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Controllable emulsifying preparation method of PLGA micro-nano carriers of different scales

A PLGA, micro-nano technology, applied in the directions of non-active ingredients medical preparations, pharmaceutical formulas, emulsion delivery, etc., can solve the problems of inconsistency, difference in preparation technology, and unfavorable conversion.

Inactive Publication Date: 2016-09-21
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation of PLGA microcarriers mainly includes methods such as emulsification, crosslinking, and physical encapsulation, but only for a single scale, such as nano or micro carriers.
The preparation techniques of PLGA micro-nano carriers of different scales are significantly different, and the reagents used are different, which is not conducive to conversion through simple adjustments. There is no controllable and convenient process for preparing PLGA micro-nano carriers of different scales.

Method used

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  • Controllable emulsifying preparation method of PLGA micro-nano carriers of different scales
  • Controllable emulsifying preparation method of PLGA micro-nano carriers of different scales

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 60 mg of PLGA (LA / GA=75 / 25, Mw=40 K) and dissolve it in 10 mL of ethyl acetate as the oil phase. Tween 80 and Span 80 are surfactants with HLB value of 12.5, mixed with oil phase. The mixture was added dropwise into 0.5% (w / v) hydroxyethylcellulose deionized aqueous solution with a syringe, stirred continuously at 1000 rpm, and reacted for 10 min. The total volume of the emulsion was fixed at 32 mL, where oil phase:water phase:surfactant=1.5:30:0.5 (v / v). Ethyl acetate was removed by rotating the emulsion under reduced pressure at room temperature, filtered to obtain a solid, washed three times with deionized water, and freeze-dried to obtain PLGA microcarriers. The average particle size is 150±5.6 μm.

Embodiment 2

[0020] Weigh 60 mg of PLGA (LA / GA=50 / 50, Mw=38 K) and dissolve it in 10 mL of ethyl acetate as the oil phase. Tween 80 and Span 80 are surfactants with an HLB value of 14, which are mixed with the oil phase. The mixture was added dropwise into 0.5% (w / v) hydroxyethylcellulose deionized aqueous solution with a syringe, stirred continuously at 1000 rpm, and reacted for 10 min. The total volume of the emulsion was fixed at 32 mL, where oil phase:water phase:surfactant=1.75:30:0.25 (v / v). Ethyl acetate was removed by rotating the emulsion at room temperature under reduced pressure, and the solid was obtained by filtration. The filter residue was washed three times with deionized water, and lyophilized to obtain PLGA microcarriers. The average particle size is 225±6.7 μm.

Embodiment 3

[0022] Weigh 10 mg of PLGA (LA / GA=75 / 25, Mw=40 K) and dissolve it in 10 mL of ethyl acetate as the oil phase. Tween 80 and Span 80 are surfactants with HLB value of 13, mixed with oil phase. The mixture was added dropwise into 0.1% (w / v) hydroxyethylcellulose deionized aqueous solution with a syringe, and stirred to form a primary emulsion. The obtained colostrum was ultrasonically mixed, the ultrasonic power was 200 W, the time was 180, 2 s on and 2 s off. The total mass of the emulsion is fixed at 12 g, where oil phase: water phase: surfactant = 1.75: 10: 0.25 (m / m). Ethyl acetate was removed by rotating the emulsion at room temperature under reduced pressure, centrifuged to obtain a solid, washed three times with deionized water, each time for 10 min, and the rotation speed was 8500 rpm, and freeze-dried to obtain PLGA nanocarriers. The average particle size is 330±4.3 μm.

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Abstract

The invention relates to a controllable emulsifying preparation method of PLGA micro-nano carriers of different scales. According to the preparation method, PLGA is dissolved in ethyl acetate to serve as an oil phase, polysorbate and sorbitan fatty acid ester form a mixed nonionic surfactant, a solution containing stabilizer hydroxyethyl cellulose serves as a water phase, O / W PLGA micro / nano emulsion with a stable structure and a uniform particle size can be obtained by controlling the quality or volume of the system, adjusting the component ratio of the water phase, the oil phase and the surfactant and changing uniform mixing manner, and the PLGA micro / nano carriers are obtained by carrying out reduced-pressure rotary distillation at room temperature to remove ethyl acetate, washing with deionized water, separating and drying. The particle sizes of the PLGA micro / nano carriers can be adjusted under single scale by adjusting the hydrophilic / hydrophobic equilibrium value of the mixed nonionic surfactant. The prepared PLGA micro / nano carriers can meet the requirement of different administration manners and loading substances for the particle size of the carrier.

Description

technical field [0001] The invention relates to the preparation technology of polymer micro-carriers, in particular to a controllable emulsification preparation method of PLGA micro-nano carriers of different scales. Background technique [0002] Polylactic acid-glycolic acid (PLGA) is a biodegradable and controllable functional polymer organic compound, non-toxic, and has good biocompatibility, cystic and film-forming properties, because Two monomers - lactic acid and glycolic acid are polymerized. The ratio of lactic acid (LA) to glycolic acid (GA) affects the mechanical strength and degradability of PLGA. In the United States, PLGA has passed FDA certification and has been officially included in the United States Pharmacopoeia as a pharmaceutical excipient. It has a wide range of uses in the field of biomedical engineering: it has been made into degradable sutures, drug sustained-release carriers and tissue engineering scaffold materials. Among them, PLGA microspheres, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/38A61K47/26
CPCA61K9/1075A61K47/26A61K47/34A61K47/38
Inventor 孔明朱明哲陈西广冯超程晓杰刘雅
Owner OCEAN UNIV OF CHINA
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