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Method for preparing colon-targeted microcapsules by applying microfluid technology

A colon-targeting and microfluidic technology, which is applied in the preparation, application, and microcapsules of microspheres, can solve the problems of unfriendly bioactive proteins, long preparation process, easy inactivation and decomposition of proteins, etc., and achieve good biocompatibility and degradability, to achieve colon-specific release, to protect the structure and activity

Active Publication Date: 2021-04-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The common shortcoming of these methods is: 1, can't precisely control microcapsule structure, mechanical emulsification can't prepare the double emulsion of uniform single core-shell structure, can't control the core number of double emulsion, and the particle diameter of core-shell, cause active compound Controlled release performance and poor stability
2. The preparation process needs to provide a lot of mechanical force, the preparation process takes a long time, is extremely unfriendly to the biologically active protein, the protein is easily deactivated and decomposed, the stability is poor, and the encapsulation efficiency is low

Method used

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  • Method for preparing colon-targeted microcapsules by applying microfluid technology
  • Method for preparing colon-targeted microcapsules by applying microfluid technology
  • Method for preparing colon-targeted microcapsules by applying microfluid technology

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Construction of a glass microfluidic device

[0058] The glass microfluidic device is a self-made one-step double-emulsion device, including an internal phase capillary, a collection tube, a square tube, and two injection needles; a capillary of appropriate length (outer diameter 960 μm, inner diameter 550 μm) was burnt and pulled into a Two capillaries with sharp ends were ground with a needle grinder until the tip diameters were 20-100 μm and 150-400 μm, respectively, as the internal phase capillary and the emulsion collection tube. Specifically, the tip diameter of the internal phase capillary is 60 μm, the tip diameter of the collection tube is 350 μm, the outer diameter of the square tube is 1.4 mm, and the inner diameter is 1.1 mm. The square tube is fixed at the center of the slide, and the tip of the internal phase capillary is inserted into the square tube. In the middle position, the other end of the internal phase liquid inlet capillary protrudes a...

Embodiment 2

[0059] Embodiment 2: Preparation and characterization of modified chitosan

[0060] (1) Preparation of modified chitosan

[0061] Weigh 1.0g of chitosan and place it in a 250mL round bottom flask, add 99mL of ultrapure water, add 1mL of acetic acid under magnetic stirring, until the chitosan is completely dissolved, add 1-5mL of 2-methacrylic anhydride solution, 60 ℃, 1000r / min reaction for 10h, the reaction solution was cooled to room temperature, and saturated Na 2 CO 3 Adjust the pH of the aqueous solution to 7.0, put the reaction solution into a 3.5K cellulose dialysis bag, dialyze for 72 hours in pure water to remove small molecular substances in the reaction solution, and finally freeze-dry the solution to obtain a white spongy substance, which is modified chitosan.

[0062] (2) Fourier transform infrared spectroscopic analysis

[0063] Using infrared spectroscopy to analyze the chemical structure of modified chitosan, 400~4000cm -1 The solid samples of modified and ...

Embodiment 3

[0070] Embodiment 3: the preparation of microcapsule

[0071] (1) Preparation of three-phase solution

[0072] The modified chitosan obtained in Example 2 is dissolved in 1% (v / v) aqueous acetic acid solution, stirred until completely dissolved, and the prepared concentration (w / v) is 1%, 1.5%, 2% (w / v ) modified chitosan aqueous solution. Then add 1mol / L NaOH solution dropwise in the modified chitosan aqueous solution, adjust the pH to 7.0, use bovine serum albumin as the model protein, add bovine serum albumin in the modified chitosan solution and stir until completely dissolved, The protein concentration (w / v) is 1%, 5%, 10%, 15%, then add 2-hydroxy-2-methyl propiophenone, the concentration is 0.1% (v / v), stir vigorously until the dispersion is even, static Place to remove air bubbles to obtain an internal phase aqueous solution containing protein and core material; add ethyl cellulose to dichloromethane, keep in a closed place in the dark until the ethyl cellulose is com...

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Abstract

The invention discloses a method for preparing colon-targeted microcapsules by using a microfluid technology. The method comprises the following steps of S1, dissolving modified chitosan in an acetic acid aqueous solution, regulating the pH value to 7.0, and dissolving a photoinitiator and model protein in the acetic acid aqueous solution to obtain an internal phase solution; S2, dissolving ethyl cellulose in dichloromethane to prepare an intermediate phase solution; S3, dissolving polyvinyl alcohol in pure water to prepare a continuous phase solution; S4, wrapping the internal phase solution obtained in the step S1 in droplets of the intermediate phase solution obtained in the step S2, dispersing the droplets in the continuous phase solution obtained in the step S3, and preparing a W / O / W emulsion in one step; S5, irradiating the emulsion obtained in the step S4 with ultraviolet light to solidify the inner phase into a spherical core, and heating to volatilize the organic solvent completely to solidify the intermediate phase into a capsule shell; and S6, washing the microcapsules cured in the step S5 with pure water for multiple times, and performing freeze drying. The microcapsules prepared by the method has a colon-specific release effect and is used for protein embedding and oral delivery.

Description

technical field [0001] The invention relates to the preparation of colon-targeted microcapsules, in particular to a method for preparing microcapsules using a double emulsion as a template using microfluidic technology. Background technique [0002] In addition to being used as nutrients, bioactive proteins can also prevent or alleviate certain diseases, and have great nutritional and health value. However, in the field of food and health care, it is difficult for bioactive protein to exert its beneficial effect on health, mainly because protein is easily inactivated and degraded in the digestive system of the gastrointestinal tract after ingestion, and it is difficult to absorb. It is of great significance and market value to develop oral protein delivery systems to protect them from degradation and to release and absorb them in target areas of the gastrointestinal tract. [0003] Microencapsulation technology is to wrap the core material such as protein in the wall layer ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/36A61K47/38A61K38/00B01J13/04B01J19/00A23L33/17A23L33/18A23L29/30A23P10/30
CPCA61K9/5042A61K9/5036A61K38/00B01J19/0093B01J13/046A23L33/17A23L33/18A23L29/30A23P10/30A23V2002/00A23V2200/32A23V2250/511A23V2250/51088A23V2250/54A23V2250/55Y02A50/30
Inventor 王志祥朱蜜蜜王新杨倩袁彪
Owner CHINA PHARM UNIV
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