A novel long |
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A novel long
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BACKGROUND
Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatment, because of its high potency and broad spectrum. Liposomal doxorubicin (Doxil®) is the first FDA-approved PEG-liposomes of DOX for the treatment of over 600.000 cancer patients, and it can overcome doxorubicin-induced cardiomyopathy and other side effects and prolong life span. The addition of MPEG2000-DSPE could elevate the total cost of the cancer treatment. OBJECTIVE
We intended to prepare a novel DOX liposome that was prepared with inexpensive materials egg yolk lecithin and Kolliphor HS15, thus allowing it to be much cheaper for clinical application. METHOD
DOX liposomes were prepared using the combination of thin-film dispersion ultrasonic method and ammonium sulfate gradient method and the factors that influenced formulation quality were optimized. After formulation, particle size, entrapment efficiency, drug loading, stability, and pharmacokinetics were determined. RESULTS
DOX liposomes was near-spherical morphology with the average size of 90 nm and polydispersity index (PDI) of less than 0.30. The drug loading was up to 7.5%, and the entrapment efficiency was over 80%. The pharmacokinetic studies showed that free DOX could be easily removed and the blood concentration of free DOX group was significantly lower than that of DOX liposomes, which indicated that the novel DOX liposome had a certain sustained-release effect. CONCLUSION
In summary, DOX liposome is economical and easy-prepared with prolonged circulation time.
中文翻译：
背景技术阿霉素（DOX）由于其高效力和广谱性而在癌症治疗中是领先的化学疗法。脂质体阿霉素（Doxil®）是FDA批准的首个DOX PEG脂质体，可治疗60万以上的癌症患者，它可以克服阿霉素引起的心肌病和其他副作用并延长寿命。MPEG2000-DSPE的添加可能会增加癌症治疗的总成本。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制成，因此其在临床上的使用更加便宜。方法采用薄膜分散超声法和硫酸铵梯度法相结合的方法制备DOX脂质体，并优化影响制剂质量的因素。配制后，确定粒径，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，平均大小为90 nm，多分散指数（PDI）小于0.30。载药量高达7.5％，包封率超过80％。药代动力学研究表明，游离DOX很容易被清除，游离DOX组的血药浓度明显低于DOX脂质体，这表明新型DOX脂质体具有一定的缓释作用。结论总而言之，DOX脂质体经济且易于制备，并且循环时间延长。结果DOX脂质体呈近球形，平均大小为90 nm，多分散指数（PDI）小于0.30。载药量高达7.5％，包封率超过80％。药代动力学研究表明，游离DOX很容易被清除，游离DOX组的血药浓度明显低于DOX脂质体，这表明新型DOX脂质体具有一定的缓释作用。结论总而言之，DOX脂质体经济且易于制备，并且循环时间延长。结果DOX脂质体呈近球形，平均大小为90 nm，多分散指数（PDI）小于0.30。载药量高达7.5％，包封率超过80％。药代动力学研究表明，游离DOX很容易被清除，游离DOX组的血药浓度明显低于DOX脂质体，这表明新型DOX脂质体具有一定的缓释作用。结论总而言之，DOX脂质体经济且易于制备，并且循环时间延长。药代动力学研究表明，游离DOX很容易被清除，游离DOX组的血药浓度明显低于DOX脂质体，这表明新型DOX脂质体具有一定的缓释作用。结论总而言之，DOX脂质体经济且易于制备，并且循环时间延长。药代动力学研究表明，游离DOX很容易被清除，游离DOX组的血药浓度明显低于DOX脂质体，这表明新型DOX脂质体具有一定的缓释作用。结论总而言之，DOX脂质体经济且易于制备，并且循环时间延长。 |
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