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首页> 外文期刊>Pharmaceutical Nanotechnology >A Novel Long-circulating DOX Liposome: Formulation and Pharmacokinetics Studies | Bentham Science
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A Novel Long-circulating DOX Liposome: Formulation and Pharmacokinetics Studies | Bentham Science

机译：一种新型长循环DOX脂质体：制剂和药代动力学研究| Bentham Science.

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摘要

Background: Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatmentbecause of its high potency and broad spectrum. Liposomal doxorubicin (Doxil?) is the firstFDA-approved PEG-liposomes of DOX for the treatment of over 600,000 cancer patients, andit can overcome doxorubicin-induced cardiomyopathy and other side effects and prolong lifespan. The addition of MPEG2000-DSPE could elevate the total cost of cancer treatment.Objective: We intended to prepare a novel DOX liposome that was prepared with inexpensivematerials egg yolk lecithin and Kolliphor HS15, thus allowing it to be much cheaper for clinicalapplication.Methods: DOX liposomes were prepared using the combination of thin-film dispersion ultrasonicmethod and ammonium sulfate gradient method and the factors that influenced formulationquality were optimized. After formulation, particle size, entrapment efficiency, drug loading,stability, and pharmacokinetics were determined.Results: DOX liposomes were near-spherical morphology with the average size of 90 nm andpolydispersity index (PDI) of less than 0.30. The drug loading was up to 7.5%, and the entrapmentefficiency was over 80%. The pharmacokinetic studies showed that free DOX could beeasily removed and the blood concentration of free DOX group was significantly lower thanthat of DOX liposomes, which indicated that the novel DOX liposome had a certain sustainedreleaseeffect.Conclusion: In summary, DOX liposome is economical and easy-prepared with prolonged circulationtime.Lay Summary: Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatment becauseof its high potency and broad spectrum. Liposomal doxorubicin (Doxil?) is the first FDAapprovedPEG-liposomes of DOX to treat over 600.000 cancer patients, overcoming doxorubicin-induced cardiomyopathy and other side effects and prolonging life span. The addition ofMPEG2000-DSPE could elevate the total cost of cancer treatment. We intend to prepare a novelDOX liposome prepared with inexpensive materials egg yolk lecithin and Kolliphor HS15, thusallowing it to be much cheaper for clinical use. The novel DOX liposome is economical andeasy-prepared with prolonged circulation time.
机译：背景：阿霉素（Doxorubicin，DOX）因其高效性和广谱性而成为癌症治疗中的主要化疗药物。脂质体阿霉素（多柔比星？）是FDA批准的首个用于治疗60多万癌症患者的聚乙二醇阿霉素脂质体，它可以克服阿霉素诱导的心肌病和其他副作用，延长寿命。MPEG2000-DSPE的加入可能会提高癌症治疗的总成本。目的：我们打算制备一种新型的DOX脂质体，该脂质体由廉价的蛋黄卵磷脂和Kolliphor HS15制备，从而使其在临床应用中更便宜。方法：采用薄膜分散超声法和硫酸铵梯度法制备DOX脂质体，并对影响处方质量的因素进行优化。处方后，测定粒径、包封率、载药量、稳定性和药代动力学。结果：DOX脂质体呈近球形，平均粒径90nm，多分散指数（PDI）小于0.30。载药量达7.5%，包封率达80%以上。药代动力学研究表明，游离DOX组的血药浓度明显低于DOX脂质体，表明新型DOX脂质体具有一定的持续释放作用。结论：综上所述，DOX脂质体制备简单、经济、循环时间长。综述：阿霉素（DOX）因其高效性和广谱性而成为癌症治疗中的主要化疗药物。脂质体阿霉素（多柔比星？）是第一个FDAapprovedPEG脂质体，用于治疗60多万癌症患者，克服阿霉素诱导的心肌病和其他副作用，延长寿命。MPEG2000 DSPE的加入可能会提高癌症治疗的总成本。我们打算用廉价材料蛋黄卵磷脂和Kolliphor HS15制备novelDOX脂质体，从而使其在临床上更便宜。新型DOX脂质体经济、制备简单、循环时间长。

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  • 来源
    《Pharmaceutical Nanotechnology》 |2020年第5期|共8页
  • 作者

    Peihong Xiao; Juan Zhao; Yi Huang; Rongrong Jin; Zhonglan Tang; Ping Wang; Xu Song; Hongfei Zhu; Zibin Yang; Nie Yu;

  • 作者单位

    College of Pharmacy and Chemistry Dali University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

    Beibei Traditional Chinese Medical Hospital;

    College of Pharmacy and Chemistry Dali University;

    Institute of Regulatory Science for Medical Devices National Engineering Research Center for Bio-materials Sichuan University;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 制药化学工业;
  • 关键词

    DOX liposome; drug loading; entrapment efficiency; Kolliphor HS15; particle size; pharmacokinetics;

    机译：dox脂质体;药物载荷;夹带效率;kolliphor hs15;粒度;药代动力学;

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