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Preparation of Rutin-loaded Solid Lipid Nanoparticles Using Emulsion Evaporation at a High temperature and Solidification at a low Temperature and Their Physicochemical Properties

Wang Fang

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Abstract

Objective To prepare rutin-loaded solid lipid nanoparticles(RT-SLN)using emulsion evaporation at a high temperature and solidification at a low temperature and investigate its physicochemical properties and release behavior in vitro.Methods RT-SLN was prepared with the method of emulsion evaporation at a high temperature and solidification at a low temperature.Stearic acid with high biocompatibility was used as lipid carrier.The optimum formulation was selected by uniform design,the morphology,particle size and size distribution,Zeta potential,entrapment efficiency(EE)and release behavior in vitro were evaluated.Results The obtained RT-SLN was spherical with mean particle size of(192.47±31.8)nm,Zeta potential of(-18.90±0.27)mV.The formulation using the EE as the indicator was screened and the optimized procedure parameters were obtained:drug-stearic acid 1∶4,stearic acid amount 200 mg,Tween-80 concentration 12 mg/ml,PEG-400 concentration 5%,rotation rate 1500 rpm,the ration of volume of coarse emulsion and disperse phase was 1∶7,the calculated EE was 90.11%(95% confidence interval:83.71%~96.51%),the average EE was(89.34±0.93)%.The in vitro release profile of the nanopartilces was expressed well by Higuchi equation:Q=8.345 t1/2+15.023(r=0.9892),85% was released at 72 h.Conclusion RT-SLN with sustained released property can be prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature.RT-SLN can lead to steady blood curve which is beneficial for the patients's compliance.

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Objective To prepare rutin-loaded solid lipid nanoparticles(RT-SLN)using emulsion evaporation at a high temperature and solidification at a low temperature and investigate its physicochemical properties and release behavior in vitro.Methods RT-SLN was prepared with the method of emulsion evaporation at a high temperature and solidification at a low temperature.Stearic acid with high biocompatibility was used as lipid carrier.The optimum formulation was selected by uniform design,the morphology,particle size and size distribution,Zeta potential,entrapment efficiency(EE)and release behavior in vitro were evaluated.Results The obtained RT-SLN was spherical with mean particle size of(192.47±31.8)nm,Zeta potential of(-18.90±0.27)mV.The formulation using the EE as the indicator was screened and the optimized procedure parameters were obtained:drug-stearic acid 1∶4,stearic acid amount 200 mg,Tween-80 concentration 12 mg/ml,PEG-400 concentration 5%,rotation rate 1500 rpm,the ration of volume of coarse emulsion and disperse phase was 1∶7,the calculated EE was 90.11%(95% confidence interval:83.71%~96.51%),the average EE was(89.34±0.93)%.The in vitro release profile of the nanopartilces was expressed well by Higuchi equation:Q=8.345 t1/2+15.023(r=0.9892),85% was released at 72 h.Conclusion RT-SLN with sustained released property can be prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature.RT-SLN can lead to steady blood curve which is beneficial for the patients's compliance.

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Available abstract

Objective To prepare rutin-loaded solid lipid nanoparticles(RT-SLN)using emulsion evaporation at a high temperature and solidification at a low temperature and investigate its physicochemical properties and release behavior in vitro.Methods RT-SLN was prepared with the method of emulsion evaporation at a high temperature and solidification at a low temperature.Stearic acid with high biocompatibility was used as lipid carrier.The optimum formulation was selected by uniform design,the morphology,particle size and size distribution,Zeta potential,entrapment efficiency(EE)and release behavior in vitro were evaluated.Results The obtained RT-SLN was spherical with mean particle size of(192.47±31.8)nm,Zeta potential of(-18.90±0.27)mV.The formulation using the EE as the indicator was screened and the optimized procedure parameters were obtained:drug-stearic acid 1∶4,stearic acid amount 200 mg,Tween-80 concentration 12 mg/ml,PEG-400 concentration 5%,rotation rate 1500 rpm,the ration of volume of coarse emulsion and disperse phase was 1∶7,the calculated EE was 90.11%(95% confidence interval:83.71%~96.51%),the average EE was(89.34±0.93)%.The in vitro release profile of the nanopartilces was expressed well by Higuchi equation:Q=8.345 t1/2+15.023(r=0.9892),85% was released at 72 h.Conclusion RT-SLN with sustained released property can be prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature.RT-SLN can lead to steady blood curve which is beneficial for the patients's compliance.

Key concepts: Stearic acid, Solid lipid nanoparticle, Emulsion, Zeta potential, Particle size, Materials science, Rutin, Chromatography

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