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盐霉素纳米结构脂质载体的制备及处方优化

韩翠艳 金珊珊 王晓丽 简白羽 隋小宇 曹立新

中国药房2018,Vol.29Issue(3):317-321,5.
中国药房2018,Vol.29Issue(3):317-321,5.DOI:10.6039/j.issn.1001-0408.2018.03.07

盐霉素纳米结构脂质载体的制备及处方优化

Preparation of Salinomycin Nanostructured Lipid Carriers and Formulation Optimization

韩翠艳 1金珊珊 1王晓丽 2简白羽 1隋小宇 1曹立新1

作者信息

  • 1. 齐齐哈尔医学院药学院, 黑龙江 齐齐哈尔 161006
  • 2. 北京万全德众医药科技股份有限公司制剂部, 北京 100000
  • 折叠

摘要

Abstract

OBJECTIVE: To prepare Salinomycin nanostructured lipid carriers (Sal-NLCs) and optimize its formulation. METHODS: Sal-NLCs was prepared by emulsion evaporation-low temperature solidification method. Using particle size, Zeta potential, encapsulation efficiency and drug loading as evaluation indexes, central composite design-response surface methodology was used to optimize the amount of Sal, the ratio of solid lipid glyceryl bisstearate to liquid lipid glyceryl octanoate in oil phase, ratio of surface active agent polyoxyethylene 35 castor oil (EL) to polyethylene glycol-15-hydroxy stearate (HS 15), the amount of polyoxyethylene (40) stearate (P40). The morphology, particle size, polydispersity index (PDI), Zeta potential, encapsulation efficiency, drug loading and in vitro release mechanism of Sal-NLCs were investigated. RESULTS: The optimal prescription was as follows as Sal 0. 86 mg, glyceryl bisstearate 40.70 mg, glyceryl octanoate 11.30 mg, EL 44.05 mg, HS15 7.95 mg, P40 3.8 mg. Prepared Sal-NLCs was round-like and dispersed evenly. The particle size, PDI, Zeta potential, encapsulation efficiency and drug loading of prepared Sal-NLCs were(81.81 ± 2.60) nm, 0.183 ± 0.042, (-24.9 ± 3.4) mV,(94.35 ± 1.50)% and (1.47 ±0.04)% (n=5), respectively.24 h accumulative release rate was (99.81 ± 3.90)% (n=3).Drug release behavior was in line with Higuchi model, and relative error of particle size, Zeta-potential, encapsulation efficiency and drug loading to predicted value of model were all lower than 4%. CONCLUSIONS: Sal-NLCs with sustained-release effect is prepared successfully according to optimized formulation, and its quality meets the expected standard.

关键词

盐霉素/纳米结构脂质载体/熔融乳化-低温固化法/星点设计-响应面法/处方优化

Key words

Salinomycin/Nanostructured lipid carriers/Emulsion evaporation-low temperature solidification method/Central composite design-response surface methodology/Formulation optimization

分类

医药卫生

引用本文复制引用

韩翠艳,金珊珊,王晓丽,简白羽,隋小宇,曹立新..盐霉素纳米结构脂质载体的制备及处方优化[J].中国药房,2018,29(3):317-321,5.

基金项目

黑龙江省自然科学基金资助项目(No. H2015070) (No. H2015070)

中国药房

OA北大核心CSTPCD

1001-0408

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