

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  • Dual drug-loading composite microsphere and preparation method thereof
  • Dual drug-loading composite microsphere and preparation method thereof
  • Dual drug-loading composite microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1: the preparation I of composite microsphere of the present invention

[0045] 1) Prepare PLGA internal microspheres Take 0.4mL of 5% (w / v) bovine serum albumin (BSA) aqueous solution and place in 2mL of PLGA containing 10% (w / v) (molecular weight 50KDa, LA: GA mole percentage is 75:25) in DCM solution, ultrasonic emulsification at 60w for 10 seconds, with an interval of 10 seconds, and repeat the "ultrasonic-interval" process 5 times to obtain an inner emulsion (w / o); in 30mL deionized water, add 0.3mL Tween 80, mechanically stirred until uniformly dispersed, and the outer water phase was obtained; the inner emulsion was added to the outer water phase, ultrasonically emulsified, and emulsified with an ultrasonic intensity of 400w for 10 seconds, with an interval of 10 seconds, and repeated 5 times to obtain a complex emulsion (w / o / w); the solution was stirred at a medium speed for 2 hours until the DCM was volatilized, and left to stand overnight. After c...

Embodiment 2

[0048] The preparation II of embodiment 2 composite microspheres of the present invention

[0049] 1) Preparation of PLGA internal microspheres

[0050] Get 0.2 mL of 5% bovine serum albumin (BSA) aqueous solution and place it in 2 mL of DCM solution containing 5% (w / v) PLGA (molecular weight 5KDa, LA: GA molar percentage is 75: 25), with 100w Intensity ultrasonic emulsification for 10 seconds, with an interval of 10 seconds, and repeat the "ultrasound-interval" process 5 times to obtain an inner emulsion (w / o); add 0.3mL Tween 80 to 30mL deionized water, stir mechanically until uniformly dispersed, and obtain The outer water phase; add the inner emulsion to the outer water phase, ultrasonically emulsify, emulsify with an ultrasonic intensity of 800w for 10 seconds, and repeat 3 times at intervals of 10 seconds to obtain a double emulsion (w / o / w); stir the liquid at a medium speed Wait for 2 hours for the DCM to volatilize, and let stand overnight. After centrifugation, wash...

Embodiment 3

[0052] Embodiment 3 Preparation III of composite microspheres of the present invention

[0053] 1) Preparation of PLGA internal microspheres

[0054] Take 0.2 mL of 5% gentamycin aqueous solution and place it in 2 mL of DCM solution containing 5% (w / v) PLGA (molecular weight 100 KDa, LA: GA mole percentage is 50: 50), and ultrasonically emulsify at 40 w 10 seconds, with an interval of 10 seconds, repeat the "ultrasound-interval" process 5 times to obtain the inner emulsion (w / o); add 0.3mL Tween 80 to 30mL deionized water, stir mechanically until the dispersion is uniform, and obtain the outer aqueous phase Add the inner emulsion to the outer water phase, supersonic emulsify, emulsify for 10 seconds with an ultrasonic intensity of 400w, and repeat 3 times at an interval of 10 seconds to obtain a double emulsion (w / o / w); stir the liquid at a medium speed for 2 hours and wait The DCM was evaporated and left to stand overnight. After centrifugation, wash with water three times ...

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Abstract

The invention discloses a dual drug-loading composite microsphere and a preparation method thereof, belonging to the technical field of biomedical materials. The composite microsphere has a microsphere-in-microsphere structure, a matrix consists of polylactic-co-glycolic acid microspheres in the interior and a chitosan shell at the outer layer, and drugs are respectively embedded in the interior microspheres and the shell, wherein the total drug-loading rate is 1 to 10 percent, the average grain diameter of the interior microspheres is 100-1000nm, and the average grain diameter of the composite microspheres is 10-100 mum. The invention also discloses the preparation method of the composite microsphere. The composite microsphere has good biocompatibility and biodegradability, and can control drug adding amount of the two times or the drug concentration or the drug species, thus reducing burst effect and alleviating the acidity caused by PLGA degradation.

Description

technical field [0001] The invention belongs to the technical field of biomedical materials, and in particular relates to a double-loaded composite microsphere and a preparation method thereof. Background technique [0002] In recent years, the research and application of polymer microsphere materials have developed very rapidly. This type of material has its special size and shape, and has special functions that other morphological materials do not have. In general, the application of polymer microspheres is divided into the following fields: nanotechnology, functional materials, analytical fields, biomedical fields, etc. In addition to the advantages of easy separation and purification that are unique to solid phase carriers, polymer microspheres also have the advantages of low cost, large specific surface area, good monodispersity, easy preparation and functionalization. The research on the use of microspheres as drug carriers began in the mid-1970s. Because of its targ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/36A61K38/00A61K38/18
Inventor 冯庆玲王明波
Owner TSINGHUA UNIV
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