海参皂苷nobilisideA注射用脂质体冻干制剂的制备及其性质考察
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国家高科技研究发展计划(“863”计划,2006AA090304)


Preparation and characterization of Holothuria nobilis saponins nobilisideA freeze-dried liposome
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Supported by the National High-tech R&D Program(“863 Program”,2006AA090304).

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    摘要:

    目的:制备海参皂苷nobilisideA冻干脂质体并对其性质进行考察。方法:采用薄膜分散法制备了nobilisideA脂质体并将其冻干制成nobilisideA冻干粉,测定冻干脂质体的药物含量和包封率、粒径、ζ电位等指标,考察其与葡萄糖配伍的稳定性和溶血性,了解nobilisideA冻干脂质体的性质。结果:通过工艺优化,制备了以蔗糖为冻干保护剂的nobilisideA冻干脂质体,具有较好的成型性和复溶能力。测得冻干前后nobilisideA脂质体的百分含量分别为108.3%和108.6%,包封率分别为98.4%和97.8%,粒径分别为89.9 nm和115.8 nm,ζ电位分别为-19.9 mV和-15.9 mV。脂质体在葡萄糖输液中8 h内含量、包封率、粒径以及溶血率均无明显变化。结论:所制得的nobilisideA冻干脂质体粒径分布范围窄,包封率高,性质稳定,是一种很有应用前景的nobilisideA脂质体制剂。

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    Objective:To prepare and characterize nobilisideA freeze-dried liposome. Methods: The nobilisideA liposomes were prepared using a film dispersion method followed by a freeze-dried technique. The freeze-dried liposomes were characterized with regard to the drug content, entrapment efficiency, the particle size, ζ potential, and its stability and hemolytic rate in glucose transfusion. Results: Through optimized technique, the prepared nobilisideA freeze-dried liposome, with sucrose as protective agent, had satisfactory structure and redissolubility. The contents of nobilisideA liposome before and after freeze-drying were 108.3% and 108.6%, the entrapment efficiency were 98.4% and 97.8%, the particle sizes were 89.9 nm and 115.8nm, and the ζ potentials were -19.9mV and -15.9mV, respectively. The liposome content, entrapment efficiency, particle size and hemolytic rate were stable within 8 h during glucose transfusion. Conclusion: NobilisideA freeze-dried liposomes have a narrow size distribution range, a high entrapment efficiency and a stable character, making it a promising candidate for nobilisidesA liposome.

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  • 收稿日期:2008-06-20
  • 最后修改日期:2008-12-09
  • 录用日期:2008-12-30
  • 在线发布日期: 2009-02-17
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