2016•Zhongguo xin yao zazhiRequires access

Lyophilization of solid lipid nanoparticles loaded with brucine

Qingxia Guan, Yuwei Zhao, Zhenqiang Liu, Yufei Feng, Hua Xiao-dan, Zhao Yi-jun

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Abstract

Objectivet: To prepare and evaluate the quality of brucine solid lipid nanoparticles( B-SLN)lyophilized powder. Methods: Emulsification evaporation was employed to prepare B-SLN. Freeze-drying support agent and freeze drying process were screened to optimize the prescription of the lyophilized powder. TEM was used to observe B-SLN morphology; particle size and Zeta potential were measured by laser particle size analyzer; HPLC was used to determine the entrapment efficiency; the characterization was performed by differential thermal analysis. Results: B-SLN was spherical solid particles which dispersed uniformly. The average particle size was( 101. 3 ± 2. 2) nm,potential was(- 21. 6 ± 1. 6) mv,encapsulation rate was( 64. 88 ± 3. 9) %,and drug loading was( 2. 75 ± 20. 03) %. Differential thermal analysis showed that brunice existed in a non-crystalline state in BSLN,indicating that brunice may exist in solid lipid nanoparticles in a molecular or amorphous state. Conclusion:Using 0. 7% trehalose as cryoprotectant can obtain B-SLN with the smallest particle size,highest entrapment efficiency,good stability,and desirable appearance and redispersibility by the most reasonable preparation process.This study provides a reliable reference for future research.

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What this paper is about

Objectivet: To prepare and evaluate the quality of brucine solid lipid nanoparticles( B-SLN)lyophilized powder. Methods: Emulsification evaporation was employed to prepare B-SLN. Freeze-drying support agent and freeze drying process were screened to optimize the prescription of the lyophilized powder. TEM was used to observe B-SLN morphology; particle size and Zeta potential were measured by laser particle size analyzer; HPLC was used to determine the entrapment efficiency; the characterization was performed by differential thermal analysis. Results: B-SLN was spherical solid particles which dispersed uniformly. The average particle size was( 101. 3 ± 2. 2) nm,potential was(- 21. 6 ± 1. 6) mv,encapsulation rate was( 64. 88 ± 3. 9) %,and drug loading was( 2. 75 ± 20. 03) %. Differential thermal analysis showed that brunice existed in a non-crystalline state in BSLN,indicating that brunice may exist in solid lipid nanoparticles in a molecular or amorphous state. Conclusion:Using 0. 7% trehalose as cryoprotectant can obtain B-SLN with the smallest particle size,highest entrapment efficiency,good stability,and desirable appearance and redispersibility by the most reasonable preparation process.This study provides a reliable reference for future research.

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Available abstract

Objectivet: To prepare and evaluate the quality of brucine solid lipid nanoparticles( B-SLN)lyophilized powder. Methods: Emulsification evaporation was employed to prepare B-SLN. Freeze-drying support agent and freeze drying process were screened to optimize the prescription of the lyophilized powder. TEM was used to observe B-SLN morphology; particle size and Zeta potential were measured by laser particle size analyzer; HPLC was used to determine the entrapment efficiency; the characterization was performed by differential thermal analysis. Results: B-SLN was spherical solid particles which dispersed uniformly. The average particle size was( 101. 3 ± 2. 2) nm,potential was(- 21. 6 ± 1. 6) mv,encapsulation rate was( 64. 88 ± 3. 9) %,and drug loading was( 2. 75 ± 20. 03) %. Differential thermal analysis showed that brunice existed in a non-crystalline state in BSLN,indicating that brunice may exist in solid lipid nanoparticles in a molecular or amorphous state. Conclusion:Using 0. 7% trehalose as cryoprotectant can obtain B-SLN with the smallest particle size,highest entrapment efficiency,good stability,and desirable appearance and redispersibility by the most reasonable preparation process.This study provides a reliable reference for future research.

Key concepts: Solid lipid nanoparticle, Particle size, Brucine, Zeta potential, Differential scanning calorimetry, Freeze-drying, Chromatography, Nanoparticle

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